Proceedings of the PSK Conference (대한약학회:학술대회논문집)
The Pharmaceutical Society of Korea
- 기타
Domain
- Health Sciences > Development of Pharmaceutical
2003.10b
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Organic compounds play an important role in the area of pharmaceutical, agrochemical, and other materials, which possess useful biological activities. Generally, such biological activities are come from the interaction of the organic compounds with the receptors in biological system, such as enzymes. Such receptors are composed of the chiral building blocks such as amino acid or carbohydrate, which means the biological active sites of receptors are chiral. (omiited)
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General headache is one of the most frequently encountered diseases to the clinical pharmacists. In this study, we examined the correlation between the type and frequency of headaches and the characteristics of patients and individual preferences of specific treatment for the relief of headache. This study analyzed the questionnaires from the 229 patients, who are 18years over and had experienced headache more than once per month and had used pharmacy for the relief of their headache.As Results, the average duration time and severity of the headache pain was sex-dependent in the patients that female patients showed longer duration and stronger severity than male patients (p=0.007). (omitted)
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Natural benzo[c]phenanthridine and protoberberine alkaloids which have been attractive to synthetic organic chemists and biochemists over the last 2 decades since such compounds have shown interesting biological properties such as antitumor, antiviral and antimicrobacterial activities. For the systematic research on these alkaloids, several total syntheses of these alkaloids have been reported. However, the bulk of reported benzo[c]phenanthridine synthetic studies to date have involved multistep sequences for assembly of the target molecules as well as lack of generality for synthesizing substituted molecules. (omitted)
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88 selective COX-2 inhibitors belonging to three chemical classes (triaryl rings, diaryl cycloalkanopyrazoles, and diphenyl hydrazides) were studied using comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA). Partial least squares analysis produced statistically significant models with q values of 0.84 and 0.79 for CoMFA and CoMSIA, respectively. The key spatial properties were detected by careful analysis of the isocontour maps. The binding energies calculated from flexible docking correlated with inhibitory activities by the least-squares fit method. (omitted)
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Suh, Young-Ger;Seo, Seung-Yong;Paek, Seung-Mann;Jung, Jae-Kyung;Han, Young-Taek;Kim, Seok-Ho 65.3
Bacillariolide III was isolated from the culture medium of the marine diatom, Pseudonitzschia multi series, a causative organism of amnesic shellfish poisoning by Shimizu et al. This extracellular metabolite features bicyclic system of hydroxycyclopentane and (Z)-pentenoic acid-bearing lactone ring. Bacillariolide I is known to possess significant inhibitory activity against phospholipase A$_2$ , but the biological function of bacillariolide III is still under investigation. The unique structural feature as well as the promising biological activity led us to the total synthesis of bacillariolide III. (omitted) -
Rhizomes of Polygonatum species belong to Liliaceae are important herbal drugs in the traditional medical practice of Asian region. Two representative Chinese drugs derived from this genus are Hwangjeong and Okjuk. Though botanical origins of these drugs are officially listed as P. falcatum, P. sibiricum and P. kingianum for Hwangjeong and P. odoratum var. pluriflorum for Okjuk in the Korean Pharmacopoeia and Korean Herbal Pharmacopoeia, respectively, they are often sold as a mixture of several different species in the market. (omitted)
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Han, Ah-Reum;Kim, Hyang-Rim;Min, Hye-Young;Windono, Tri;Jeohn, Gwang-Ho;Lee, Sang-Kook;Seo, Eun-Kyoung 66.2
A new phenylbutenoid dimmer, ( )-trans-3-(3'-methoxy-4'-hydroxyphenyl)- 4- [(E)- 3',4'-dimethoxystyryl] cyclohexene (1), were isolated from the rhizomes of Zingiber cassumunar along with three known phenylbutenoids, ( )-trans-3-(3', 4'- dimethoxyphenyl)-4-[(E)-3'",4"'-dimethoxystyryl]cyclohexene (2), 4-(3' ,4'- dimethoxyphenyl)but-1,3-diene (3) , and 4-(2',4',5'-trimethoxy-phenyl)but-1,3-diene (4), and a known heptanoid, curcumin (7), as cytotoxic constituents against several human cancer cell lines. (omitted) -
Reactive oxygen species are capable of damaging biomolecules such as lipids, proteins, and DNA, which can not only lead to various diseases, but also oxidative damage resulting aging. In our previous study, Cercis chinensis (Leguminosae) showed a potent antioxidant activity. Twenty compounds including a new flavonol glycoside were isolated through antioxidant activity-guided fractionation. C. chinensis and some of the constituents exhibited a potent antioxidant activity on the free radicals and lipid peroxidation and a notable protective effect on the t-BuOOH induced oxidative damage. (omitted)
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Three new guaianolide type of sesquiterpene lactones, 8
${\alpha}$ -angeloyloxy-1${\alpha}$ -hydroxy-3${\alpha}$ ,4${\alpha}$ -epoxy-5${\alpha}$ , 7${\alpha}$ H-10(14), 11(13)-guaiadien-12,6${\alpha}$ -olide (1), 8${\alpha}$ -methylbutyryloxy-1${\alpha}$ -hydroxy-3${\alpha}$ , 4${\alpha}$ -epoxy-5${\alpha}$ , 7${\alpha}$ H-10(14),11(13)-guaiadien-12,6${\alpha}$ -olide (2), and 8${\alpha}$ -isovaleryloxy-1${\alpha}$ -hydroxy-3${\alpha}$ , 4${\alpha}$ -epoxy-5${\alpha}$ , 7${\alpha}$ H-10(14),11 (13)- guaiadien-12,6${\alpha}$ -olide (3), together with six known sesquiterpenes, artemisolide (4), 3-methoxytanapartholide (5), deacetyllaurenobiolide (6), moxartenolide (7), arteminolide B (8), and arteminolide D (9) were isolated by bioassay-guided fractionation using the NF-kB mediated reporter gene assay system. (omitted) -
Shim, Sang-Hee;Ryu, Ji-Young;Kim, Ju-Sun;Kang, Sam-Sik;Chung, Sang-Hun;Lee, Yeon-Sil;Lee, Sang-Hyun;Shin, Kuk-Hyun 67.2
Four new lanostane-type triterpenes were isolated from CH$_2$ Cl$_2$ fraction of Ganoderma applanatum (Polyporaceae). There structures were determined as (20S)-3${\beta}$ , 7${\beta}$ , 20,23ζ-tetrahydroxy-1l,15-dioxolanosta-8-en-26-oic acid, (20S)-7${\beta}$ ,20,23ζ- trihydroxy-3,1l,15-trioxolanosta-8-en-26-oic acid, 7${\beta}$ ,23ζ-dihydroxy-3,11,15- trioxolanosta-8,20E(22)-dien-26-oic acid, and 7${\beta}$ -hydroxy-3, 11,15,23-tetraoxolanosta-8,20E(22)-dien-26-oic acid methyl ester on the basis of spectral data. -
The purpose of this study is to improve repeatability of a non-invasive blood glucose measurement. The portable NIR system that was newly integrated by our lab includes a tungsten halogen lamp, a specialized reflectance fiber optic probe and a photo diode array type InGaAs detector, which was developed by a microchip technology based on the lithography. Reflectance NIR spectra of finger tip were recorded by using a fiber optic probe. The probe was fixed in the system and subjects put their finger on the probe head. (omitted)
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A method for determination 11 endocrine disrupting chemicals of phenols in various samples was deloped. The alkylphenols, chlorophenols and bisphenol A were determined by gas chromatography/mass spectrometry-selected ion monitoring (GC/MS-SIM) followed by two work-up methods for comparison; isobutoxycarbonyl (isoBOC) derivatization method and tert-butyldimethylsilyl (TBDMS) derivatization method. Eleven endocrine disrupting chemicals (EDCs) of phenols in biological samples were extracted with acetonitrile and then acetonitrile layer was refrigerated at -60
$^{\circ}C$ for 2 hours (freezing filtration). (omitted) -
We performed this survey to hear Yeungnam University Graduates' opinion on the current curriculum for the purpose of creating an education system of “practically competent person” instead of simply “competent person”. Questionnaire was made up of 13 multiple-choice questions and 1 descriptive question by Curriculum Reform Task Force of Yeungnam University. The survey was administered to randomly chosen 50 graduates by e-mail on August 1, 2003 and was collected between August 1 and August 10, 2003 for the analysis of respondent’s reply. (omitted)
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Matrix metalloproteinases (MMPs) play an important role in tumor invasion and metastasis by extracellular matrix degradation. To analyze the effect of DA-125, a anthracyclin derivative, on the invasion or metastasis of cancer cells the expression of matrix metalloproteases (MMPs) was investigated in human fibrosarcoma HTl080 cells by RT-PCR or gelatin zymographic methods. As result, DA-125 suppressed the expression of MMP-2 and 9 as well as tissue inhibitor of metalloproteinase-1 (TIMP-1) TIMP-2 and MT1-MMP with a time- and dose-dependent manner. Inaddition, DA-125 inhibited cancer cell migration and colony formation, and also exhibited the inhibitory activities of invasion and motility with a matrigel and type I collagen assay. (omitted)
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Fumonisins are a family of mycotoxins produced from Fusarium verticillioides. Most of fumonisin B1 (FB1) toxicities can be explained by its ability to alter sphingolipid metabolism by inhibiting ceramide synthase. At least, the elevation in dihydrosphingosine (DHS) mediates the earliest toxicity of FB1. Some tissues such as kidney and liver, may be most affected by FB1 because they shows high rates of de novo sphingolipid synthesis. Recent review on FB1 toxicity by A.H. Merrill Jr. et al. suggested the possible role of dihydrosphingosine 1-phosphate (dihydroS1P), which sometimes elevated in cell- or tissue specific manners. (omitted)
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The purpose of this study is to examine whether the efflux system for taurine from brain to blood is present on the blood-brain barrier (BBB) using the brain efflux index (BEl) method and taurine transport system is regulated by CNS cell damage with oxidative stress agent such as diethyl maleate (DEM) or tumor necrosis factor-
${\alpha}$ (TNF-${\alpha}$ ) in vivo. [$^3$ H]Taurine was microinjected into parietal cortex area 2 (Par2) of the rat brain, and was eliminated from the brain with efflux transport rate of 1.22 10$\^$ -2//min, and the process is saturable with a$K_{m}$ of 43.5${\mu}$ M. (omitted) -
A substantial body of evidence indicates that reactive oxygen intermediates (ROIs) are implicated in pathogenesis of diverse human diseases, including cancer, diabetes and neurodegenerative disorders. Oxidative stress induced by ROIs often causes cell death via apoptosis that is regulated by a plenty of functional genes and their protein products. In the present work, we have investigated the role of bcl-2 in protecting against oxidative death induced by hydrogen peroxide in cultured rat pheochromocytoma (PC12) cells. (omitted)
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Chun, Kyung-Soo;Park, Kwang-Kyun;Chung, Won-Yoon;Kim, Su-Hyeong;Song, Yong-Sang;Surh, Young-Joon 70.1
Celecoxib, the selective cyclooxygenase-2 (COX-2) inhibitor, has recently been reported to reduce the formation of polyps in patients with familial adenomatous polyposis. This specific COX-2 inhibitor also protects against experimentally induced carcinogenesis, but molecular mechanisms underlying its chemopreventive activities remain largely unresolved. In the present work, we found that celecoxib inhibited 12-O- tetradecanoylphorbol-13-acetate (TPA)-induced expression of COX-2 in female ICR mouse skin when applied topically 30 min prior to TPA as determined by both immunoblot and immunohistochemical analyses. (omitted) -
Quinolone resistance in Streptococcus pneumoniae is related to mutations in the DNA gyrase and topoisomerase IV genes. DW-286a displayed potent activity against S. pneumoniae C9211 (MIC, 0.015
${\mu}$ g/ml) compared with gemifloxacin (MIC, 0.06${\mu}$ g/ml). This study was performed to analyze the ability of DW-286a to cause resistance development in S. pneumoniae and to establish whether DNA gyrase or topoisomerase IV is primary target. DW-286a resistant mutants of S. pneumoniae C9211 were generated by stepwise selection at increasing drug concentration. (omitted) -
We show that Cdc6, an essential initiation factor for DNA replication, undergoes caspase-3-mediated cleavage in the early stages of apoptosis in HeLa cells and SK-HEP-1 cells induced by etoposide, paclitaxel, ginsenoside Rh2, or TRAIL. The cleavage occurs at the SEVD
$\^$ 442//G motif and generates an N-terminal truncated Cdc6 fragment (p49-tCdc6) that lacks the carboxy-terminal nuclear export sequence (NES). Cdc6 is known to be phosphorylated by cyclin A-Cyclin A-dependent kinase 2 (Cdk2), an event that promotes its exit from the nucleus and probably blocks it from initiating inappropriate DNA replication. (omitted) -
This presentation is to enhance the pharmacist's role in Over-The-Counter(OTC) drug selection and patient counseling for diversification of pharmacy management after the separation of prescribing and dispensing practice in Korea. Self-medication by OTC drugs may be viewed as one element of the broader self-care treatment. The patient may use a OTC drug to manage a minor ailment, a process that may be supported by counseling from a pharmacist. Pharmacists involved in self-medication decisions have a greater involvement with patients and an enhanced professional role. (omitted)
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The use of auxiliary labels in many advanced countries has shown that patients and caregivers understanding, safety and compliance with proper administration of medication is significantly increased. Although in Korea we give required information orally and written on the packaging when we dispense medication, many international studies have demonstrated a marked increase in full compliance when auxiliary labels were used. The pharmacist must insure that the patients understand how to take correctly in order to get the maximum effect of treatment. (omitted)
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Lifestyle change in the world is spawning an epidemic of Global Obesity. (Newsweek August 11. 2003) People with overweight are at great risk of developing Type II diabetes. The A1C value provides an objective assessment of glucose control over the previous six to eight weeks. The American Diabetes Association recommended values for blood glucose and A1C appear in TABLE 4. In case one who was found to have >7% HbA1C, he(she) may be a patient with pre-DM or DM II. (omitted)
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Low-frequency electrical field stimulation of transmural nerves of cat esophageal circular smooth muscle produces an “off contraction”, which occurs after electirical field stimulation (EFS) of transmural nerves is stopped. We previously examined signal transduction pathways mediating ACh-induced contraction of circular smooth muscle of esophagus. The extracellular Ca
$\^$ 2+/ is needed for the contraction, results in the activation PKC. EFS-induced contraction was abolished by the pretreatments of tetrodotoxin(1${\mu}$ M) and atropine (1${\mu}$ M). (omitted) -
The present study was designed to compare the effects of conotoxin GVIA, a selective blocker of N-type voltage-dependent calcium channels (VDCC) and cilnidipine, a blocker of both L- and N-type VDCC, on the secretion of catecholamines (CA) evoked by cholinergic stimulation and membrane-depolarization in the isolated perfused rat adrenal gland, and also to establish the mechanism of action. 1. The inhibition of the CA secretory response evoked by acetylcholine (5.32 x 10
$\^$ -3/${\mu}$ M) was stronger in cilnidipine-treated glands than in conotoxin GVIA-treated glands. (omitted) -
The present study was performed to examine mitogen-activated protein kinase associated pathways in mediation of 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD)-induced cell apoptosis in cultured Jurkat T cells. TCDD significantly decreased cell viability in a concentration-dependent manner (p<0.05 at 10-300 nM). TCDD (10 nM) also time-dependently decreased cell viability (p<0.05 at 12-48 h). c-Jun NH
$_2$ -terminal kinase was significantly phosphorylated with TCDD treatment in a time dependent manner. (omitted) -
The influence of melatonin on carrageenan-induced paw edema in Sprague-Dawley rats has been studied. The injection of 1% carrageenan (given at 0.1ml/paw) into the intraplantar induced an inflammatory response, and the maximal increase of paw volume, edema, was observed at 4hour. The levels of nitric oxide (NO), malondialdehyde (MDA) or prostaglandin E
$_2$ (PGE$_2$ ) were increased after edema generation. Also, the expression of the inducible NO synthase (iNOS) were increased in the western blot. (omitted) -
Although sphingosine-1-phosphate (S1P) is a well-known mitogen, our results show that S1P potently inhibits keratinocyte proliferation, and that this leads the inhibition of DNA synthesis. Interestingly, the prolonged activation of extracellular signal-regulated protein kinase (ERK) and the transient inactivation of Akt/protein kinase B (PKB) were also oberved in concert with the inhibition of keratinocyte proliferation by S1P. To further verify the anti-proliferative action of S1P, we examined changes in cell cycle related proteins. (omitted)
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Kim, Eun-Joo;Kim, Ki-Suk;Shin, Won-Ho;Seo, Joung-Wook;Choi, Gyu-Kap;Park, Eun-Kyung;Hwang, Ji-Yoon;Han, Sang-Seop 77.1
Prolongation of the QT interval may result in a potentially dangerous arrhythmia. The most commonly proposed mechanism for QT interval prolongation(LQT) by pharmaceuticals is inhibition of the rapid delayed rectifier potassium channel (I$\sub$ Kr). The LQT potency of pharmaceuticals can be effectively evaluated by examining the effect on human ether-a go-go-related gene (hERG) channels expressed in CHO cells, known to be equal to I$\sub$ kr/. We have transfected JERG into CHO cell lines transiently to express high levels of functional hERG channels. (omitted) -
The dopamine D2 receptor (D
$_2$ R) is target for antipsychotic drugs and associated with several neuropsychiatric disorders. The internalization (sequestration) of G protin-coupled receptor is caused by agonist-induced receptor phosphorylation mediated by GRK, followed by the interaction with${\beta}$ -arrestin. In this study, we examined the agonist-dependent sequestration/internalization of dopamine D$_2$ R, which were transiently expressed in HEK 293 cells with of without GRK co-expression. Co-expression of GRK2 or GRK3 markedly enhanced the sequestration of D$_2$ R. (omitted) -
We previously shown that sphingosylphosphorylcholine, a lysophosphatidic acid, produced contraction in isolated single cells of cat ilium. We investigated the mechanism of sphingosine-1-phosphate (S1P)-induced contraction of circular smooth muscle cells in cat esophagus. S1P produced esophageal contraction in a dose dependent manner. The maximal contraction (l0
$\^$ -7/ M) induced at 1min. Pertusis toxin (PTX) inhibited contraction induced by S1P, suggesting that the contraction is mediated to a PTX-sensitive G-protein. (omitted) -
Sauchinone, a known lignan, was isolated from the root of Saururus chinensis as an active principle responsible for inhibiting the production of NO in LPS-stimulated RAW264.7 cells by activity-guided fractionation. Sauchinone dose-dependently inhibited not only the production of NO, but also the expression of iNOS mRNA and protein in LPS-stimulated RAW 264.7 cells. Furthermore, sauchinone prevented LPS-induced NF-kB activation, which is known to play a critical role in iNOS expression, assessed by a reporter assay under the control of NF-kB. (omitted)
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We have previously reported that green tea catechins (GTC) displayed anti-thrombotic activity, and that this might be due to anti-platelet rather than anti-coagulation effects. In the present study, we have studied the anti-platelet activity and mechanism of gallocatechin gallate (GCG), which is a component of GTC. GCG inhibited the collagen- and U46619-induced aggregation of rabbit platelets, with IC
$\^$ 50/ values of 63.0 and 48.3${\mu}$ M, respectively. GCG also inhibited collagen-induced serotonin release and TxB$_2$ formation in a similar manner of platelets aggregation. (omitted) -
Dongchunghacho (Dong-Chong-Xia-Cho in Chinese) is one of entomogenous fungi that grow as parasites mainly to pupae or larvae. It includes many different genera such as Cordyceps, Paecilomyces, Torrubiella and Podonectria. The ethanolic extract of Cordyceps scarabaeicola, prepared from its fruiting bodies, showed significant inhibitory activity on angiogensis, which was detected by chick embryo chorioallantoic membrane (CAM) assay. The ethanolic extract of media-cultured Paecilomyces japonica also showed significant anti-angiogenic activity in CAM assay. (omitted)
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Aster scaber T. (Asteraceae) has been used in traditional Korean and Chinese medicine to treat bruises, snakebites, headaches and dizziness. (-) 3,5-Dicaffeoyl-muco-quinic acid (DQ) isolated from Aster scaber induced neurite outgrowth in PC12 cells. It has been reported that the activation of the extracellular signal regulated kinase1/2 (Erk 1/2) and phosphoinositide 3 (P13) kinase plays a crucial role in the NGF-induced differentiation of PC12 cells. This study showed that the effect of DQ on neurite outgrowth is mediated via the Erk 1/2 and PI3 kinase-dependent pathways like NGF. (omitted)
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Minocycline is known to protect neurons from microglia-mediated cell death in many experimental models of brain diseases including ischemic stroke, Huntington's disease (HD), amyotrophic lateral sclerosis (ALS), traumatic brain injury, multiple sclerosis, and Parkinson's disease. Activation of caspase-2, 3, 8, and 9 was evident within 2-8 hr following oxidative insult with 0.5 mM hydrogen peroxide in PC12 cells. Minocycline significantly attenuated activation of these caspases up to 18 hr, resulting a significant increase in cell viability as assessed by MTT assay. (omitted)
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Jin, Chun-Mei;Lee, Jae-Joon;Kim, Yu-Mi;Yang, Yoo-Jung;Kang, Min-Hee;Rhu, Shi-Yong;Lee, Myung-Koo 79.3
The effects of anonaine, an aporphine isoquinoline alkaloid, on dopamine biosynthesis and L-DOPA-induced neurotoxicity in PC12 cells were investigated. Treatment of PC12 cells with 0.05${\mu}$ M anonaine showed a significant inhibition of dopamine content. The IC$\sub$ 50/ value of anonaine was 0.05${\mu}$ M. Under the same conditions, 0.05${\mu}$ M anonaine also inhibited tyrosine hydroxylase (TH) activity at 24 h (62.0% inhibition of the control level). TH mRNA levels were also decreased by the treatment with anonaine. (omitted) -
Intestinal epithelial cells can produce cytokines and chemokines that play an important role in the mucosal immune response. Regulation of this production is important to prevent inflammatory tissue damage. Glycyrrhiza glabra has been shown to inhibit inflammation. The aim of this study was to examine the inhibitory effect of 18- beta-glycyrrhetinic acid, a triterpenoid saponin of Glycyrrhiza glabra, on IL-S production via mitogen-activated protein kinases (MAPKs) and nuclear factor-kappa B (NF-kB) in TNF-alpha-stimulated human colon epithelial cells. (omitted)
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The nucleoside analogue, L-FMAUS was synthesized from L-FMAU which has been shown to have significant antiviral acitivity against hepatitis B virus (HBV). The anti-HBV activity and toxicity of the L-FMAUS were examined by a cell culture system using a hepatitis B virus (HBV) producing cell line, HepG2 2.2.15. L-FMAUS was assayed for the inhibition of HBV multiplication by measurement of HBV DNA and surface antigen (HBsAg) levels in the extracellular medium of HepG2 2.2.15 cells after an 8-day treatment. (omitted)
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Nitric oxide (NO) has been reported to play an important role as an effector molecule in cytokine signal transduction in cardiomyocytes. The treatment of IL-1b/ TNF-a (2 ng/ml)/ IFN-g (50 U/ml) induced apoptosis in neonatal rat ventricular cardiomyocytes via NO-dependent pathway. When cardiomyocytes were treated with IL-1b (20 ng/ml)/TNF-a (2 ng/ml)/ IFN-g(50 U/ml) in the presence of catalase, the cells were much more resisant to the cell death as well as NO synthesis. However, catalase significantly enhanced the expression of iNOS protein in cardiomyocytes. (omitted)
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Ahn, Mee-Ryung;Yoo, Tae-Moo;Sohn, Soo-Jung;Park, In-Sook;Suh, Soo-Kyung;Yang, Ji-Sun;Choi, Hong-Serck 81.1
Buprenorphine(BPN) is used to treat withdrawal syndromes in narcotic addictions. When narcotics are stopped, withdrawal syndromes such as pupil dilation and blood pressure increment are appeared. And BPN is often prescribed concomitantly with antihypertensives. We researched whether combined medicines of BPN and antihypertensives affected on the metabolism of BPN. After BPN was incubated with antihypertensives such as nifedipine, verapamil, captopril and propranolol in rat or human microsomes, amounts of BPN and its metabolite, norbuprenorphine (NBPN), were measured. (omitted) -
Pyroligneous liquid is produced by process carbonizing Oak in 350 ∼ 400 . There are 200 kinds of constituents including minerals, vitamin B-complex and organic acids in it. The organic acids of them were presumed as active materials. It is traditionally used for treatment of stress related disorder, hepatic disease, immune disorder, G-I disorder and inflammatory disease. The aim of this study was to investigate anti-stress effects of Pyroligneous liquid(Pyroligneous liquid produced from Choa company). (omitted)
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The protective adaptive response to electrophiles and reactive oxygen species is mediated by enhanced expression of phase II detoxifying genes including glutathione S-transferases.
${\alpha}$ -Lipoic acid, which exerts prooxidant or antioxidant activities, has been shown to activate the insulin signaling pathway and thus to induce insulin-like actions via PI3-kinase and Akt. Our previous studies have shown that PI3-kinase plays an essential role in Nrf2-or C/EBP${\beta}$ -mediated glutathione S-transferase A2 (GSTA2) induction. (omitted) -
Lee, Sun-Young;Lee, Seung-Ho;Son, Dong-Ju;Kim, Su-Jin;Ha, Tae-Youl;Yun, Yeo-Pyo;Oh, Ki-Wan;Hong, Jin-Tae 82.2
Beta-amyloid peptide (A${\beta}$ ) is considered to be responsible for the pathogenesis of the Alzheimer's disease. Several lines of evidence support that A${\beta}$ -amyloid-induced cytotoxicity is mediated through the generation of reactive oxygen species (ROS). Agents that are able to scavenge excess ROS may be useful as protecting or reducing agents for development or progress of AD. Green tea extract has been known to have antioxidant property. Our previous studies also demonstrate that green tea extract protected ischemia/reperfusion-induced brain injury by reduction of cell death through scavenging of oxidative damages of macromolecules. (omitted) -
The heterotrimeric G protein subunits (G ) are region-specifically expressed in brain such as hypothalamus and pituitary gland in abundant, suggesting that is may be associated with “stress-axis”. This study was designed to examine the effect of stress on the region-specific expression of various G subunits in rat brain. The localization of mRNAs encoding seven of G and striking region-specific patterns of expression were observed in 12 different regions of both non-stressed and stressed rat brain; (1) frontal cortex area, (2) cerebral cortex area, (3) striatum, (4) hippocampus area, (5) thalamus, (6) brain stem, (7) cerebellum area, (8) hypothalamus, (9) septum, (10) amygdala, (11) preoptic area, and (12) pituitary gland. (omitted)
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It has been demonstrated the presence of leptin receptors (Ob-Ra) on epinephrine-secreting chromaffin cells in rat adrenal medulla, suggesting that leptin may directly affect the adrenal medulla (Cao et al., 1997). Leptin is found to stimulate catecholamine (CA) synthesis in cultured bovine adrenal medullary cells (Utsumomiya et al., 2001; Shibuya et al., 2002)and cultured porcine adrenal medullary cells (Takekoshi et al., 2001). Thus, the present study was designed to examine the effect of leptin on CA release from the isolated perfused rat adrenal gland, and to establish its mechanism of action. (omitted)
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Kim, Kyung-In;Yoo, Ji-Hoon;Cho, Jae-Han;Im, Ki-Dong;Lee, Seok-Yong;Lee, Sun-Bok;Jang, Choon-Gon 84.1
Methamphetamine is a powerful stimulant that appears to produce locomotor activity and behavioral sensitization. Previous study has indicated that dopaminergic receptors are implicated in the behavioral responses of methamphetamine. Recently, it has been reported that other receptors, especially, M1 muscarinic acetylcholine receptor (M1R) plays an important role in the regulation of behavioral responses, and this receptor is abundantly expressed in brain regions, including the cerebral cortex, striatum, and the hippocampus of the animal. (omitted) -
The number of patients suffering from atrial fibrillation is increasing and many cardiologists is trying to develop the ideal antiarrhythmic drugs for atrial fibrillation. An ideal antiarrhythmic agent would selectively prolong the action potential duration more in extraordinarily depolarized cardiac myocytes than in normal cells, and show tissue selectivity. Voltage-gated K
$\^$ +/ (Kv) channels represent a structurally and functionally diverse group of membrane proteins. These channels play an important role in determining the length of the cardiac action potential and are the targets for antiarrhythmic drugs. (omitted) -
Shim, Young-Hoon;Choi, Jung-Ho;Park, Chan-Dong;Lim, Chul-Joo;Kim, Do-Hun;Cho, Jung-Hee;Kim, Hong-Jin 85.1
Previously, we found the operon random primer (OP-5A) that is characteristic the genus Panax by randomly amplified polymorphic DNA (RAPD) analysis. However, OP-5A primer is limited to apply on the differentiation of only crude herbal plants. To construct more sensitive and unique primers on the genus Panax, ginseng-specific DNA profile (350 bp) that was amplified by OP-5A primer were inserted in a plasmid vector in the TA cloning method and sequenced. We designed the PCR primers (Forward: 5"-AGGGGTCTTGCTAT AGCGGAAC-3", Reverse: 5"-AGTCTTAATTTCATATTTTCGTATG-3") and identified the unique ginseng band (350 bp) in commercial granule products including ginseng extracts as well as crude ginseng plants by nascent PCR.(omitted) -
Effects of
$\beta$ -carbolines on Dopamine Biosynthesis and L-DOPA-Induced Cytotoxicity in PC12 CellsYang, Yoo-Jung;Lee, Jae-Joon;Kim, Yu-Mi;Jin, Chun-Mei;Yoo, Seung-Hee;Kang, Min-Hee;Lee, Myung-Koo 85.2
In vivo aromatic${\beta}$ -carbolines, such as harman and norharman, may easily be formed by cyclization of indoleamines with e.g. aldehydes. Because of the structural similarity to MPTP,${\beta}$ -carbolines have been proposed as endogenous toxins. In this study, we have investigated the effects of harman and norharman on dopamine biosynthesis and L-DOPA-induced cytotoxicity in PC12 cells. Treatment of PC12 cells with harman and norharman showed 48.8% and 49.5% inhibition of dopamine content at a concentration of 20${\mu}$ M and 100${\mu}$ M for 48h. (omitted) -
Oltipraz, a cancer chemopreventive agent, induces CYP1A1 to a certain extent by transactivation of the gene via the Ah receptor (AhR)-xenobiotic response element (XRE) pathway. Previously, we showed that oltipraz promoted CCAAT/enhancer binding protein (C/EBP ) activation, which leads to the induction of glutathione S-transferase. Given that oltipraz activates C/EBP for gene transactivation and that the putative C/CBP binding site is located in CY)1A1 promoter region, this study investigated the effect of oltipraz on CYP1A1 induction by 3-methylcholanthrene (3-MC). (omitted)
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High-dose extracts from artichoke leaves are traditionally used for treatment of stress related disorder, that is, hepatic disease, dyspeptic disorder, hyperlipidemic disorder and diuretic disorder. The aim of this study was to investigate anti-stress effects of Artichoke extract(Archoke juice produced from Choa company). The experiments were performed with the use of young(6-8 weeks of age) male mice of ICR stain weighing between 20 and 25 g at the time of first treatment with Archoke juice. The were grouped normal, control, Ginseng, diazepam and Arcoke juice group. (omitted)
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Introduction: Liver fibrosis is defined unbalance of collagen metabolism, especially a stimulation of collagen synthesis and inhibition of collagen degradation, and antifibrotic effect is delaying or inhibition of new collagen synthesis and deposition in liver tissue. In this study, we investigated the antifibrotic and antioxidative effect of Solanum lycopersicum (SL) in liver fibrosis induced rats. Methods: : Rats were randomly divided in three groups (normal, CCl
$_4$ and CCl$_4$ -SL group) and were received 0.6 ml mixture of CCl$_4$ and olived oil (1:1 v/v) 3 times/week for 4 weeks except of the normal group. (omitted) -
Kim, Eun-Joo;Seo, Joung-Wook;Choi, Gyu-Kap;Park, Eun-Kyung;Kim, Ki-Suk;Shin, Won-Ho;Han, Sang-Seop 87.1
With the issuance of the ICH “Guidance for industry S7A Safety Pharmacology Studies For Human Pharmaceuticals” in July 2001 came the preference for the use of unanesthetized animals when evaluation the safety profile of new pharmaceutical agents. Telemetry provides a means of obtaining measurements of physiological functions in conscious animals without the problems associated with classical cardiovascular measuring methods. The Korea Institute of Toxicology (KIT) established the telemetric measurement of cardiovascular parameters, such as Blood pressure, Heart rate, ECG (PR, RR, QRS, QT and QTcB interval) under GLP conditions. (omitted) -
The present study was conducted to investigate the effects of pinacidil, a potassium channel opener, on arterial blood pressure, catecholamine release and vascular contractile responses in the normotensve rats and to establish the mechanism of action. Phenylephrine (an adrenergi
$_1$ -receptor agonist) and high potassium (a membrane- depolarizing agent) caused greatly contractile responses in the isolated aortic strips, respectively. These phenylephrine (10$\^$ -5/ M)-induced contractile responses were dose-dependently depressed in the presence of pinacidil (25 ∼ 100${\mu}$ M). (omitted) -
Park, Hyun-Jung;Kang, Hye-Jung;Chung, Young-Mee;Chun, Hyung-Ok;Hong, Kwang-Hee;Kim, Il-Hwan;Kim, Taek-Rho;Noh, Hyun-Jung;Kim, Deog-Yeor 88.1
CJ-11668 is a new potent and selective COX-2 inhibitor (IC$\sub$ 50/ COX-2 65nM; COX-l/COX-2 ratio 770). The pharmacokinetic profile of CJ-11668 (20 mg/kg, p.o.) in the rat was characterized by high bioavailability (90%) and long plasma half-life (11.7 hr) with low clearance (0.4 L/hr/kg). In the dog, the PK profiles (2 mg/kg, p.o.) also showed long plasma half-life (l7.9hr) with low clearance (0.5 L/hr/kg), and the bioavalability of 60%. The inhibition of CJ-11668 infive different cytochrome P450 isozymes (1A2, 2C9, 2C19, 2D6 and 3A4) was determined in vitro and had observed no significant effect. (omitted) -
Ascorbic acid (vitamin C) has been shown to have anti-cancer actions. However, the exact mechanism of this action is not fully understood. In this study we investigated the possible mechanism of anti-cancer action of ascorbic acid in HepG2 human hepatoblastoma cells. Ascorbic acid induced apoptotic cell death in a dose-dependent manner in the HepG2 cells, assessed by the flow cytometric analysis of hypodiploid nuclei stained with propodium iodide. In addition, ascorbic acid increased intracellular Ca
$\^$ 2+/ concentration, whereas the level of reactive oxygen species was not significantly changed, suggesting that ascorbic acid may not alter cellular redox potential in the cells. (omitted) -
Kang, Ok-Hwa;Tae, Jin;Choi, Yeon-A;Kwon, Dong-Yeul;Kim, Yun-Kyung;Cai, Xing-Fu;Kim, Young-Ho;Bae, Ki-Hwan;Lee, Young-Mi 88.3
Acanthoic acid (AA) is a pimaradiene diterpene isolated from the Korean medicinal plant, Acanthopanax koreanum (Araliaceae), which has been traditionally used as a tonic and sedative as well as in the treatment of rheumatism and diabetes in korea. Proteinase-activated receptor-2 (PAR-2) agonist trypsin plays a role in inflammation, and human leukemic mast cells (HMC-l) express PAR-2. In the present study, the effect of acanthoic acid on production of tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$ ) and tryptase in trypsin-stimulated HMC-1 was examined. (omitted) -
The signaling pathway of dopamine D
$_2$ receptor was studied using yeast two-hybrid system. The 3rd cytoplasmic loop of rat D$_2$ receptor was fond to interact with ALY. The interaction in the yeast was observed only with the 3rd cytoplasmic loop of D$_2$ receptor but not with that of D$_3$ or D$_4$ dopamine receptor. The interaction between two proteins was also confirmed by GST pull-down assay. Co-expression of D$_2$ receptor and ALY enhanced the expression of Lef-1 promoter in C6 cells and the promoter of D$_2$ dopamine receptor itself. -
Ral GDP dissociation stimulator (Ral GDS) has been found to be an effector protein of Ras, and Ral, a member of small GTP-binding protein (G protein) superfamily, has been suggested to act downstream of Ras. Ral GDP dissociation stimulator-like (RGL) shares 50% amino acid identity with Ral GDP dissociation stimulator, and assumed to possess similar functional role. Using yeast two-hybrid screening, we found that dopamine D3 receptor interacts with RGL. Since RGL is known to regulate the expression of c-fos promoter, effects of D3R on gene expression of c-fos promoter was studied. (omitted)
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This study shows that sphingosine-1-phosphate (S1P) significantly inhibits melanin synthesis in a concentration-dependent manner, and that the activity of tyrosinase was also reduced in S1P-treated cells. In contrast, a specific extracellular signal-regulated protein kinase (ERK) pathway inhibitor, PD98059 increased tyrosinase activity and melanin production, and PD98059 restored the reduced tyrosinase activity and pigmentation induced by SIP. We also found that S1P induces the sustained activation of ERK and the subsequent degradation of microphthalmia-associated transcription factor (MITF), which plays a key role in melanogenesis. (omitted)
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In a continuous effort to develop novel anticancer agents we newly synthesized and evaluated the antitumor activity of nucleoside analogues. One analogue, 4-[2-Chlor-6-(3-iodo-benzylamino)-purin-9-yl]-2,3-dihydroxy-cyclopentanecarboxylic acid methylamide (LJ-331), has been shown to exert a potent inhibition of human cancer cell growth in vitro including human lung (A549), stomach (SNU-638) and leukemia (HL-60) cancer cells. Following mechanism of action study revealed that LJ-331 induces cell cycle arrest at the G
$_1$ phase in HL-60 cells and evokes apoptotic phenomena such as an increase in DNA ladder intensity and chromatin condensation by a dose-and time-dependent manner. (omitted) -
Kim, Eun-Joo;Kim, Ki-Suk;Shin, Won-Ho;Seo, Joung-Wook;Choi, Gyu-Kap;Park, Eun-Kyung;Hwang, Ji-Yoon;Han, Sang-Seop 90.3
The most commonly proposed mechanism for QT interval prolongation(LQT) by pharmaceuticals is inhibition of the rapid delayed rectifier potassium channel (I$\_$ Kr/). The LQT potency of pharmaceuticals can be effectively evaluated by examining the effect on hERG channels expressed in CHO cells, known to be equal to I$\_$ Kr/. But, It was known that hERG channels according to increase the bath temperature have several changes, including a marked increase in the amplitude of the outward and tail currents, and acceleration of the rates of activation, recovery from inactivation, and deactivation. (omitted) -
Asparate-arginine-tyrosine (DRY) motif is highly conserved among GPCRs, and the alternation of this motif has been reported to exist naturally and involved with various diseases that involves constitutive activation or desensitization of receptor. To understand the interaction between G protein and
${\beta}$ -arrestin more systemically, we produced the DHY mutants for the D2R and D3R. The introduction of R to H mutation in DRY motif caused differential effects on the characteristics of D2R and D3R: for both receptors receptor-effector coupling and (omitted) -
Cyclin-dependent kinases (CDKs) regulate the cell division cycle, apoptosis, transcription and differentiation. Inhibition of CDK is a promising target in development of anti-cancer agents. An indirubin analog (AGM01l), a CDK inhibitor, is a synthetic compound that inhibits human cancer cell growth in vitro. AGM01l showed a potent cytotoxicity in cultured human cancer cell lines (IC
$\sub$ 50/ = 5.43${\mu}$ M for A549, human colon cancer cell; IC$\sub$ 50/ = 1.21${\mu}$ M for SNU-638, human stomach cancer cell; IC$\sub$ 50/ 9.23${\mu}$ M for HL-60, human leukemia cell). (omitted) -
The present study was performed to investigate the effects of chronic administration of quercetin on lipid peroxidation and glutathione concentrations in rat liver. Male Sprague-Dawley rats were divided into two groups, one of which was fed a normal diet and the other a vitamin E-free diet. Each of these groups was divided further into three subgroups and treated with quercetin administered orally at either 2 or 20 mg/day or with vehicle for four weeks. The concentrations of
${\alpha}$ -tocopherol in serum and liver increased following quercetin treatment, and these increases were significantly greater in rats maintained on vitamin E-free diet. (omitted) -
In our search for NF-kB inhibitors from natural resources, we have previously identified two structurally related dilignans, manassantin A and B as specific inhibitors of NF-kB activation from Saururus chinensis. However, their molecular mechanism of action remains unclear. We here demonstrate that manassantin A and B are potent inhibitors of NF-kB activation by the suppression of transciptional activity of RelA/p65 subunit of NF-kB. These compounds significantly inhibited the induced expression of NF-kB reporter gene by LPS or TNF-a in a dose-dependent manner. (omitted)
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This study with the object of reported to depigment agent, oxyresveratrol derivative, compound DMPB. Compound DMPB with a two methoxy groups and modified connection chain. It was synthesized in accordance with a simple combination process. Compound DMPB exhibits depigmentaion ability on ultraviolet B-induced hyperpigmention of the brown guinea pig skin. In addition, this Compound exhibited 30% inhibitory effect of melanin generation without cell toxicity as a result of the treatment with 100 ppm in melan-a cells. (omitted)
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Anti-inflammatory mechanism of melittin, a component of bee venom in Raw 264.7 cells and SynoviocytePark, Hye-Ji;Kim, Kee-Hyun;Lee, Chung-Ou;Lee, Sun-Young;Lee, Seung-Ho;Son, Dong-Ju;Yun, Yeo-Pyo;Oh, Ki-Wan;Oh, Goo-Taeg 93.1
Bee Venom (BV) has been treated in inflammatory diseases such as rheumatoid arthritis (RA). Bee venom contains several biologically active non-peptide substances as well as two major known peptides; the hemolytic peptide melittin (50%) and the neurotoxic peptide apamin, and a number of minor peptides. Previous our study showed that BV blocked LPS and SNP-induced production of NO and PG through inactivation of NF-kB which regulates expression of COX-2 and iNOS. (omitted) -
To get a better insight into the biophysical mechanism of action of chlorhexidine digluconate, we examined the effect of chlorhexidine digluconate on the thickness of outer membranes isolated from cultured Porphyromonas gingivalis using energy transfer between the membrane surface fluorescent probe (l-anilinonaphthalene-8-sulfonic acid) and the hydrophobic fluorescent probe [1,3-di(l-pyrenyl)propane]. 1-Anilinonaphthalene-8-sulfonic acid quenches the monomer fluorescence of 1,3-di(1-pyrenyl)propane. (omitted)
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The signaling components of high affinity IgE receptor (Fc RI) were searched by yeast-hybrid screening of the cDNA library constructed from RBL-2H3 cells. The cytoplasmic part of the Fc RI- chain was found to specifically interact with PLC 2, and further comparatives studies were conducted focusing on the differential regulation of two PLC- isoforms through Fc RI. The inhibitors of Src, Syk, and protein kinase C similarly affected the tyrosine phosporylations of PLC 1 and PLC 2 but the inhibitors of PI3-kinase and p42/44 ERK effectively inhibited the activation of PLC 1 but not PLC 2. (omitted)
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This research was performed to investigate the protective effect of Chungpesagan-tang (CPS) against ischemic damage in PC12 cells. To elucidate the mechanism of the protective effect of CPS on ischemic insult, cell viability and changes in activities of Superoxide dismutase, Glutathione Peroxidase, Catalase, Caspase 3 and the production of Malondialdehyde were observed after treating PC12 cells with CPS which was metabolized by rat liver homogenate. Pretreatment of CPS with liver homogenate increased its protective effect against ischemic insult by reducing the harmful effect of CPS itself. (omitted)
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Kim, Seong-Woo;Park, Hyun-Jung;Kim, Young-Gi;Yeon, Kyu-Jeong;Ryu, Hyung-Chul;Park, Sang-Wook;Kim, Jong-Hoon;Ko, Dong-Hyun;Chae, Myeong-Yun 94.2
CJ-11668 is a new potent and selective COX-2 inhibitor. CJ-11668 showed COX-2 inhibition (IC50) of 65nM and selectivity ratio (COX-l/COX-2) of 770 in the cell based assay. In the human whole blood assay, CJ-11668 showed COX-2 inhibition (IC50) of 370nM and selectivity ratio (COX-l/COX-2), 135. The treatment of CJ-11668 (5 mg/kg, p.o) produced a significant inhibition (35%) of inflamed rat paw volume in the carrageenan-induced acute inflammation. CJ-11668 also suppressed the PGE2 level (69% inhibition, 1 mg/kg, p.o) in the zymosan-induced mouse air pouch model after 3 hrs. (omitted) -
Lee, Sun-Young;Song, Yeun-Suk;Hwang, Dae-Yeun;Kim, Young-Kyu;Yoon, Do-Young;Lim, Jong-Seok;Hong, Jin-Tae 94.3
Familial form of Alzheimer's disease (FAD) is caused by mutations in presenilin-l (PS-1) and presenilin-2 (PS-2). PS1 and PS2 mutation are known to similar effects on the production of amyloid peptide (A ) and cause of neuronal cell dath in the brain of patient of Alzheimer's disease. The importance of the alternation of cellular calcium homeostasis in the neuronal cell death by PS1 mutation in a variety of experimental systems has been demonstrated. However, no studies on the effect of PS2 of mutant PS2 on cellular calcium homeostasis, and relevance of its change to neuronal cell vulnerability against neurotoxins have been reported. (omitted) -
Sopungsungi-won has been used as a traditional medicine for diabetes and it has been proved evidently as a potential remedy for type 2 diabetes mellitus. Both in vivo and in vitro experiments with water extract of Sopungsungi-won have been reported to exhibit anti-diabetic effects in our previous studies. In the present study, we have chosen Rheum undulatum (RU), which is the main component of Sopungsungi-won, to examine its anti-apoptotic effect on pancreatic b-cells, HIT-T15, against oxidative stress induced by hydrogen peroxide (H
$_2$ O$_2$ ). (omitted) -
Sphingosine-1-Phosphate-Induced ERK Activation Protects Human Melanocytes from UVB-Induced ApoptosisUltraviolet B (UVB) is known to induce apoptosis in human melanocytes. Here we show the cytoprotective effect of sphingosine-1-phosphate (S1P) against UVB-induced apoptosis. We also show that UVB-induced apoptosis of melanocytes is mediated by caspase-3 activation and poly(ADP-ribose) polymerase (PARP) cleavage, and that S1P prevents apoptosis by inhibiting this apoptotic pathway. We further investigated three major subfamilies of mitogen-activated protein (MAP) kinases and the Akt pathway after UVB irradiation. (omitted)
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Lysophosphatidic acid (LPA) is a well-known mitogen in various cell types. However, we were surprised to find that LPA inhibits melanocyte proliferation. Thus, we further investigated the possible signaling pathways involved in melanocyte growth inhibition. We first examined the regulation of the three major subfamilies of mitogen-activated protein (MAP) kinases and of the Akt pathway by LPA. The activations of extracellular signal-regulated protein kinase (ERK) and c-Jun N-terminal kinase (JNK) were observed in concert with the inhibition of melanocyte proliferation by LPA, whereas p38 MAP kinase and Akt were not influenced by LPA. (omitted)
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Carbofuran(CF) is one the most widely used carbamate pesticides in the world applied for insect and nematode control. Due to its widespred use in agriculture and households, contamination of food, water, and air has become serious, and consequently adverse health effects are inevitable in humans, animals, wildlife and fish, it has reported that CF alone or in combination with other carbamate insecticides influences the level of reproductive and metabolic hormones such as thyroxine and corticosterone, and results in impairment of endocrine. (omitted)
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Antidiabetic activity of formular containing an Euonymus alata (EA) and Mori Foluim (MF) was investigated in oral glucose tolerance test (OGTT) and multiple low dose Streptozotocin (MLDSTZ)-induced rats. Optimum ratio between EA and MF was found to be 1:1 in OGTT, and two strengths (250 and 500 mg/kg for each medicinal plant) were coadministered with 20 mg/kg of STZ in 5 consecutive days. At 3rd week, water and food intakes were compared between groups and polydipsia and polyphagia shown in diabetic control were markedly improved in dose dependent manner. (omitted)
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Kim, Yu-Mi;Lee, Jae-Joon;Jin, Chun-Mei;Yang, Yoo-Jung;Yin, Shou-Yu;Kang, Min-Hee;Lee, Myung-Koo 97.2
(1R,9S)-(${\beta}$ )-Hydrastine (HS) at 10-50${\mu}$ M has been proven to have an inhibitory effect on dopamine biosynthesis in PC12 cells by the inhibition of tyrosine hydroxylase (TH) activity and TH gene expression. In the present study, therefore, the effects of HS on the basal and K$\^$ +/-induced dopamine release, and Ca$\^$ 2+/ influx induced by high K$\^$ +/ and caffeine in PC12 cells were investigated. The dopamine release by high K$\^$ +/ (56 mM) was inhibited by co-incubation of 20${\mu}$ M HS. Application of HS also significantly reduced the magnitude of the maintained Ca$\^$ 2+/ influx induced by K$\^$ +/ depolarization. (omitted) -
The inhibitory effects of tetrahydropapaverine on serotonin biosynthesis in serotonin-producing murine mastocytoma P815 cells were investigated. Tetrahydropapaverine at concentration ranges of 5-20 M decreased serotonin content in a concentration-dependent manner in P815 cells and showed 42.1 % inhibition of serotonin content at 5.0 M for 24 hr. The value of 50 % inhibitory concentration, IC
$\sub$ 50/, of tetrahydropapaverine was 6.2 M. Under these conditions, tryptophan hydroxylase (EC 1.14.16.4, TPH), was inhibited for 24-36 hr after treatment with tetrahydropapaverine in P815 cells(49.1 % inhibition at 7.5 M). (omitted) -
Bee venom (BY) has been utilized to relieve pain and to treat inflammatory diseases such as rheumatoid arthritis (RA). However, the molecular mechanism by which BV-induced anti-arthritis effect has been not reported yet. Therefore, in the present study we investigated anti-inflammatory effect of BV in a murine marcrophage cell line Raw 264.7 cell and synoviocyte obtained from RA patients. The present data showed that BV has a preventive effect on lipopolysaccharide (LPS) and sodium nitroprusside (SNP) induced induction of COX-2, cPLA2 and iNOS. (omitted)
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Introduction: We previously reported that a new glycosaminoglycan, acharan sulfate (AS) from the African giant snail Achatina fulica showed anticoagulation activity in vitro, but it was much less than that of heparin. In the present study, the anticoagulant activity of AS was investigated in vivo. Methods: AS and heparin were administered to rats in various concentrations and anticoagulant activities were measured. Both were also compared in thrombin-induced Results: Intravenous administration of acharan sulfate prolonged the coltting time (APTT) in mice and rats in a dose-dependent manner. (omitted)
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Lee, Seung-Ho;Lee, Sun-Young;Park, Hye-Ji;Lee, Yoot-Mo;Lee, Hee-Soon;Song, Suk-Gil;Yoo, Hwan-Soo;Oh, Ki-Wan;Kwon, Byoung-Mog 99.1
Cinnamaldehyde is the main component of cinnamon bark oil and show several biological activities such as anti-tumor, anti-fungal, anti-mutagenic and anti-inflammatory effects. A couple of studies have investigated how the natural compound exerts its anti-inflammatory effect. In despite of numerous investigations, the biological mechanism of effects belong to cinnamaldehyde remain unclear. We isolated 2-hydroxycinnamaldehyde(HCA) from the bark of Cinnamomun cassia Blume and reported a various of biological activities of HCA. (omitted) -
Park, Mi-Sun;Kang, Ho-Il;Lim, Sin-Ae;Jee, Seung-Wan;Eom, Mi-Ok;Ryeom, Tai-Kyung;Kim, Ok-Hee 99.2
One of the major limitations in using adenoviral vector for gene therapy is inefficient infection of host cells. The presence of coxsackievirus and adenovirus receptor (CAR) and${\alpha}$ -integrin on cell surfaces is required for efficient adenovirus infection. In this study, we investigated the effect of trichostatin A, a histone deacetylase inhibitor, on transfection efficiency after transduction of adenovirus mediated p16$\^$ INK4a/ gene transfer. In our previous study, p16$\^$ INK4a/ tumor suppressor gene transfer in the non-small cell lung cancer cells (A549 cells) by transduction of recombinant adenovirus (Ad5CMV-p16) resulted in significant inhibition of cancer cell proliferation. (omitted) -
It is desirable to improve the tumor targeting and blood clearance pharmacokinetics of radiolabeled monoclonal antibodies. To achieve this goal, several avidin-biotin (Bt) binding systems have been developed to decouple large molecular weight antibodies from small radiolabels, thereby achieving high tumor-to-background radioactivity ratios. We inserted a readily catabolizable linker, triglycine (TG), between 3-[/sup125/I]iodobenzoate and dendrimer (G3). We also neutralized the positive charges of G3 by acylation with tetrafluorophenyl glycolate, thereby blocking proximal tubular reabsorption of G3 mediated by charge attraction. (omitted)
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Oh, Ho-Jung;Lee, Nam-Kyung;Kim, Soon-Nam;Hong, Choong-Man;Lee, Ki-Hong;Yoo, Si-Hyung;Shin, In-Soo;Lim, Jae-Hyun;Choi, Seung-Eun 100.1
Tissue engineering has arisen to address the extreme shortage of tissues and organs for transplantation and repair. One of the most successful techniques has been the seeding and culturing cells on three-dimensional biodegradable scaffolds in vitro followed by implantaion in vivo. We used PLA and PLGA as biodegradable polymers and rabbit chondrocytes were isolated and applied to PLA and PLGA to make artificial cartilage. To evaluate the biocompatibility and biological safety of polymers, in vitro cytotoxicity and in vivo animal tests were investigated. (omitted) -
Shin, In-Soo;Kwon, Oh-Hee;Kim, Soon-Nam;Hong, Choong-Man;Lee, Ki-Hong;Oh, Ho-Jung;Yoo, Si-Hyung;Lim, Jae-Hyun;Choi, Seung-Eun 100.2
To satisfy the increasing medical demanding especially for sever burn patients to regenerate full thickness wound cure, this study developed dermis with gelatin based scaffold and perform the biocompatibility tests. To prepare scaffold 30% of gelatin was mixed with sieved salt and dried in the mold to shape then, cross linked with a water-soluble cross-linker, EDAC. Preparing the cell for seeding from a rabbit skin, the fibroblast and keratinocyte were successfully isolated and cultured in vitro. After cell and scaffold were ready, the fibroblast was seeded to the scaffold (∼10$\^$ 6/ cell/cm ) for preparing dermis and keratinocyte was cultured until forming the sheet. (omitted) -
The therapeutic goal in liver fibrosis is to reverse fibrosis and selective clearance of activated hepatic stellate cells (HSCs), which playa central role in liver fibrogenesis, by apoptosis might be essential during resolution of fibrosis. Past several years we screened for natural products which mediate apoptosis in activated HSCs, and among the candidates honokiol, isolated from Magnoliae Cortex, was found to induce apoptotic death in activated rat HSCs in a dose- and time-dependent manner at the concentration between 12.5 microM and 50 microM. (omitted)
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Baicalein (5,6,7-trihydroxyflavone), a flavonoid originated from the root of Chinese medicinal herb Scutellaria baicalensis, has been shown to exert anti-inflammatory and antioxidant effects and hepatic stellate cells play an important role in the pathogenesis or hepatic fibrosis. In this study, we investigated apoptosis stimulation by baicalein in activated rat hepatic stellate cells (T-HSC/C1-6). Transformed rat hepatic stellate cells (T-HSC/C1-6) were treated with baicalein(100uM, 70uM, 40uM). Apoptosis was determined by detection of DNA fragmentation in gel electrophoresis, morphological alternations by flow cytometry and quantification of phosphatidylserine externalization by Annexin V labeling. (omitted)
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Jeong, Eui-Man;Jun, Hyung-Jin;Kim, Ha-Dong;Lee, Ho-Sup;Min, Pil-Gi;Jo, Dong-Hwan;Jung, Sung-Yun;Kim, Dea-Kyong 102.1
Phospholipase A$_2$ (PLA$_2$ ) catalyzes the hydrolysis of the sn-2 position of membrane glycerophospholipids to liberate arachidonic acid(AA), a precursor of eicosanoids including prostaglandins(PGs) and leukotrienes (LTs). The same reaction also produces lyso-phospholipids. So far, at least 19 enzymes that possess PLA2 activity have been identified, consists of low-molecular-weight, Ca$\^$ 2+/-requiring, secretory enzymes that have been implicated in a number of biological processes, such as modification of eicosanoid generation, inflammation, host defense, and atherosclerosis. (omitted) -
Kim, Jin-Ho;Kim, Soo-Yeon;Lim, Yong;Pyo, Hyeong-Bae;Park, Byeoung-Soo;Yoo, Hwan-Soo;Yun, Yeo-Pyo 102.2
It has been previously reported that luteolin and luteolin-7-glucoside displayed the potent anti-oxidant and anti-inflammatory effects, which have also been successful in reducing vascular smooth muscle cells(VSMCs) proliferation. In this study, a possible anti-proliferative effect and its mechanism on rat aortic VSMCs by luteolin and luteolin-7-glucoside were investigated. Luteolin significantly inhibited the platelet-derived growth factor(PDGF)-BB-induced proliferation of rat aortic VSMCs. While luteolin-7-glucoside weakly inhibited the proliferation. (omitted) -
This study was carried out to investigate sulfur dioxide in herb drugs.(Puerariae Radix, Lycii Fructus, Platycodi Radix, Dioscoreae Rhizoma, Mori Radicis Cortex, Nelumbo Seed, Paeoniae Radix, Remotiflori Radix, Astragali Radix, Polygonatum Rhizome) Experimental subjects included 105 cases of 10 species of herb drugs collected in Kyung-dong market from December in 2001 to February in 2002. Sulfur dioxide was determined by Optimized Monier-Wiliams method. In 65 cases(61.9%) of the 105 cases, we detected
$SO_2$ over 10mg/kg. (omitted) -
Jung, Sang-Mi;Jung, Sung-Yun;Chang, Dong-Hoon;Jeong, Hyun-Chul;Chin, Mi-Reyoung;Jeong, Eui-Man;Jo, Dong-Hwan;Jeon, Hyung-Jun;Jung, Kwnag-Mook 103.2
The hydrolysis of sphingomyelin (SM), known as the SM pathway, is induced by the activation of sphingomyelinase (SMase) to generate the second messenger ceramide, which plays a key role in cellular responses such as apoptosis, differentiation, senescence, and inflammation. Here, we identified a 60 kDa membrane-associated, neutral and Mg$\^$ 2+/-dependent SMase, termed N-SMase$\varepsilon$ , from mammalian brains, which was revealed as the heat shock protein 60 (HSP60) through cDNA cloning and mass spectrometrical analysis. (omitted) -
Lee, Kyung-Jin;Shin, Dong-Weon;Chung, Young-Chul;Kim, Young-Sup;Ryu, Si-Yung;Roh, Sung-Hwan;Cho, Young-Soo;Jeong, Hye-Gwang 103.3
Activation of hepatic stellate cell has been identified as a critical step in hepatic fibrogenesis and is regulated by several factors including cytokines and oxidative stress. In this study, we assayed effects of saponin (CKS), inulin (CKI) and oligo-sugars (CKO) isolated from Platycodon grandiflorum A. DC, changkil (CK) on experimental cell cycle arrest and apoptosis in hepatic stellate cell line (HSC-T6). CKS induced cell arrest at G$_1$ . CKS also reduced intercellular reactive oxygen species and collagen synthesis in hydrogen peroxide-induced oxidative stress and acetaldehyde-stimulated collagen synthesis, respectively, in HSC-T6 cells. (omitted) -
The purpose of this study is to investigate the effect of the samples on the blood levels of glucose, glycohemoglobin(HbAlc), total cholesterol and triglyceride. The samples have been used in the treatment of a type 2 diabetic animal model (C57BlKsj db/db). The samples were administrated orally before each meal for 6 weeks. Cinnamon dose was 50mg/kg/day, 100mg/kg/day, 150mg/kg/day and 200mg/kg/day, respectively. Rhodiola rosea dose was 50mg/kg/day, 100mg/kg/day, 15-mg/kg/day and 200mg/kg/day, respectively. (omitted)
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Cadmium is an environmental pollutant and exhibits nephrotoxicity, hepatotoxicity and immunotoxicity. Recently, cadmium was found to induce DNA fragmentation, a biochemical hallmark of apoptosis, in cultured renal cells, hepatocytes and neuroblastoma cell. Therefore, the various toxicities of cadmium are thought to be caused by the induction of apoptosis. Lipids-derived pro-apoptotic ceramide has emerged as an important intracellular signaling molecule that mediates diverse cellular effects, of which programmed cell death, or apoptosis, has attracted significant interest. (omitted)
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Chronic Effects of Hair, Blood And Testis In Black Mouse With Neutron Irradiation By Lying Flat PoseThe purpose of this study is to investigate the biological effects in black mouse by neutron irradiation at HANARO reactor in KAERI. Neutrons readily penetrate the charged field of an atomic nucleus because they are electrically neural. And so it can fight cancer with the radiation released when an atom of the element boron absorbs a neutron. The main patient in BNCT facility is brain cancer and sometimes skin cancer in foreign countries until now. Therefore, mice were laid flat and so irradiated at the direction of the front. (omitted)
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Recently, several reports suggest that ceramide formation has been implicated in the apoptosis signaling in response to chemotherapeutic agents. In this study, to enhance paclitaxel-mediated cytotoxicity and endogenous ceramide levels, we blocked ceramide metabolism using an inhibitor of glucosylceramide synthase, l-phenyl-2- dacanoylamino-3-morpholino-l-propanol(PDMP) and SM synthase, D609. Exposure of human breast cancer cells to paclitaxel accumulated de novo ceramide synthesis by enhancement of SPT activity 1.2-fold, whereas ceramide synthase activity was not altered. (omitted)
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Cadmium (Cd) is an inorganic toxicant of great environmental and occupational concern which was classified as a human carcinogen in 1993. Occupational cadmium exposure is associated with lung cancer in human. In the present study, we established the mechanistic basis of apoptotic cell death induced by Cd in WI38 human lung fibroblast. Cd at 20-80
${\mu}$ M decreased viablility of cells in a concentration-dependent manner. PI staining, TUNEL staining and DNA fragmentation analysis demonstrated the apoptotic cell death by Cd. (omitted) -
Hangover is associated with alcohol metabolism in body after the ingestion of an alcoholic beverage. It has been known that hangover is caused by increasing blood acetaldehyde concentration. This study was carried out to evaluate effect against blood ethanol(EtOH) and acetaidehyde(AcH) on the seven natural products samples(Lotus seed, Sweet chest nut rose, Kohki, Gurume-K, Gurume-J, Phytic acid and Chlorophyll). Also, samples which were selected as good products were mixed. Then, effect against blood EtOH and AcH formulas were tested in vivo. (omitted)
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Baeck, Seung-Kyung;Yang, Hoo-Yul;Lim, Mie-Ae;Park, Yoo-Sin;Kim, Sun-Chun;Kim, Dong-Woo;Park, She-Youn;Lee, Ju-Seon 106.3
VIAGRATM, an oral therapeutic agent for erectile dysfunction, is the citrate salt of sildenafil. VIAGRATM is formulated as blue, film-coated rounded-dia-mond-shaped tablets, equivalent to 25mg, 50mg and 100mg of sildenafil for oral administration. ViagraTM has been allowed to be sold at the drug store in Korea officially, but it is still increased to sell or use counterfeits or smuggled goods, because of its high price or strict restriction on both sale and purchase. Discrimination and analysis of 13 cases of VIAGRATM tablets for verification of genuineness or counterfeit were requested to our institute on the period, from January 1999 to July 2003. (omitted) -
20-O-(
${\beta}$ -D-Glucopyranosyl)-20(S)-protopanaxadiol (IH901), an intestinal bacterial metabolite of ginseng saponins formed from ginsenosides Rb1, Rb2 and Rc, is suggested to be a potential chemopreventive agent. Here we show that IH901 induces apoptosis in human hepatoblastoma HepG2 cells. IH901 led to an early activation of procaspase-3 (6 h posttreatment), and the activation of caspase-8 became evident only later (18 h posttreatment). Caspase activation was a necessary requirement for apoptosis because caspase inhibitors significantly inhibited cell death by IH901. (omitted) -
Bisphenol A(BPA) is a monomer widely used in the manufacturing polycarbonate plastic or epoxy resin and Mancozeb (MCZ), a polymeric complex of zinc and manganese salts of ethylene bisthiocarbamate, is widely used in agriculture as fungicide, insecticide and herbcide. These chemicals have been recently known as endocrine disruptors. To investigate the effects of BPA and MCZ on LPS-induced cytokine production (TNF-
${\alpha}$ ) in vivo, female ICR mice were administered to various concentration of these materials (BPA; 100, 500, 1000 mg/kg/day, and MCZ; 250, 500, 1000, 1500 mg/kg/day) for 30 days and serum cytokine levels were measured at 1h post LPS injection (day 32) in BPA- or MCZ-administered mice. (omitted) -
The purpose of this study is to investigate the effect of Sungkangwon (Astragalus membranaceus Bunge + Pueraria lobata Ohwi + Salvia miltiorrhiza Bunge) on fatty liver induced by alcohol diet. Rats were either fed control diet or alcohol diet. On 6 weeks, alcohol group were randomly assigned to groups as follows; supplemented without SKW and with SKW (.033g/kg, 1g/kg, and 3g/kg). all of five groups were fed the chow diet for 4 weeks. After 6 weeks. the blood and liver concentration of TG and total-C is comparably high in alcohol group. (omitted)
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Kaempferol, a flavonol compound, has been reported as the anti-oxidant and anti-angiogenic agent and it has been found to inhibit cell growth in vitro. Abnormal proliferation of vascular smooth muscle cells (VSMCs) plays an important role in development of atherosclerosis. In this study, we examined the anti-proliferative effect and its mechanism on rat aortic VSMCs treated by kaempferol. kaempferol significantly inhibited the platelet-derived growth factor (PDGF)-BB-induced proliferation of rat aortic VSMCs in concentration-dependent manner by cell count and [
$^3$ H]-thymidine incorporation assay. (omitted) -
In the present study, we investigated the antitumor effects of Ginsenoside Rh2 and
$\beta$ -glucan using an experimental metastatic mouse model intravenously injected with B 16 melanoma F10 cells. Oral administration to various concentration of$\beta$ -glucan (50mg/kg, l00mg/kg and 200mg/kg) dose-dependently reduced the lung-metastatic potential of metastatic BI6 melanoma F10 cells in syngenic mice. At same dose, Ginsenoside Rh2(50mg/kg) has more antitumor effect than$\beta$ -glucan(50mg/kg). (omitted) -
The aim of this study was to investigate the biological effects of blood and testis by neutron or gamma-ray irradiation in black mouse. Six-week-old C57BL male mice were irradiated with neutron (flux: 1.036739E+09) or Co60 gamma rays(dose rate: lGy/min.) The irradiation method of animal was abdominal irradiation and dose of irradiation was 10 and 20 Gy added with 5 and 15Gy in neutron irradiation.. After that, the mice were sacrificed 3 days later. Blood and testis were taken and then composition of blood in blood cell were investigated. (omitted)
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Estrogen is the most important endocrine hormone that has reproduction and physiological process in a number of tissues. However, an excess of estrogen can promotes the growth of hormone-dependent breast cancer. Thus the regulation of estrogen level is important a prevention of estrogen-related cancer. It has been reported that some of flavonoids could inhibit estrogen-dependent cancer. And these compounds are expected as chemopreventive agents on estrogen related disease. (omitted)
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Choi, Heon-Kyo;Yoo, Jae-Myung;Tudev, Munkhtsetseg;Lee, Yong-Moon;Yun, Yeo-Pyo;Yoo, Hwan-Soo 110.1
Fumonisins are specific inhibitors of ceramide synthase in sphingolipid metabolism. Sphingolipids are biologically active lipid mediators in cellular physiology and involved in cell signaling, growth, transformation, angiogenesis and differentiation. The objective of this study was to determine the effect of fumonisin B1 on$Na^+, \;K^+$ -pump activity when fumonisin B1 was exposed to LLC-PK1 cells. Fumonisin B1 elevated free sphingoid bases and their 1-phosphates, while total complex sphingolipids were depleted at 20$\mu$ M fumonisin B1 during the 3 day exposure. (omitted) -
The ethanol extracts of mixed vegetables (Bioactive V, BV), mixed fruits (Bioactive F, BF) and its liquid formulation (Chungpae Plus
$\circledR$ ) were evaluated for their antioxidative and antigenotoxic activity. They were shown to possess the significant free radical scavenging effect against l,l-diphenyl-2-picryl hydrazine (DPPH) radical generation and were revealed to show the inhibitory effect of lipid peroxidation as measured by malondialdehyde (MDA) formation. (omitted) -
In the previous studies, we have reported that NQ30l, a synthetic l,4-naphthoquinone derivative, displayed a potent antithrombotic activity, and that this might be due to antiplatelet effect, which was mediated by inhibition of cytosolic
$Ca^{2+}$ mobilization in activated platelets. In the present study, the effect of NQ301 on arachidonic acid cascade in activated platlets was examined. NQ301 concentration-dependently inhibited washed rabbit platelet aggregation induced by collagen (10$\mu$ g/ml), arachidonic acid (100$\mu$ M) and U46619 (1$\mu$ M), a thromboxane$A_2$ receptor agonist, with$IC_50$ values of 0.60$\pm$ 0.02, 0.79$\pm$ 0.04 and 0.58$\pm$ 0.04$\mu$ M, respectively. (omitted) -
Park, Mi-Ja;Oh, Mi-Jung;Jo, Dong-Hwan;Chin, Mi-Reyoung;Lee, Ji-Yeon;Park, Ji-Woo;Lee, Na-Gyong;Kim, Dae-Kyong 111.1
Bacterial infection is a very complex process in which both pathogens and host cells play crucial roles, and the host cells undergo drastic changes in their physiology, releasing various proteins in response to the pathogenic infection. Human airway epithelial surface serves as a first line of defense against microorganisms and the external environment. It is well known that bronchial epithelial cells secrete various chemokines and cytokines such as IL-6 and IL-8 to cope with various respiratory pathogens. (omitted) -
Yang, Won-Kyung;Han, Eun-Young;Lee, Jae-Sin;Park, Yong-Hoon;Park, Hwa-Kyung;Lim, Mi-Ae;Chung, Hee-Sun 111.2
Dextromethophan and carisoprodol have been abused to obtain a hallucination for longer than 10 years in Korea. Due to their seriousness of abuse liablility, recently government decided to control them as a psychotropic agents. As these are controlled, it is necessary for us to establish the analysis of these medicine and their metabolites in hair to prove the abuse of these drugs. This study is described for the determination of dextrometorphan and carisoprodol in hair. (omitted) -
Han, Eun-Young;Yang, Won-Kyung;Lee, Jae-Sin;Park, Yong-Hoon;Kim, Eun-Mi;Lim, Mi-Ae;Chung, Hee-Sun 112.1
The qualitative and quantitative analysis of MDMA and MDA in hair samples by GC/MS were reported. Hairs were collected from subjects aged 22-37 years, who were suspected of abusing MDMA. After washing with methanol, hair samples were cut into small pieces, extracted with methanol containing 1 percent hydrochloric acid for 20th, and the solution was evaporated. MDMA or MDA in the extract were determined by GC/MS using selected ion monitoring after derivatization with trifluoroacetic anhydride. (omitted) -
CYP1 enzymes, CYP1A1, CYP1A2 and CYP1B1, are known to bioactivate procarcinogens particularly polyaromatic compounds. Flavonoids are a class of natural compounds that are present in edible plants. Structurally, these compounds are polyphenols with two aromatic rings (A, B) and a heterocycyclic ring (C). We observed the differential inhibition of 5,7-dihydroxyflavones which are different in numbers of B-ring-OH, to the activity of ethoxyresorufin O-deethylase (EROD) in human hepatic microsomes with the IC50 values, ie, 0.57 mM, 1.28 mM, and 3.62 mM, chrysin, apigenin, and Luteolin, respectively. (omitted)
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Park, Mee-Jung;Choi, Sang-Kil;Son, Haeng-Ja;Lee, Jae-Sin;Kim, Eun-Mi;Lim, Mi-Ae;Chung, Hee-Sun 113.1
A 35-year-old Perubian who suffered from grand mal seizures died in aircraft on his way from United States to Hongkong. When he boarded the aircraft, he was normal but later he suffered from hyperthermia, dizziness, abdominal pain, agitation and convulsion in the flight before dead. While performing the autopsy, 115 cocaine packs were found in the GI tract. To determine the concentration of cocaine and its metabolites, blood, urine, bile juice, gastric content, liver, spleen, heart, kidney, cellebrum and lung were taken and analyzed. (omitted) -
Chung, Yung-Chul;Choi, Chul-Yung;Kim, Ji-Young;Chun, Hyo-Kon;Gho, Young-Hee;Jeong, Hye-Gwang 113.2
Inducible cyclooxygenase-2 (COX-2) has been implicated in the processes of inflammation and carcinogenesis. Thus, the potential COX-2 inhibitors have been considered as anti-inflammatory or cancer chemopreventive agents. In this study, we investigated the effect of Caffeoyl-4-dihydrocaffeoyl quinic acid (CDCQ) isolated from Salicornia herbacea on the expression of cyclooxygenase (COX-2) in lipopolysaccharide (LPS)-activated RAW 264.7 macrophages. When CDCQ was treated with LPS, the prostaglandin$E_2$ production and COX-2 gene expression induced by LPS were markedly reduced in a dose-dependent manner. (omitted) -
Lee, Kyung-Jin;Shin, Dong-Weon;Chung, Young-Chul;Kim, Young-Sup;Ryu, Si-Yung;Roh, Sung-Hwan;Jeong, Hye-Gwang 113.3
The increased deposition of extracellular matrix by hepatic stellate cells following liver injury in a process known as activation is considered a key mechanism for increased collagen content of liver during the development of liver fibrosis. In this study, we investigated the protective effects of an aqueous extract from the roots of Platycodon grandiflorum A. DC (Campanulaceae), Changkil (CK), on hepatic fibrosis in hepatic stellate cells. We report that CK reduces the accumulation of collagen in acetaldehyde-induced hepatic stellate cells. (omitted) -
Mancozeb is a protective fungicide on plants and a polymeric complex of ethylene bisdithiocarbamate manganese with zinc salt. It is reported to induce teratogenic and carcinogenic effect in laboratory animals. But the immunomodulating effects of Mancozeb exposure have not been systemically evaluated. The purpose of this study was to investigate the effects of Mancozeb on cell-mediated immunity in mice. For ex vivo assessment, mice were orally exposed to Mancozeb dissolved in distilled water as concentrations of 2,500, 5,000, 10,000 mg/kg for single occasion (acute exposure) or 250, 1,000, 1,500 mg/kg/day 5 days a week for 30days(subacute). (omitted)
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Kwack, Seung-Jun;Kim, Soon-Sun;Rhee, Gyu-Seek;Lee, Rhee-Da;Chae, Soo-Young;Choi, Yo-Woo;Lee, Hyun-Joo;Park, Kui-Lea 114.2
3-Monochloro-1, 2-propanediol(3-MCPD) is a toxic compound, often present in different foods containing acid hydrolyzed(AH) protein, like seasonings and savory food products. In Korea, 3-MCPD is currently being a problem because of its toxicity in AH soybean sauce. The purpose of the present studies was to investigate the effects of 3-MCPD on male fertility, sperm and testosterone secretion. In vivo male fertility test was performed for observing the adverse effects of 3-MCPD on the function of male reproductive system and pregnancy outcome. (omitted) -
Lee, Su-Jung;Ho, Shin-Jae;Kim, Tae-Sung;Moon, Hyun-Ju;Kang, Il-Hyun;Kim, In-Young;Oh, Ji-Young;Lee, Young-Ju;Kim, An-Keun;Han, Soon-Young 115.1
Cadmium, a human carcinogen, can induce apoptosis in various cell lines. Despite extensive research, the mechanisms of cadmium-induced apoptosis are poorly understood, and its toxicity and estrogenic potential in human are not clear. This study was performed to investigate the apoptotic activities of cadmium on two human breast cancer cell lines: MCF-7 cells, an estrogen receptor (ER) positive cell line, and MDA-MB-231 cells, an ER negative cell line. Both cells were treated with$CdCl_2$ 100$\mu$ M for 12hrs, and the spoptosis was determined by DNA fragmentation, DAPI staining, and expression of caspase-9. (omitted) -
3-Monochloro-1, 2-propanediol(3-MCPD) was analyzed in soy sauce products commercially available in Korea. A total of 24 samples were collected and 3-MCPD was determined by GC/MS. Sources of 24 samples were classified by manufacturing methods as naturally brewed(NB), acid hydrolyzed(AH) and mixed(M=NB+AH) soy sauces. 3-MCPD was not detected in NB soy sauce products (< 0.01 ppm, mg/kg) whereas AH and M soy sauce products showed a wide range of 3-MCPD contamination(0.01~2.038ppm). (omitted)
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Saururus chinensis Baill (Saururaceae) is a perennial plant that has been used in the treatment of edema, jaundice and gonorrhea in Korean folk medicine. This study was carried out to investigate the inhibitive effects of Saururus chinensis Baill (SCB) on lipid metabolism in Sprague-DaweIy rat(SD-rat) accutely exposed to 2,3,7,8-tetrachlorodibenzo-p-dioxin(TCDD). After 7 days from TCDD(1
$\mu$ g/kg) injection, SCB(200mg/kg) was administered into rats intraperitoneally for 4 weeks. (omitted) -
Lee, Yoot-Mo;Seong, Min-Je;Lee, Sun-Young;Lee, Sang-Min;Kim, Tae-Seong;Han, Soon-Young;Yoo, Han-Soo;Lee, Myung-Koo;Oh, Ki-Wan;Hong, Jin-Jae 116.1
Bisphenol A (BPA) mimics estrogen and its activity is one third to one quarter that of estradiol. BPA, an ubiquitous environmental contaminent has been shown to cause development reproductive toxicity and carcinogenic effect. BPA may do physiological action through ER$\alpha$ and ER$\beta$ which are expressed in central nerve system. We previously found that expose of BPA to immature mice resulted in behavial alternation, suggesting that overexposure of BPA could be neurotoxic. (omitted) -
Lee, Dong-Soo;Lee, Hye-Eun;Shin, Ji-Young;Lee, Hee-Woo;Chung, Hae-Young;Yoon, Sik;Moon, Jeon-Ok 116.2
Aspirin and aspirin-like nonsteroidal antiinflammatory drug have been the mainstay of therapy for rheumatoid arthritis. In this study, we investigated the hepatoprotective effect of aspirin on the dimethylnitrosamine (DMN)-induced liver damage in rats. Oral administration of aspirin (7.5, 15mg/kg daily for 4 weeks) into the DMN-treated rats remarkably prevented the elevation of serum alanine transaminase, aspartate transaminase and alkaline phosphatase, and bilirubin levels. Aspirin also increased serum protein level and reduced the hepatic level of malondialdehyde in DMN-treated rats. (omitted) -
Colchicine is a drug well known for its use in the therapy of acute attacks of gouty arthritis. Two death caused by oral ingestion of colchicine was reported. Two persons were all women. The one was 34 years old woman and with his boyfriend in a inn and the other was a housewife. The first one was a alcoholic but his boyfriend was afflicted with gout. So her boy friend carried over about 60 tablets of colchicine, 4 tablets of naltrexone and 22 tablets of fluoxetine. After her death there were remained colchicine, 2 tabs, naltraxone 4 tabs and fluoxetine 22 tabs. (omitted)
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Cheong, Jae-Hoon;Tan, Tan Blendyl;Kim, Y.B.;Bannon, Bannon Desmond;Olivi, Olivi Luisa;Bressler, Bressler Joseph 117.2
The mechanism by which lead enters glial cells was examined. The uptake of lead reached saturation when assays were performed in buffers at pH 5.5 and 7.4. The Vmax and Km was 2.7 pmoles/mg protein/min and 13.4 M in the buffer at pH 7.4, respectively, whereas the Vmax and Km was 329 fmoles/mg and 8.2 M in the buffer at pH 5.5, respectively. Uptake in a buffer at pH 5.5 but not at pH 7.4 was inhibited by iron. Cells treated with the iron chelator desferoxamine displayed higher levels of the divalent metal transporter mRNA and protein. (omitted) -
The acetylation of histone is one of the mechanisms involved in the regulation of gene expression and is tightly controlled by two core enzymes, histone acetyltransferase (HAT) and deacetylase (HDAC). There are several reports that imbalance of HAT and HDAC activity is associated with abnormal behavior of the cells in morphology, cell cycle, differentiation, and carcinogenesis. Recently, an increasing number of structurally diverse HDAC inhibitors have been identified that inhibit proliferation and induce differentiation and/or apoptosis of tumor cells in vivo and in vitro. (omitted)
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Park, Jie-Eun;Lee, Sung-Hak;Choi, Jae-Mook;Kim, Il-Hwan;Kim, Taek-Rho;Kim, Deog-Yeor;Noh, Hyun-Jung;Kang, Hee-Chol;Cho, Hi-Jae;Kim, Young-Hoon 118.1
SS cream and its revised formula, CJ-4001 is topical Chinese herbal drugs for premature ejaculation. To evaluate the genotoxic potentials of these drugs, micronucleus test using Acridine orange (AO) staining method was performed. Acridine orange (AO) staining is adopted in OECD guideline 474 and widely used in micronucleus test. In dose range finding study, no mouse was dead at 2000 mg/kg using single treatment subcutaneously. Therefore, 3 dose levels were chosen at 500, 1000, 2000 mg/kg. (omitted) -
Propofol(2, 6-diisopropylphenol) is rapid, short-acting intravenous anaesthetic agent. It is used for the induction and maintenance of general anaesthesia or sedation. The recommended doses are 2-2.5mg/kg given as a titration infusion over about 30min to achieve anaesthesia. Recently, we encountered 4 fatalities related to propofol. One death is a suicide by self-administered of propofol and the others are therapeutic misadventures during surgical care. The propofol level in the blood and tissues were determined by gas chromatographic analysis with mass spectral detection. (omitted)
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Diazepam (DZ) is one of the most frequently prescribed drugs as an antianxiety agent, muscle relaxant, and anticovulsant and sometimes causes intoxication due to accidental overdose, misuse or abuse. Screening or confirmation methods for DZ and NDZ in plasma are very important for clinical and toxicological studies and in forensic cases. GC/MS assay with SPE was developed for the determination of diazepam and its metabolite, nordiazepam in human plasma. Diazepam in plasma was extracted by a rapid and sensitive procedure based on C18 bonded-phase extraction. (omitted)
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To determinate dextromethorphan (DMP) and its active metabolite dextrorphan (DRP) in urine was performed using
$REMEDi^TM$ (Rapid EMErgency Drug identification) that is a fully automated multicolumn high performance liquid chromatographic (HPLC) system with a scanning ultraviolet detector. The limits of detection for DMP and DRP were 0.10 and 0.15$\mu$ g/mL, respectively. The standard curves were linear, with correlation coefficients (r > 0.975) in the concentration range of 0.5~10.0$\mu$ g/mL. (omitted) -
Exposure of 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) causes a variety of biological and toxicology effects, most of which are mediated by aryl hydrocarbon receptor (AhR). The ligand-bound AhR as a heterodimer with AhR nuclear translocator (ARNT) binds to its specific DNA recognition site, the dioxin-responsive element (DRE), and it results in increased transcription of CYP1A1 gene. Retinoic acid (RA) regulates the transcription of various genes for several essential functions through binding to two classes of nuclear receptors, the retinoic acid receptor (RAR) and retinoid X receptor (RXR). (omitted)
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The mutagenic potential of Gryllus bimaculatus was evaluated using the short-term genotoxicity tests including Ames, chromosome aberration and micronuclei tests. In salmonella typhimurium assay, G. bimaculatus did not show any mutagenic response in the absence or presence of S9 mix with TA98, TAl00, TA1535, and TA1537. In chromosome aberration test, G. bimaculatus did not show any significant effect on Chinese Hamster Ovary (CHO) cells compared with control. (omitted)
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Cytochrome P-450 3A4 (CYP3A4) is major enzyme in human liver, the role of this is detoxification and metabolizing more than 50% clinical drugs in use. Expression of CYP3A4 is transciptionally regulated by the Pregnenolone X receptor (PXR), of which human form is Steroid and Xenobiotics receptor (SXR). SXR is activated by wide range of endogenous and exogenous compounds, and then induces CYP3A4 gene expression. In the previous study, it has been known that proximal promoter (-864 to +64) does not response to chemical inducers such as pregnenolone 16a-carbonitrile (PCN), Rifampicin, Estrogen in terms of transcription of CYP 3A4 in cultured cells. (omitted)
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Choi, Chul-Yung;Kim, Ji-Young;Lee, Kyung-Jin;Oh, Duk-Hee;Han, Song-Hee;Woo, Eun-Rhan;Jeong, Hye-Gwang 120.3
Lycii Radicis Cortex, the root bark of Lycium chinense Miller (Solanaceae) is used in oriental medicine as a tonic and is reported to exhibit hypotensive, hypoglycemic, and antipyretic activity. Recently, we have isolated dihydro-N-caffeoyltyramine, a phenolic amide, from the Lycii Radicis Cortex. Treatment with dihydro-N-caffeoyltyramine significantly inhibited the proliferation of human leukemia cell lines HL-60 in a dose-dependent manner. We found also that the growth inhibition of HL-60 by dihydro-N-caffeoyltyramine is associated with induction of apoptosis of cells. (omitted) -
Houttuynia cordata Thunb (HCT) is a herbal plant growing in China, Japan and Korea. According to the records of the Chinese medicine, this plant has been used as folk medicine for analgesics, beriberi, edema, hepatitis, icterus, etc. TCDD (2, 3, 7, 8 -tetrachlorodibenzo-p-dioxin), one of the notorious toxic environmental pollutants, damages various organs including liver and is regarded as an endocrine disrupter. After 7 days from TCDD (1
$\mu$ g/kg) injection, HCT (200 mg/kg) was administered into rats intraperitoneally for 4 weeks. (omitted) -
Kim, Ji-Young;Lee, Kyung-Jin;Oh, Duk-Hee;Jung, Kyung-Sik;Shin, Dong-Weon;Cho, Young-Rhan;Jeong, Hye-Gwang 121.2
Synthetic polymers, biological polymer such as collagen and gelatin are employed extensively as backbones in the construction of hydrogels or cell/tissue scaffoldings for various biomedical applications. In the present study, we investigated the effect of collagen and gelatin on the inducible nitric oxide synthase (iNOS) gene expression in the mouse macrophage cell line RAW 264.7. The production of nitric oxide and expression level of iNOS mRNA were induced by both of collagen and gelatin in dose-dependent manner. (omitted) -
This report describes the fatal case of a 13-year-old middle school girl(MSG) whose cause of death might be attributed to a intoxication involving Venlafaxine(VEN). MSG's mother had the history of depression for 11 years. She and her daughter were found dead in the same room of their apartment, with hanged herself. We analyzed the postmortem of MSG which were requested to our institute for the cause of her death. We couldn't get any blood samples from MSG's postmortem. (omitted)
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Shin, Dong-Soo;Lee, Hye-Eun;Lee, Hee-Woo;Shin, Ji-Young;Yoon, Sik;Chung, Hae-Young;Moon, Jeon-Ok 122.1
Morin, one of the major natural flavonoids has been reported to exhibit a wide range of pharmacological properties. In this study, we investigated the hepatoprotective effect of morin on the dimethylnitrosamine (DMN)-induced liver damage in rats. Oral administration of morin (10, 20mg/kg daily for 4 weeks) into the DMN-treated rats remarkably prevented the elevation of serum alanine transaminase, aspartate transaminase and alkaline phospatase, and bilirubin levels. Morin also increased serum protein level and reduced the hepatic level of malondialdehyde in DMN-treated rats. (omitted) -
Kim, Ji-Young;Moon, Ae-Ran;Kim, Hyung-Gyun;Choi, Chul-Yung;Chung, Yung-Chul;You, Ho-Jin;Jeong, Hye-Gwang 122.2
Gelatin protein is derived from animal collagen tissues and is therefore present in many kinds of animal protein food. The biological origin and biocompatibility of gelatin has led to wide-ranging applications in the pharmaceutical and medical fields; for example, as sealants for vascular prostheses, bone-repairing materials, wound healing agents and scaffolds for tissue engineering purposes. In the present study, we investigated the effects of collagen and gleatin on the cyclooxygenase-2 (COX-2) gene which plays a crucial role in many physiological and pathological processes in macrophages. (omitted) -
To investigate the effect of chitosn oligosaccharide on skin care, we measured tyrosinase activity and melanin production in B16 melanoma cells, and elastase and hyaluronidase activity. Chitosan oligosaccharide itself did not have any anti-oxidant activity in DPPH radical scavenging, and did not affect the proliferation of B16 melanoma cells. Chitosan oligosaccharide dose-depednetly increased mealnin production in the absence or presence of MSH. However, chitosan oligosaccharide did not have any influence on the tyrosinase activity and tyrosinase expression in B16 melanoma cells. (omitted)
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The cellular mechanisms by which excess exposure to the excitatory neurotransmitter glutamate can produce neuronal injury are unknown. In this study, we found that glutamate induced cell death at IC (50) of 100 microM on the cultured human SH-SY5Y neuroblastoma cells. It has been hypothesized that glutamate excitotoxicity is related with the elevation of calcium (Ca) levels. To determine the dependence of glutamate neurotoxicity on Ca environment, extracellular (EDTA) and intracellular (BAPTA/AM) chelator were used. (omitted)
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To investigate the relationship between structure and biological activity of phenylpropanoids, we measured effects of phenylpropanoids on anti-oxidant and whitening activity. In DPPH radical scavenging activity, caffeic acid analogues had anti-oxidant activity in a dose-dependent manner. Although phenylpropanoids did not inhibit purified tyrosinase activity, they significantly inhibited tyrosinase activity and melanin production in MSH-stimulated B16 melanoma cells. (omitted)
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We investigated whether the mushroom extracts can protect neuronal death and ameliorate memory deficits in Alzheimer"s disease induced by
$\beta$ -amyloid peptide[A$\beta$ (25-35)]. Cellular model of Alzheimer"s disease was produced by using SK-N-SH human neuronal cells treated with$A\beta$ . Treatment with 40uM$A\beta$ for 48hours caused a 46% loss of cell viability. First, we examined the effects of 22 mushroom extracts on neuronal death using MTT assay. We found that 3 mushroom extracts increased viability of the cells from 46% to 87%. (omitted) -
Taurine is present in a variety of tissue and exhibits many important physiological functions in the cell. Although it is known that many tissues mediate taurine transport, its functions of taurine transport in bone have not been identified yet. In the present study, we investigated the expression of taurine transporter (TauT) and taurine uptake using mouse stromal ST2 cells and osteoblast-like MC3T3-E1 cells, which is bone related cells. Detection of TauT MRNA expression in these cells were performed by reverse transcription polymerase chain reaction (RT-PCR). (omitted)
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Effects of Compound-A, a phenylpropanoid isolated from Arctium lappa fruit, on sheep red blood cells (sRBC)-induced arthus reaction (AR) were studied in ICR male mice and determined the plaque forming cells (PFC) numbers and hemagglutinin (HA) titer. Two weeks after sensitization of i.p. injection of sRBC (4x10
$^{8}$ cells), ICR male mice were challenged by i.p. injection of sRBC (2$\times{10}^8$ cells). Five days after the challenge of antigen, paw edema induced three hours after the last challenge by Arthus reaction. (omitted) -
Hepatic ischemia and reperfusion predisposes the liver to secondary stresses such as endotoxemia possibly via dysregulation of the hepatic microcirculation secondary to imbalanced regulation of vascular stress gene. In this study, we determined the effect of endotoxin on hepatic vasoregulatory gene expression in response to hepatic ischemia and reperfusion (I/R). Rats were subjected to 90 min of hepatic ischemia and 6 h of reperfusion. Lipopolysaccharide (LPS, 1 mg/kg) was injected intraperitoneally after reperfusion. (omitted)
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Effect of Compound-A, a phenylpropanoid isolated from Arctium lappa fruit, on heterologous passive cutaneous anaphylaxis (HPCA), the release of histamine, and Phospholipase
$A_2$ (PLA2) and phosphadiesterase (PDE) activities were studied by the method of Levine and Vaz. Anti-serum was prepared from ovalbumin (OA)-sensitized male Balb/c mouse at two weeks after the last challenge of OA and alumina gel. Heterologous PCA test in rats were carried out to determine the contents of leakaged pigment in the dorsal skin 30 minutes after i.v. injection of 0.2 ml of 1 % OA and 1 % Evans blue mixture (1:1). (omitted) -
Compound-A is a phenylpropanoid isolated from Arctium lappa fruit. In this experiments, effect of Compound-A on sheep red bood cells (sRBC) - induced delayed type hypersensitivity (DTH) were studied in ICR male mice and determined the Rosette Forming Cells (RFC). Two weeks after sensitization of i.p. injection of sRBC (4
$\times{10}^8$ cells), ICR male mice were challenged by i.p. injection of sRBC (2\times{10}^8$ cells). Five days the challenge of antigen, paw edema induced twenty-four hours after the last challenge by DTH. (omitted) -
Effect of Compound-A, a phenylpropanoid isolated from Arctium lappa fruit, on the reversed cutaneous anaphylaxis (RCA) and complement-dependent hypersensitivity (CDH) were studied in SD male rats and ICR male mice, respectively. RCA and hemolysin (HY) titer test are related to reaction of Type II Hypersensitivity. Experiments were carried out to determine RCA as the edema of skin two hours after injection of 0.05 ml/site of anti-rat serum rabbit serum in SD rat. Drugs were orally administered one hour before antigen challenge. (omitted)
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Effect of Compound-A, a phenylpropanoid isolated from Arctium lappa fruit, on the early- (EAR) and late-phase asthmatic responses (LAR) of guinea pigs were studied in vivo. Guinea pigs were sensitized by injection of 100 mg of ovalbumin (OA). Twenty-one days after sensitization, animals were challenged with exposure to aerosolized 1 % OA for five minutes in double-chambered plethysmograph box with jet nubulizer. Immediately and twenty-four hours after challenge, EAR and LAR ashmatic responses were determined the tidal volume (TV), respiration rate (RR) and specific airway resistance (sRaw), and then animals anethetized and taken the bronchoalveolar lavage fluid (BALF) by lavage the lung with HEPES buffer through cannulation into trachea. (omitted)
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Sepsis remains common surgical problems with high morbidity and mortality despite improvement in the management for septic patient. Although hepatocellular dysfunction occurs during sepsis, the mechanism responsible for this remains unclear. In sepsis, a state of severe oxidative stress is encountered, with host endogenous antioxidant defenses overcome. Therefore, the aim of this study was to determine whether specific abnormality exists in cytochrome P450 (CYP)-mediated metabolizing function associated with polymicrobial sepsis and whether role of ascorbic acid (AA) in the alterations during sepsis. (omitted)
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Koo, Jae-Yeon;Kim, Sang-Sung;Kim, Man-Soo;Park, Seung-Pyo;Shim, Won-Sik;Yang, Young-Duk;Cho, Hwa-Won;Kim, Mi-Sook;Kim, Byung-Moon;Oh, Uh-Taek 128.1
VR1, a capsaicin receptor, is now known to playa major role in mediating inflammatory thermal nociception. Although the physiological role or biophysical properties of VR1 are known, its activation mechanisms by ligands are poorly understood. Here, we show that VR1 requires phosphorylation by$Ca^{2+}$ -calmodulin-dependent kinase II (CaMKII) for its activation by capsaicin. In contrast, dephosphorylation by calcineurin, leads to desensitization of the receptor. Point mutation of VR1 at two putative consensus sites for CaMKII fails to elicit capsaicin-sensitive currents with concomitant reduction in phosphorylation of VR1 in vivo. (omitted) -
We previously reported that phospholipase
$A_2$ ($PLA_2$ )-related pathway and capacitative calcium entry (CCE) via store-operated calcium channel (SOC) were involved in the regulation of muscarinic receptor- mediated sAPP release. We also observed that stimulation of muscarinic receptor associated with the inositol phosphate cascade resulted not only in increase of CCE but also in activation of PLA$_2$ in SH-SY5Y cells. In this study, we further investigated whether the$PLA_2$ isoforms differently regulate the muscarinic receptor-mediated sAPP release, and examined the relationships between activation of$PLA_2$ isoforms and CCE mediated by muscarinic receptors in SH-SY5Y cells. (omitted) -
According to recent reports, cefodizime (CEF), a third generation cephalosporin has the capability of chemotactic activity of neutrophils and monocytes and may act as the strong immuno-modulator. This study was planned to demonstrate whether CEF has the proposed effect on rat dendritic cells in vitro. Dendritic cells were taken from rat spleen tissue and cultured for a week. The obtained dendritic cells were treated with 10
$\mu$ g/ml, 50$\mu$ g/ml, 100$\mu$ g/ml cefodizime and 10IU/$m\ell$ IFN-Υ+1$\mu$ g/ml LPS. (omitted) -
Antitumor and immunomodulatory activities of an aqueous extract (GF100) of Acanthopanax senticosus was examined. In experimental lung metastasis of colon26-M3.l carcinoma cells, intravenous (i.v.) administration of GF100 2 days before tumor inoculation significantly inhibited lung metastasis in a dose-dependant manner. The i.v. administration of GF100 also exhibited the therapeutic effect on tumor metastasis of colon26-M3.1 cells, when it was injected 1 day after tumor inoculation. In an in vitro cytotoxicity analysis, GF100 enhanced the responsiveness to a mitogen, concanavalin A (ConA), of splenocytes in a dose-dependent manner. (omitted)
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As a potent antigen presenting cells and a powerful inducer of antigen specific immunity including cytotoxic T cell activity, dendritic cells(DCs) are being considered as a promising anti-tumor therapeutic module. Unlike solid tumors, leukemia is the hematologic malignancy involving immune effector cells. The expected usage of DCs in leukemia is the treatment of minimal residual disease(MRD) after the remission or stem cell transplantation. In this study, syngeneic leukemia cells were inoculated intra-venously into the mouse (WEHI-3 into the Balb/c), and the autologous tumor cell lysate pulsed DCs were injected as a therapeutic module twice in two weeks. (omitted)
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Betulinic acid (BA), a pentacyclic triterpene isolated from Lycopus lucidus, has been reported to be a selective inducer of apoptosis in various human tumor cells. It also exhibits anti-inflammatory and immunomodulatory properties. Due to its high level of these activities and lack of toxicity, BA is an attractive and promising compound as a new drug and recently undergoing preclinical development as an immunomodulators. How BA mediates these matters is not known yet. (omitted)
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Inflammation is a frequent radiation-induced following therapeutic irradiation. Since the upregulation of adhesion molecules on endothelial cell surface has been known to be associated with inflammation, interfering with the expression of adhesion molecules is an important therapeutic target. We examined the effect if allicin, a major component of garlic, on the induction of intercellular adhesion molecule-l (ICAM-1) by gamma-irradiation and the mechanisms of its effect in gamma-irradiated human umbilical vein endothelial cells (HUVECs). (omitted)
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Phytoestrogens are naturally occurring compounds derived from plants. Structurally, some phytoestrogens resemble endogenous estrogen of humans and animals. Phytoestrogens exhibit estrogen agonist/antagonist properties and have many biological effects such as prevention of hormone-dependent breast cancer, anti-oxidative activity, inhibition of tyrosine kinase activities and inhibition of angiogenesis. In this study we investigated whether biochanin A, a phytoestrogen, and its metabolites such genistein, p-ethylphenol and phenolic aic affect IL-4 production in EL-4 thymoma cell-line and primary lymph node cells. (omitted)
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Artemisia Folium is a preparation of dried leaves from Artemisia species and has been used traditionally to prevent or treat various kinds of woman's diseases. A similar preparation called Chinese Moxa has been used to treat rheumatism by moxibustion in Chinese medicine. A small carbohydrate fraction of approximately 1,000 dlaton from the water-soluble extract of the Artemisia Folium promoted survival of the mouse thymocytes in culture. A mouse gene array study suggested that the fraction might modulate Fas/FasL dependent apoptotic cell death and thus had influence on the survival of the thymocytes in culture. (omitted)
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Biphenyl dimethyl dicarboxylate (DDB) is a by-product produced in process of synthesizing Schizandrin-C. Generally, DDB has known to protect hepatocytes and to decrease the index of liver enzyme (e.g. GOT and GPT) in chronic hepatitis. The present study was aimed to demonstrate whether DDB can protect the brain cell, especially the Alzheimer brain in vitro. As Alzheimers disease can be induced by activated microglia, a macrophage in the brain, through Abeta peptide (A
$\beta$ ) produced from amyloid precursor protein (APP). (omitted) -
Vibrio vulnificus, a Gram-negative estuarine bacterium, is the causative agent of food-borne diseases, such as life-threatening septicemia. V. vulnificus penetrating into the intestinal epithelial barrier stimulates an inflammatory response in the adjacent intestinal mucosa. Therefore, interaction between V. vulnificus and intestinal cells is important for understanding of both the immunology of mucosal surfaces and V. vulnificus. In this study we investigated the effects of V. vulnificus infection on cytokine gene expression of human intestinal epithelial cells, Caco-2 and INT-407 cells. (omitted)
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Kim, Hyung-Soo;Park, Jae-Hyun;Ryu, Mi-Hyun;Lee, Jong-Kwon;Eom, Juno-H;Byun, Jung-A;Oh, Hye-Young 132.3
The purpose of this study was to investigate the effect of manufacturing process for food on allergenicity of soybean or soybean products. Crude extracts of each soybean (SB), weaning diet A (WA) and B (WB) or soybean paste C (SC) and D (SD) were digested a simulated gastric fluid (SGF) to characterize the physicochemical stability of allergens. Allergens of each smaple except a SB (82, 39, 35 kDa) were not rapidly digested in SGF. The endogenous allergens in each sample were separated by gel electrophoresis and immunobloted with serum from soybean-sensitive patients of normal subjects. (omitted) -
Yun, Yun-Ha;Han, Shin-Ha;Lim, Hee-Jung;Park, Eun-Jung;Son, Han-Shik;Lee, Seung-Jeong;Lee, M-In-Won;Lim, Yeong-Seon;Kim, Kyung-Jae 133.1
The antidiabetic effect of Cordyceps militaris (CM) extracted fractions, Fl (CCCA, Crude Cordycepin Containing Adenosine), F2 (Ethanol precipitation), F3 (Ethanol soluble supernatant) and F4 (fraction of through SK-1B), was investigated in streptozotocin (STZ)-diabetic mice. The results indicated F3 of CM lowered the blood glucose level than control in STZ-diabetic mice. High blood glucose was induced in mice by intraperitoneal injections of STZ (150 mg/kg). The F3-ESS, which contents cordycepin, strongly showed inhibitory actibity by 33.4% in mice loaded with starch (2 g/kg). (omitted) -
Lee, Hyun-Ah;Kim, Eui-Jin;Yu, Jeong-Jun;Shu, Soo-Won;Ko, Young-Hyeh;Baek, So-Young;Park, Jin-Hee;Lee, Hong-Gi 133.2
The major hurdle of conventional chemotherapeutics is the toxicity to normal tissue. The possible therapeutic advantage(s) of nano-particle encapsulated chemotherapeutics (nano-molecules) may be the enhanced permeability and retention (EPR) effect. Nano-molecules with increase volume may incorporated into the tumor tissue selectively, which is composed of rather sparse structure. EPR effect may cause of increased effectiveness with lower tixicity to normal tissue of nano-chemotherapeutics. (omitted) -
In regard to
$A\beta$ toxicity and AD, reactive oxygen species (ROS) are produced by macrophage families in response to$A\beta$ stimulation. In addition to this, neurotrophins (NTs) regulate the neuronal function as well as cell survival and the growth of various types of neurons in both the peripheral nervous system (PNS) and central nervous system (CNS). As high expressions of the ROS and NTs are a routine findings in neuronal cell damage, we wanted to investigate whether Rg3 can inhibit the production of ROS and NTs primary cell cultures. (omitted) -
We examined the minimal amino acid sequence of bovine lactoferricin (Lfcin-B), a cationic peptide corresponding to residues 17-41 near the N-terminus of bovine lactoferrin, to induce apoptosis in THP-l human monocytic leukemic cells using synthetic peptides. A synthetic peptide (Lfc-17/29, amino acid sequence; FKCRRWQWRMKKL) which is consist of 13 amino acids near the N-terminus of Lfcin-B induced cell death in THP-1 cells in a dose-dependent manner, showing apparent apoptotic changes such as hypodiploid forms of genomic DNA and apoptotic DNA fragmentation. (omitted)
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The rat mast cell line RBL-2H3 contains both phospholipase D (PLD)1 and PLD2. Previous studies with this cell line indicated that expressed PLD1 and PLD2 are both strongly activated by stimulants of secretion. We now show by use of PLDs tagged with enhanced green fluorescent protein that PLD1, which is largely associated with secretory granules, redistributes to the plasma membrane in stimulated cells by processes reminiscent of exocytosis and fusion of granules with the plasma membrane. (omitted)
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Cho, Jun-Young;Kim, Kwang-Dong;Kho, Chang-Won;Park, Sung-Goo;Chung, Kyeong-Soo;Lim, Jong-Seok 135.2
Plasma membrane blebs are observed in many types of apoptotic cells, but their processes of formation remain to be clarified. In the present study, we investigated whether there is a relationship between change of intracellular phosphotyrosine levels and biochemical apoptotic events in Jurkat T cells undergoing apoptosis by agonistic anti-Fas antibody. When Jurkat cells were treated with Fas-antibody in the presence or absence of pretreatment with sodium orthovanadate ($Na_3${VO}_4$ ), a phosphotyrosine phosphatase (PTPase) inhibitor, membrane blebs disappeared in orthovanadate-treated cells. (omitted) -
Chung, Young-Mee;Kim, Seong-Woo;Chun, Hyung-Ok;Kim, Young-Gi;Kim, Hyun-Ah;Kim, Yeon-Hee;Ha, Suk-Hoon;Chae, Myeong-Yun;Park, Wan-Je 135.3
In the present study, type A influenza live virus, NC-22-8, which is a combination of a cold-adapted attenuated donor virus (HTCA-A101) and a wild type virus (A/New Caledonia/20/99), was constructed and the efficacy of this new virus was assessed by immunogenicity and protection tests in the mouse model. NC-22-8 (1'$10^7, 1'10^5, 1'10^3$ pfu/mouse) was intranasally administered to mice. Four weeks later, the titers of specific IgG and haemagglutinin inhibiton (HI) were measured from blood and the titer of secretary IgA (sIgA) was also detected from boncho alveolar lavage (BAL) and mucosal fluid. (omitted) -
$\beta$ -amyloid (A$\beta$ ) peptide produced from amyloid precursor protein (APP) is a major cause of Alzheimer's disease (AD). Therefore, in early phase of AD, imbalance of the production and the clearance of$A\beta$ is regarded as an important factor to progressive AD presenting senile plaque, a hallmark of AD. In the present study, we wanted to verify whether Rg3 can playa role in helping microglia engulfing$A\beta$ peptides. Validations for the study was conducted by using DiI-Ac-LDL, which attached only on type A macrophage scavenger receptor (MSR-A) and ligands for he receptor, fucoidan. (omitted) -
Previously, we showed that cyclosporin A and tacrolimus, but not rapamycin, inhibit MHC class I-restricted presentation of exogenous antigen in dendritic cells (DCs). We further characterized the effects of cyclosporin A and tacrolimus on the uptake, processing and cross-presentation of a model antigen, ovalbumin (OVA), in DCs. Treatment of DCs with cyclosporin A or tacrolimus did not inhibit phagocytic activity of DCs. Instead, treatment of DCs with cyclosporin A or tacrolimus inhibited the expression of
$H-2K^b$ / molecules complexed with the OVA peptied, SIINFEKL, specifically. (omitted) -
We investigated immunoactivity of ginkgolides (GLS), the primary active constituent of Ginkgo biloba leaves, against disseminated candidiasis due to Candida albicans. This fungus is a polymorphic opportunistic pathogen. BALB/c mice were induced neutropenia by intraperitoneal (i.p.) injection of cyclophosphamide (CP) 24 hours before an i.p administration of GLS (2 mg/mouse) to the mice. Control mice received diluent (Dulbecco's phosphate saline solution; DPBS) instead of GLS. (omitted)
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Dendritic cells (DCs) are known to professional antigen presenting cell (APC). Due to the role as an effective activator of cytotoxic T Lymphocytes by expressing MHC, adhesion and co-stimulatory molecules, DCs are now widely recognized to play an important role in the immune responses to tumors.We investigated the effect of cultured DCs in murine melanoma pulmonary metastasis model. To follow the metastasis protocol, syngenic melanoma cells were inoculated intra-venously into the mouse (B16F10 into the C57BL/6)8 days prior to the first DC injection (1
$\times$ 106 DCs/ mouse, i.p.) and the autologous tumor cell lysate pulsed-DCs were injected as a therapeutic module twice in two weeks. (omitted) -
The major active components of EGb 761, extract of Ginkgo biloba leaves, include flavonoid glycosides and unique diterpenes known as ginkgolides. Ginkgolides are potent inhibitors of platelet activating factor. In this study, we investigated antiinflammatory activity of ginkgolides on the Complete Freund"s Adjuvant (CFA)-induced mice. The ginkgolides were extracted from commercially available EGb 761. This extracting procedure was done by sequential treatments of the EGb 761 with chloroform, methanol, and water. (omitted)tted)
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Inflammatory responses from activated microglia are one of major causes of Alzheimer's disease (AD). Particularly, proinflammatory cytokines (PC), such as IL-l
$\beta$ and TNF-$\alpha$ , and nitric oxide (NO) are correlated with AD by inducing the chronic inflammation in the brain. In the present study, we found that microglia are activated by lipopolisaccharide (LPS) and Abeta42 (A$\beta$ 42), and those activated microglia produced such repertoires up to 72h with a turning point at 24h. However, no dose dependecy was found during the chasing time courses (6h to 72h). (omitted) -
Apoptosis has been implicated as an important mediator in immunosuppression observed in a depleted nutritional state. The recent report has indicated that IFN-
$\gamma$ treated bone marrow macrophages were protected from apoptosis induced by several stimuli in complete medium condition. However, our previous study demonstrated that IFN-$\gamma$ treated peritoneal macrophages were enhanced the apoposis in a depleted nutritional state. Therefor, we investigated the apoptotic regulatory mechanism of IFN-$\gamma$ in malnutrition-induced macrophage. (omitted) -
Since radiotherapy has been suspected to promote tumor metastasis and the presence of increase levels of adhesion molecules have implications for metastasis, we decided to investigate whether gamma-irradiation alters the expression of intercellular adhesion molecule-1 (ICAM-1) on neuroblastoma cells and the activities of relevant intracellular signaling molecules. In the present study, the relative of ICAM-1 expression under gamma-irradiated neuroblastoma cells were assessed by Western blot analysis. (omitted)
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Han, Shin-Ha;Lee, Seung-Jeong;Song, Young-Cheon;Lim, Hee-Jung;Lee, Chong-Kil;Kwon, Oh-Seung;Ha, Nam-Joo;Kim, Kyung-Jae 139.2
The in vitro effects of extracted fractions of C. militaris on the secretion of cytokines in murine macrophage cell line, RAW 264.7 were studied. F1 (crude cordycepin containing adenosine), F2 (ethanol precipitation), F3 (ethanol soluble supernatant) and F4 (fraction of through SK-1B) significantly stimulated the production of cytokine and nitric oxide (NO) on murine macrophage cell line RAW264.7. We examined how the ethanol extract of C. militaris regulates production of interleukine 1-beta(IL-1$\beta$ ), tumor necrosis factor-alpha (TNF-$\alpha$ ), and NO in vitro. (omitted) -
Lee, Seung-Jeong;Han, Shin-Ha;Park, Eun-Jung;Lee, Chong-Kil;You, Byeong-Jin;Cho, Kyung-Hee;Ha, Nam-Joo;Kim, Kyung-Jae 140.1
Permanent cell culture lines derived from human cancer tissue are important experimental models in the study of human cancer cell proliferation. The in vitro effects of C. militaris and its extracted fractions on the human breast cancer (SK-BR3), liver cancer (SK-Hep1, HepG2), kidney cancer (p15), lymphoma (Jurkat) were studied. F1 (CCCA, crude cordycepin containing adenosine), F2 (ethanol precipitation), F3 (ethanol soluble supernatant) and F4 (fraction of through SK-1B) significantly stimulated in vitro cytotoxic in human cancer cell lines. (omitted) -
Isoflavone found in Leguminosae is one of natural phytoestrogens and its effect on bone remodeling is one of key investigational interests in terms of estrogen replacement therapy (ERT). As commonly known, osteoporosis is one of hormonal deficiency diseases, especially in menopausal women. When estrogen is blocked, local factors such as 1L-1
$\beta$ and IL-6 that are related in bone resorption are increased and enhance osteoclastogenesis, which is responsible for bone resorption. In the present study, we investigated the effect of isoflavones (Isocal) extracted from Sophorae Fructus on bone resorption in vitro. (omitted) -
Isoflavones have been a central subject in natural phytoestrogens found in Leguminosae. Their effects on bone formation and remodeling are an important turning point in that they can act like estrogen by binding on estrogen receptors on target cell surface. We, therefore, believed that isoflavones may be applied in estrogen deficiency disease such as osteoporosis in terms of estrogen replacement therapy (ERT). As commonly known, osteoporosis is one of hormonal deficiency diseases, especially in menopausal women. (omitted)
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Paraoxonase, an antioxidant enzyme, exclusively located on HDL is well known for both hydrolysis of organophosphate and prevention against LDL oxidation. It have been reported that PON1 decrease its activity under oxidative stress and that PON1 activity is lower in subject with higher vulnerability to organophosphate poisoning. The aim of our study is to examine the effect of oxidative system on paraoxon-hydrolzing activity and to elucidate the plausible mechanisms responsible for the decline of HDL-asscociated PON1 activity in vivo system. (omitted)
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beta-Amyloid (A
$\beta$ ) peptide is the major component of senile plaques and considered to have a causal role in the development and progression of Alzheimer's disease. There has been compelling evidence supporting that$A\beta$ -induced cytotoxicity is mediated through oxidative and/or nitrosative stress. Recently, considerable attention has been focused on dietary manipulation of oxidative and/or nitrosative damage. L-Egrothioneine (EGT) is a low-molecular weight naturally occurring thiol compound of dietary origin which exists in milimolar concentrations in the brain, liver, kindney, erythrocytes, ocular tissues and in seminal fluids of mammals. (omitted) -
Sensitive and safe method for visualization of DNA in agarose gels using visible dye is described. To improve the sensitivity, we studied a counterion-dye staining method using methyl orange as a counterion-dye which contributes to reduce excessive background staining by indoine blue. Dye concentrations, PH of staining solution, mixing molar ratio of two dyes, and staining times were optimized for the counterion-dye staining. By the staining with a mixed solution of 0.005% indoine blue and 0.00165% methyl orange in 10% ethanol 0.2M sodium acetate, 8 ng of the 3 kb DNA in an agarose gel was detected within 1hr. (omitted)
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The activation of the hepatic stellate cell (HSC) is a key step in liver fibrogenesis. We investigated the changes of global gene expression during activation in hepatic stellate cells using a rat cDNA microarray with 5, 000 sequence-verified clones. We identified osteopontin (OPN), a secreted matrix protein, as one of the upregulated factors. Northern analysis showed OPN mRNA was increasingly expressed during progressive activation of cultured rat HSCs and in models of experimental liver fibrosis. (omitted)
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Time-dependent PPO activity was determined at
$4^\times$C and$30^\times$C . The result of activity determination, PPO extracted by phosphate buffer containing triton x-1l4(tPPO) was more stable than PPO by phosphate buffer(bPPO). The result of electrophoresis, at first a band was appeared at 48kd. After 1-3days a partial degrade band was appeared in bPPO and three partial degrade bands in tPPO. No activity band was appeared in PPOs at$30^\times$C and bPPO at$4^\times$C after 4 days. (omitted) -
Peroxynitrite and 4-hydroxynonenal (4-HNE) are highly reactive molecules which are generated under oxidative stress condition and during aging. Many proteins in living organism are modified by them and consequently associated with various diseases including cardiovascular and neurodegenerative diseases. We hypothesize that peroxynitrite and 4-HNE modified serum proteins are also associated with aging process. To establish information on peroxynitrite and 4-HNE adducted proteins for aging study, we used proteins methods, 2D-PAGE and MALD-TOF MS, to identify modified proteins from young (70month) and old (25-month) rat serum. (omitted)
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Recent studies suggest that inflammatory events are implicated in a variety of ailments such as cancer and neurodegenerative diseases, and certain non-steroidal anti-inflammatory drugs have beneficial effects for the treatment or prevention of these disorders. Cyclooxygenase-2 (COX-2), the rate-limiting enzyme in the prostaglandin (PG) synthesis, is induced by various pro-inflammatory stimuli including nitric oxide (NO) and has been reported to cause and/or aggravate neuronal cell death. (omitted)
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We previously reported that the activation of p
$21^{WAFl/Cip1}$ transcription by histone deacetylase inhibitor apicidin was mediated through Spl sites and pointed to the possible participation of protein kinase C (PKC). In this study, we investigated the role and identity of the specific isoforms of PKC involved and identified phosphatidylinositol 3-kinase (PI 3-kinase) as an upstream effector in HeLa cells. Using an isoform-specific pharmacological inhibitor of PKC, a PKC$\varepsilon$ dominant-negative mutant, and antisense oligonucleotide to inhibit PKC$\varepsilon$ specifically, (omitted) -
Reactive Oxygen Species (ROS) are produced during normal cellular function. ROS are very transient species due to their high chemical reactivity that leads to lipid peroxidation and oxidation of some enzyme, massive protein oxidation and degradation. Under normal conditions, antioxidant are substances that either directly or indirectly protect cells against adverse effects of ROS. Several biologically important compounds have been reported to have antioxidant functions. These incluce vitamin C, vitamin E, GSH, flavonoids. superoxidee dismutase(SOD), glutathione peroxidase(GPX) and catalase(CAT). (omitted)
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Oxidative stress has been implicated in a range of disease states, including end-stage renal failure treated with hemodialysis [Westhuyzen J. et al, 2003]. Free radicals react with biological molecules and destroy the structure of cells, which eventually causes free-radical induced disease such as cancer, renal failure, aging, etc. Exogenous or endogenously produced nitric oxide (NO) inhibits superoxide-stimulated urea permeability. In the inner medulla, superoxide generation by local oxidases may stimulate urea transport, and the role of endogenous No may be to dampen this effect by decreasing superoxide levels [Zimpelmann J. et al, 2003 (Epub ahead of print)]. (omitted)
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We have developed a silver staining method using a dye as a silver sensitizer. Dye staining is performed in combination with silver nitrate staining. Dye-silver staining shortens the time of silver staining (~1 hr) and improves the sensitivity better than that of silver diamine stain (1-10 ng) or comparable to that of silver nitrate stain with glutaraldehyde as a silver sensitizer. In dye staining (silver sensitizing step), it has been proven that the sensitivity is at least 4 times comparing with that of CBBR stain and staining time is about 45 min. (omitted)
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Transgenic Eleutherococcus senticosus plants were prepared by introducing the genes for squalene synthase (SQS), hygromycin phosphotransferase (HPT) and green fluorescent Protein (GFP) through Agrobacterium-mediated transformation. The enzyme, SQS, represents a putative branch point in the isoprenoid pathway capable of diverting carbon flow specifically to the biosynthesis of phytosterol and oleanolic acid. The full SQS gene was isolated from P. ginseng roots. Early globular embryo clusters developed from embryogenic callus were used as the explant source. (omitted)
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A major protein was isolated from ginseng root (Panax ginseng C.A. Meyer) using a combination of ammonium sulfate fractionation, gel filtration chromatography, ion-exchange FPLC. Electrophoretic and gel permeation chromatographic studies revealed that the major protein, GMP, is composed of two subunits of approximately 28 kDa. In this, investigated the ability of GMP to inhibit the oxidation of low-density lipoprotein (LDL). GMP inhibited
$Cu^{2+}$ (5$\mu$ M)-promoted oxidation of LDL (125$\mu$ g protein/mL) in a dose-dependent mamer (0~5$\mu$ M), with a maximal inhibitor at GMP/copper ratio of 1:10 and an$IC_{50}$ value of 0.2$\mu$ M, as determined by measurement TBARS. (omitted) -
The benzoxathiol LYR-71 compound was discovered as an inhibitor of NF-kB transcriptional activity with an IC50 value of 5.4 uM. Furthermore, benzoxathiol LYR-71 compound inhibited the NF-kB binding activity to DNA in a dose-dependent manner, which was identified by EMSA with oligonucleotide corresponding to NF-kB consensus sequence. It is well known that NF-kB is an important transcription factor to regulate the expression of inflammatory enzymes (iNOS and COX-2) and cytokines (TNF, IL-1 and IL-6). (omitted)
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As an attempt to search for bioactive natural products exerting antiinflammatory activity, we have evaluated the anti-inflammatory and antinociceptive activities of the methanol extract from the Fomes fomentarius (MEFF). MEFF (50, 100 mg/kg/day, p.o.) significantly reduced an acute paw edema induced by carrageenan in rats. When analgesic activity was measured by acetic acid-induced writhing test and hot plate test, MEFF showed a dose-dependent inhibition in animal models. In addition, MEFF potently inhibited the LPS-induced production of NO,
$PGE_2$ and TNF-$\alpha$ production of macrophages. (omitted) -
A fast and matrix-assisted laser desorption/ionization-mass spectrometry compatible protein staining method in one- and two-dimensional sodium dodecyl sulfate-polyacrylamide gel electrophoresis is described. It is based on the counterion dye staining method that employs oppositely charged two dyes, Zincon and Ethyl Violet to form an ion-pair complex. It is safe to use since the methanol used previously in staining solution was replaced with ethanol, which is not toxic. The protocol including fixing, staining and quick washing steps can be completed in 1 to 1.5 h depending upon gel thickness. (omitted)
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Recently, there have been considerable efforts to search for naturally occurring substances for the intervention of carcinogenesis. Curcumin, a yellow coloring ingredient of turmeric (Curcuma longa L., Zingiberaceae), has been shown to inhibit experimental carcinogenesis and mutagenesis, but molecular mechanisms underlying its chemopreventive activities remain unclear. In the present work, we found that curcumin inhibited 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced expression of CPX-2 in female ICR mouse skin when applied topically 30 min prior to TPA as determined by both immunoblot and immunohistochemical analyses. (omitted)
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Ceramide is an important lipid messenger involved in mediating a variety of cell functions including apoptosis. Previously, we have shown that ceramide induces Bax translocation which is associated with cytochrome c release from the mitochondria. In this study, we show that p38 MAP kinase is involved in ceramide-induced Bax translocation. In human leukemic cells, ceramide stimulated the phosphorylation of p38 MAP kinase. Preincubation of cells with SB203580, a specific inhibitor of p38 inhibited DNA fragmentation induced by cell-permeable ceramide. (omitted)
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Recently we have reported that various hydroxystilbenes show strong inhibition of human cytochrome P450 1 enzyme activities. A series of syntheic trans-stilbene derivatives were prepared and their inhibitory potentials were evaluated with the bacterial membrane of recombinant human cytochrome P450 1A1, 1A2 and 1B1 coexpressed with hyman NADPH-P450 reductase to find a new inhibitor of cytochrome P450 enzymes. Of the compounds tested, SY-081 exhibited a potent inhibition of human cytochrome P450 1B1 with an
$IC_50$ value of 2.6 nM. (omitted) -
We have previously shown that 2,4,3',5'-tetramethoxystilbene (TMS), a synthetic trans-stilbene analogue, is one of the most potently selective inhibitor of human cytochrome P450 1B1 in vitro and in vivo. In the present studies, the apoptotic effects of TMS were investigated in HL-60 cells. The effects of TMS on the proliferation of HL-60 cells were determined with MTT assay. TMS exhibited cytotoxicity with an
$IC_50$ value of 37 nM. Cotreatment with TMS and etoposide, a well-known anticancer drug significantly enhanced the cytotoxicity. (omitted) -
Nitric oxide (NO) is known to work as an important signaling molecule involved in regulating a wide range of biological activities in the neuronal, vascular, and immune system. NO and its metabolites mediate a number of host defence functions and are also implicated in the pathogenesis of tissue damage associated with inflammation. Cyclohexylimminobenzoxathiol LYR-64 compound inhibited LPS-induced NO production in murine macrophages Raw264.7 with an IC50 value of 0.7 uM with 95.9% inhibition at 3 uM, 63.5% at 1 uM and 30.2% at 1 uM. (omitted)
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[6]-Gingerol, a major pungent ingredient of ginger (Zingiber officinale Roscoe, Zingiberaceae) has a wide array of pharmacologic effects. Our previous studies have demonstrated that [6]-gingerol inhibits mouse skin tumor promotion and anchorage-independent growth of cultured mouse epidermal cells stimulated with epidermal growth factor. In this study, we have investigated the molecular mechanisms underlying anti-tumor promoting effects of [6]-gingerol on mouse skin carcinogenesis. (omitted)
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Gelsolin, a actin binding protein, has been demonstrated to be involved in controlling cell morphology, motility, signaling, and apoptosis. It's expression is frequently downregulated in cervix cancer and several types of different human cancers indicating the role of gesolin in suppression of tumorigenicity. Apicidin, a novel histone deacetylase inhibitor, has been shown to cause growth arrest and morphological change of cancer cells, resulting from the alternation of protein expression, such as
p21^${WAF1/Cip1}$ and gelsolin. (omitted) -
We have focused on various biological activities of acharan sulfate (AS) isolated from the giant African snail Achatina fulica. In a previous study, AS showed antiangiogenic and immunomodulating activity. We also investigated antitumor activity of AS. In vitro AS had no cytotoxicity within 0 to 200 ug/ml in tumor cells such as Lewis lung carcinoma(LLC) , KM1214 (human colon cancer cell) and Caki-1 (human kidney cancer cell) by both MTT and SRB assay. In vivo AS was used to treat C57BL/6 mice bearing LLC by subscutaneous injection. (omitted)
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Polyunsaturated fatty acids (PUFAs) play many important physiological roles on cellular process through the regulations of intracellular signaling. Recent clinical studies suggest that PUFAs such as n-3 fatty acids (docosahexaenoic acid, 22:6 and a-lnolenic acid, 18:3) may reduce the risk of incident Alzheimer's disease (AD). And also the reports regarding the decrease of n-3 fatty acids in AD brain support the correlation between PUFAs and AD. AD is a neurodegenerative disorder with pathological hallmarks of amyloid plaques and neurofibrillary tangles. (omitted)
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For the purpose of the development of a skin-whitening agent, Sophora flavescens was evaluated for tyrosinase inhibitory activity and its active principles were identified followed activity-guided isolation. The ethanol extract and dichloromethane fraction from S. flavescens showed significant inhibition of mushroom tyrosinase. From the dichloromethane fraction, three known prenylated flavonoids, sophoraflavanone G, kuraridin, and kurarinone, were isolated. Compared with kojic acid (
$IC_50$ =20.5$\mu$ M), these compounds possessed more potent tyrosinase inhibitory activity. (omitted) -
Aromatic diamine JSH-21 showed an IC50 value of 9.2 uM with 74.5% inhibition at 30 uM, 53.5% at 10 uM and 24.5% at 3 uM on LPS-induced NO production in murine macrophages Raw 264.7. To examine whether inhibitory effect on NO production by JSH-21 was attributed to influence on iNOS expression, iNOS transcript and protein were analyzed by sequantitative RT-PCR and immunoblot analysis. Consistent with previous result on NO production, treatment of the Raw 264.7 cells with JSH-21 decreased the LPS-induced expression of iNOS transcript and protein in a dose-dependent manner with IC50 values of about 10 uM. (omitted)
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Under the vigorous search for active novel agents for cancer prevention and treatment, some agents have been found from plants and animals which are easily available. Our review of literature on them revealed that C. annuum L. var. angulosum Mill had high antiproliferating effect on cancer cells. Thus we investigated the efficacy of C. annuum L. var. angulosum Mill on cancer cell lines and to examined its effect on the mouse to detect other side effect and mechnism by which the extrat of C. annuum L. var. angulosum Mill had the anti-cancer efficacy on cancer. (omitted)
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${\beta}Although$ it has been demonstrated that$p2l^{WAFl/Cip1}$ , a well known cell cycle inhibitor, could be induced by$TGF-{\beta}$ in a p53-independent manner, the detailed signal transduction pathways still remain poorly understood. In this study, we show that ERK is required for$TGF-{\beta}$ induction of$p21^{WAF1/Cip1}$ , but JNK or p38 MAPK is not. ERK activation by$TGF-{\beta}$ significantly attenuated by treatment with ROS scavenger such as NAC or catalase, indicating that ROS, mainly$H_2O_2$ , generation by$TGF-{\beta}$ might stimulate ERK signaling pathway to require the induction of$p21^{WAF1/Cip1}$ . (omitted) -
Oxidative stress induced by reactive oxygen intermediates (ROIs) has been implicated in a variety of human diseases including cancer, diabetes, rheumatoid arthritis and neurodegenerative disorders. Hydrogen peroxide (
$H_2O_2$ ), a representative ROI which is produced during the cellular redox process, can cause cell death via apoptosis and/or necrosis depending on its concentrations. l5-Deoxy-$D^{12, 14}$ prostaglandin$J_2$ (15d-$PGJ_2$ ), a dehydration product of prostaglandin$D_2$ , has been reportd to possess a number of biological activities such as anti-inflammatory, anticarcinogenic, and antioxidative properties. (omitted) -
Extracts of Artemisia asiatica Nakai (Asteraceae) possess anti-inflammatory and anti-oxidative activities. Eupatilin (5,7-dihydroxy-3,4,6-tri-methoxy-flavone), one of the pharmacologically active ingredients derived from Artemisia asiatica, was shown to induce apoptosis in human promyelocytic leukemia (HL-60) cells (H.-J. Seo and Y.-J. Surh, Mutat. Res., 496, 191-198, 2001). In the present study, we examined the cytostatic effects of eupatilin in H-ras-transformed human breast epithelial (MCF10A-ras) cells. (omitted)
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TCTP is presented to have a retinol binding protein (RBP)-like structure by domain search. Human cellular RBP (CRBP) plays a key role in the intercellular transfer of retinol. Modulation of its expression is known to contribute to tumor growth and progression via retinoid-mediated signaling. Changes in the expression of TCTP have also been reported to be associated with carcinogenesis. Therefore, the attempt to establish the interactive relationship between the human TCTP and CRBP with retinol will be helpful in further understanding the cell signaling of TCTP. (omitted)
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Mammalian cell cycles are tightly regulated by cyclins, cyclin dependent kinase (CDK), Retinoblatoma (Rb) protein, and cellular CDK inhibitors (CDKI). Cyelin dependent kinases (CDK) are key enzymes regulating eukaryotic cell cycle. And also it is recognized that the abnormal increase of CDK activities is one of the common events in human cancer and CDK inhibitors have therapeutic values in cancer treatment. Until now it is known that over 10 different CKDs participate in cell cycle regulation. (omitted)
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Polyphenol QGR (quercetin 3-O-beta-(2"-galloyl)-rhamnopyranoside) was isolated from Persicaria lapathifolia (Polygonaceae). In this study, we investigated inhibitory effects of QGR and its building blocks (quercitrin, quercetin and gallic acid) on superoxide anion and NO productions in unopsonized zymosan-stimulated murine macrophages Raw264.7. QGR and quercetin showed potent inhibitory effects on unopsonized zymosan-induced superoxide anion production with IC50 values of 3.2 uM and 4.8 uM, respectively. (omitted)
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We previously reported the antimutagenicity, anti-lipid peroxidation and antiinflammtory properties of the three Chinese herb medicine, Kalopanax pictus, Pueraria thunbergiana and Rhus verniciflua, which have been used as therapeutics for diabetes mellitus and inflammation in Korea. Since these drugs have been used for the prescriptions consisted of several crude drugs, we investigated whether the extract of the three drugs could increase the individual drugs or not. The three extracts were independently prepared from K. pictus, P. thunbergiana, and R. verniciflua, which extracts were named the K-1, P-1 and R-1 in this order and the extract (KPR-1) was also prepared from the combined plant materials with each same weight of the three drugs. (omitted)
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Flavonoids from plant origin show anti-inflammatory activity in vitro and in vivo. In addition to inhibition of inflammation-associated enzymes such as cyclooxygenases and lipoxygenases, they have been found to regulate the expression of inflammation-associated proteins from in vitro experiments. In order to prove in vivo behavior and the potential for beneficial use against inflammatory skin disorders, the effect of wogonin (5,7-dihydroxy-8-methoxyflavone) on in vivo expression of several inflammation-associated genes was examined in the intact as well as in the inflamed mouse skin by reverse transcriptase-polymerase chain reaction analysis. (omitted)
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Cerarmide acts as a lipid second messenger in the cellular signal transduction and is involved in mediating a variety of cell functions such as proliferation, differentiation, growth arrest, and apoptosis. In the present study, we have investigated the effect of ceramide on cellular cytotoxity and reactive oxygen species (ROS) to understand the relationship between them. Ceramide treatment significantly increased cell death in RAW 264.7 murine macrophages activated with lipopolysaccharide (LPS) and interferon-g (IFN-g). (omitted)
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Lipopolysaccharide (LPS)-stimulated macrophages produced a large amounts of nitric oxide (NO) by inducible nitric oxide synthase (iNOS). This is an important mechanism in macrophages-induced septic shock and inflammation. In the present study, we tested a synthetic propenone compound, l-furan-2-yl-3-pyridin-2-yl-propenone (FPP-3) for its ability to inhibit the production of tumor necrosis factor-a (TNF-
$\alpha$ ) and an inducible enzyme, iNOS, in the LPS-stimulated murine macrophage-like cell line, Raw264.7. FPP-3 consistently inhibited nitric oxide (NO) and TNF-$\alpha$ production in a dose dependent manner, with$IC_50$> values of 10.0 and 13.1$\mu$ M, respectively. (omitted) -
This study was carried out to evaluate the cytotoxicity and anti-inflammatory effects of Resina Pini on cultured human gingival fibloblasts. We carried out a study of cytotoxic effects of Resina Pini on cultured cells by MTT assay. Various treatments on Resina Pini reduced its toxicity on cultured cells in order of natural Resina Pini, water extracted mixture of Resina Pini and Ramus Mori Albae and recrystalized Resina Pini. However, Resina Pini showed harmless levels of cytotoxicity to cultured human gingival fibroblast. (omitted)
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Panax ginseng is one of the most important medicinal plant in the Orient. The international trade of ginseng is increasing yearly. The disguise of Chinese and American ginseng into Korean ginseng became a problem in recent years in Korea and an abroad. Obviously, an effective method of authentication of Korean ginseng from others at a DNA level, is necessary for the healthy development of the ginseng market. In order to develop convenient and reproducible methods for the identification of Korean ginseng, amplified fragment length polymorphism (AFLP) analysis was applied within Panax species (Korean cultivatied and wild ginseng, Chinese wild ginseng, American cultivatied and wild ginseng). (omitted)
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The antioxidant and anticancer properties of a medicinal plant, Betula platyphylla var. japonica were investigated. The total methanol extract of B. platyphylla var. japonica had protective effects against hydrogen peroxide (
$H_2O_2$ ) in the Chinese hamster lung fibroblast (V79-4) cell line and induced apoptotic cell death in human promyelocytic leukemia (HL-60) cells, a cancer cell line. B. platyphylla var. japonica extract significantly increased cell viability against$H_2O_2$ . The extract also showed high 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity ($IC_50$ 2.4 mg/ml) and lipid peroxidation inhibitory activity ($IC_50$ below 4.0 mg/ml). (omitted) -
We report here the results on N-acetyl-N"-methylamide of oxazolidine (Ac-Oxa-NHMe) calculated using the ab initio molecular orbital method with the self-consistent reaction field (SCRF) theory at the HF level of theory with the 6-31 +G(d) basis set. The displacement of the
$\gamma$ -$CH_2$ group in proline ring by oxygen atom has affected the structure of proline, cis-trans equilibrium, and rotational barrier. The up-puckered structure is found to be prevalent for the trans conformers of the Oxa amide. (omitted) -
Vitamin K-related analogs induce growth inhibition in various cancer cell lines. We report that 2,3-dichloro-5,8-dihydroxy-1, 4-naphthoquinone (DDN), a naphthoquinone analog, induces mitochondria-dependent apoptosis in human promyeloid leukemic HL-60 cells. DDN induced cytochrome c release, cleavage of Bid, and activation of caspases -8, -9 and -3. Cleavage of Bid, the caspase-8 substrate, was inhibited by the broad caspase inhibitor zVAD-fmk, whereas cytochrome c release was not affected by zVAD-fmk. (omitted)
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Human Topoisomerase I (topo I) helps the control of DNA supercoiling in cells by assisting breaking and religation of DNA strand. It is essential for cellular metabolism and survival, hence, a good target for a novel class of anticancer drugs. As topo I inhibitor binds to the DNA-topo I complex, the religation of DNA strand is suppressed which results in the death of the target cell. Seven compounds of H-Imidazo[4, 5-g]phthalazing-4, 9-dione derivatives with
$IC_50$ in the range of 0.001 and 6.27$\mu$ M in 5 different cancer cells and four compounds of 7-chloro-6-quinazoline-5, 8-dione derivatives with positive and negative topo I inhibition activities were studied. (omitted) -
Codonopside lc is an active natural compound isolated from the roots of Codonopsis lanceolata (Campanulaceae), a Korean medicinal herb. In the present study, we investigated the in vitro effect of Codonopside 1c on the proliferation and induction of apoptosis in HL-60 human promyelocytic cells. When HL-60 cells were treated with Codonopside 1c, evidence of apoptotic features, including DNA fragmentation, formation of DNA ladder in agarose gel elecrophoresis and increse of annexin V binding, were obtained. (omitted)
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It has been known that quercetin is one of bioflavonid compounds and has anti-tumor effect by suppressing tumor growth in vitro and in vivo, including multiple biological effects by antioxidant and effective anti-inflammatory agent. The present study investigated whether quercetin can enhance antioxidant enzyme activity (glutathione proxidase: GPX, superoxide dismutase: SOD, catalase: CAT) and regulate the intracellular reactive oxygen intermediate levels on the B16F10 murine melanoma cells in the presensece of vitamin E, L-ascorbic acid (vitamin C) and reduced glutathione (GSH). (omitted)
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In order to confirm the biological function of ORF10 in cephabacin biosynthesis gene cluster of Lysobacter lactamgenus as an ATP-binding-cassette (ABC) transporter, the gene for ORF10 was amplified and subcloned into pET-28a(+) expression vector. After gene induction with 0.5 mM IPTG at 30~! and further cultivation at
$30^~$ !. for 8 hr, a lot of the recombinant ORF10 protein was produced as soluble form in cytoplasmic fraction as well as a membrane protein in the membrane fraction as likely as other ABC transporters. (omitted) -
When ginsenoside
$R_{b1}$ and$R_{b2}$ were anaerobically incubated with human fecal microflora, these ginsenosides were metabolized to compound K. When ginsenoside$R_{g3}$ was anaerobically incubated with human fecal microflora, the ginsenoside$R_{g3}$ was metabolized it to ginsenoside$R_{h2}$ . Among ginsenosides, compound K and 20(S)-ginsenoside$R_h2$ exhibited the most potent cyotoxicity against tumor cells: 50% cytotoxic concentrations of compound K in the media with and without fetal bovine serum (FBS) were 27.1 - 31.6 mM and0.1 - 0.6 mM, and those of 20(S)-ginsenoside$R_h2$ were 37.5$\rightarrow$ 50 and 0.7 - 7.1 mM mM, respectively. (omitted) -
Aldehyde and active form of free oxygen produced in alcohol metabolism in liver are the cause of liver cell damage. The main system of alcohol metabolism is composed of alcohol dehydrogenase(ADH), aldehyde dehydrogenase(ALDH) and cytochrome P4502E1. Alcohol dehydrogenase is reversible in alcohol metabolism. To block the backward reaction and enhance alcohol oxidation, acetaldehyde trapping agents were assayed. The assay was carried out by measuring decreasing NADH at 340nm, using acetaldcehyde and NADH as substrate and coenzyme respectively. (omitted)
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Two chitosanses produced by Aspergillus fumigatus KB-1 were purified by ion exchange and size exclusion chromatographies. Molecular weights of chitosanses were 111.23 KDa (chitosanase I) and 23.38 KDa (chitosanase II). The N-terminal amino acid sequence of chitosanase II was determined: YNLPNNLKQIYDKHKGKXSXVLAK(\ulcorner)GFTN. The optimum pH of the chitosanase I and II were 6.5 and 5.5 respectively. The optimum temperatures were
$60^\times$C and$70^\times$ . Two chitosanases were most stable at$10^\times$C . (omitted) -
In order to investigate the pathogenic genes and genetic relationships of Y. pseudotuberculosis, we isolated 9 strains of Y. pseudotuberculosis from about 380 spring water sites in Seoul and carried out antibiotic susceptibility test, biological test and molecular typing. All isolated strains were distributed throughout the northeast area in Seoul (Mt. Bookhan, Mt. Soorak, Mt. Boolam and etc...).Antibiotic susceptibility test revealed that all the strains were susceptible to chloramphenicol, gentamicin, neomycin and amoxicillin/clavulanic acid, but were resistant to novobiocin and vancomycin. (omitted)
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Ginseng (the root of Panax ginseng C.A
$M_{EYER}$ , family Araliaceae) is frequently used as a crude substance in Asian countries as a traditional medicine. The major components of ginseng are ginsenosides, which have been reported to show various biological activities including antiinflammatory activity and antitumor effect. In addition, Sugiyama et al. reported that ginsenoside Rg3 suppresses histamine release from mast cells due to stimulation with compound 48/80 in vitro. However, the antiallergic effects of ginsenoside Rh2, which is metabolized by human intestinal bacteria to ginsenoside Rg3, have not been studied. (omitted) -
Endotoxin has been detected by the Limulus amoebocyte lysate (LAL) test. However, aluminum hydroxide used as an adjuvant and adsorbent for the recombinant protein antigen is known to increase efficacy of lipopolysaccharide vaccine in vivo thus interfering endotoxin test. The aim of this study is to determine effect of aluminum hydroxide on the LAL test using the hepatitis B vaccine as a model and to optimize the LAL test condition not to be interfered by aluminum gydroxide. (omitted)
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Microtubule-organizing center (MOTC) plays pivotal roles in cell division process. Integrity of the spindle pole body (SPB) in Saccharomyces cerevisiae is required for migration and separation of sister chromatids in mitotic phase. Role of an essential SPB component, Spcl05, is poorly understood. Here we show that throughout all stage of cell division cycle, GFP-tagged Spcl05p localizes at SPB and its protein stability is fluctuated with mitosis-specific modifications. To gain new insights into the function of Spc105, we generated and characterized novel temperature sensitive spc105 mutants. (omitted)
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The inhibitory activities of various analogues of adenosine (Group I, Group II, Group III, Group IV, Group V) were assayed by using recombinant human placental SAH hydrolase. The activity of the SAH hydrolase was determined by measuring the formation of AdoHcy from Ado and Hcy. AdoHcy was analyzed by HPLC using C18 reverse-phase column. The peak of AdoHcy was monitored at 258 nm. Among the tested compounds, fluoroneplanocin A (LJ-276) was the most potent inhibitor.
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Hwang, Young-Chol;Park, Jong-Sun;Kang, Byoung-Yong;Choi, Sung-Sook;Kim, Kyung-Jae;Ha, Nam-Joo 163.2
The genera Bifidobacterium is a member of the normal intestinal flora in humans, and important in food industry. In order to test the genetic identity of this bacterial genera, four primers originated from rice genome (SRILS Microbial$UniPrimers^{TM}$ kit) were used in molecular typing of 7 Bifidobacterial species and 20 isolates from various source. SRILS Microbial$UniPrimers^{TM}$ kit were effectively applied to genomic fingerprinting of various organism such as plant, animal and microorganism. (omitted) -
Panax ginseng C.A. Meyer (Family Araliaceae) was treated at low (
$60^{\circ}C$ , LT), mild ($100^{\circ}C$ , MT) and high ($120^{\circ}C$ , HT) temperatures, some components (panaxytriol, ginsenosides and polysaccharides) were isolated, and their inhibitory effects on growth, infection and VacA vacuolation of Helicobacter pylori (HP) were investigated. The molecular weights of polysaccharides were decreased according to the increasing processed temperature. Ginseng polysaccharides inhibited the HP infection into KATO III cells, but did not inhibit HP growth and VacA vacuolation of HeLa cells. (omitted) -
Peptide deformylase (PDF) is essential and unique to bacteria for cytoplasmic protein synthesis, but not required in eukaryotes, thus making it an attractive target for the discovery of novel antibacterial drugs. Protein synthesis in eubacteria, under normal conditions, is initiated by formyl-methionyl-tRNA. PDF removes the formyl-group of N- formylmethionine of newly synthesized polypeptides to produce a mature protein. In this study, a pdf gene from Staphylococcus aureus 6538p was cloned in pET-14b vector and transformed in Escherichia coli BL21 (DE3). (omitted)
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Kim, Myoung-Sook;Baek, Jin-Hyen;Lee, Hyo-Jong;Hwang, Bang-Yeon;Kim, Se-Eun;Lee, Jung-Joon;Kim, Kyu-Won 164.1
Wm was isolated from Cynanchum wilfordii (Asclepiadaceae) as a mixture form of polypregnane glycosides that included wilfoside K1N and wilfoside C1N. In the present study, we investigated the anti-angiogenic effect of wilfoside glycosides using in vivo and in vitro assay systems. We first demonstrated that concentrated conditioned media obtained from Wm-treated HepG2 human hepatoblastoma cells blocked the angiogenic activation of Wm-untreated concentrated conditioned media, suggesting that Wm may have an inhibitory effect on tumor-induced angiogenesis. (omitted) -
Park, Jae-Hyun;Shin, Hwa-Yean;Kang, Yun-Hee;Kang, Young-Kook;Lee, Jung-Bok;Yoon, Hyun-Soo;Ryu, Chun-Jeih;Myung, Pyung-Keun;Hong, Hyo-Jeong 164.2
Human embryonic stem (ES) cell lines derived from the inner cell mass of human blastocysts have potential to differentiate into any cell types. We have established in vitro neural differentiation of human ES cells. After the formation of embroid bodies (EBs), the differentiating EBs formed neural tube-like rosettes in the presence of basic fibroblast growth factor (bFGF). The rosettes were selectively isolated by the treatment of dispase and cultured in a medium for human neural precursors in the presence of bFGF. (omitted) -
Transforming growth factor (TGF)-
$\beta$ , a hormonally active polypeptide found in normal and transformed tissue, is a potent regulator of cell growth and differentiation. In this study, we examined the effect of TGF-$\beta$ on invasion and motility of MCF10A human breast epithelial cells. TGF-$\beta$ -induced migration and invasive phenotype of the parental MCF10A cells in a dose-dependent manner. Activity of MMP-2 promoter was increased by TGF-b, suggesting that the TGF-$\beta$ -induced invasive phenotype may possibly be mediated by MMP-2 rather than MMP-9. (omitted) -
Phosphatidylinositol 3-kinase (PI3K) and Rac play important roles that regulate cellular functions including cell survival and migration. In the present study, we investigated the functional roles of PI3K and Rac1 pathways in H-ras-induced invasive phenotype and motility of MCF10A cells. Akt, a downstream molecule of PI3K, was effectively activated not only by H-ras but also by N-ras, suggesting that the activation of PI3K pathway is not sufficient to induce metastatic potential of MCF10A cells. (omitted)
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The c-Jun N-terminal kinase (JNK) plays essential roles in apoptosis and cell survival. Because apoptosis is promoted by blocking the MEK kinase1-mediated activation of JNK1, we tested whether JNK1 plays dual roles in apoptosis. We show here that JNK1 activity is differentially up-regulated in a two-tiered fashion by specific mechanisms during taxol- or ginsenoside Rh2-induced apoptosis. The early phase of JNK1 activation, but not apoptosis is prevented by expressing the dominant negative SEK1 mutant. (omitted)
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Jung, In-Duk;Lee, Jang-Soon;Yun, Seong-Young;Park, Jun-Hong;Park, Chang-Gyo;Lee, Hoi-Young 166.1
Autotaxin (ATX) is a 125-kDa glycoprotein and a strong motogen that can increase invasiveness and angiogenesis, originally isolated from the conditioned medium of human melanoma A2058 cells. And it is a strong. Recently, we suggested that ATX promotes motility via G protein-coupled PI3K$\gamma$ , and Cdc42/Racl are essential for ATX-induced tumor cell motility in A2058 melanoma cells. In the present study, we found that activation of p21-activated kinase1 (PAK1) was required for ATX-induced cell motility. (omitted) -
Garlic (Allium sativum) has been used as a general food and a remedy in Oriental for a long time. Since garlic compounds have been also shown to inhibit growth of tumors and to modulate the activity of carcinogenesis, the effects of allicin on growth and survival in human gastric epithelial cells were evaluated by cell viability, cell cycle analysis and DNA fragmentation. Protein levels of cytochrome C, Bcl-xL, Bax and AIF were detected by Western blotting. Effects of recombinant VacA on caspase proteases activity were also determined. (omitted)
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Helenalin, a cell-permeable pseudoguainolide sesquiterpene lactone, is a potent anti-inflammatory agent that inhibits
$NF-{\kappa}B$ DNA binding activity by selectively alkylating the p65 subunit of$NF-{\kappa}B$ . Transcription factors such as$NF-{\kappa}B$ provide powerful target of drugs to use in the treatment of cancer. Human promyelocytic leukemia HL-60 cells are differentiated into monocytic or granulocytic lineage when treated with 1,25-dihydroxyvitamin$D_3{\;}[1,25-(OH)_2D_3]$ or all-trans-retinoic acid (ATRA), respectively. (omitted) -
Here we show that panaxadiol, a ginseng saponin with a dammarane skeleton, induces acute apoptotic cell death in human hepatoma SK-HEP-1 cells as evidenced by analysis of DNA fragmentation, caspase activation, and changes in cell morphology. The kinetic study showed that panaxadiol-induced apoptosis is associated with depolarization of mitochondrial membrane potential and cytochrome c release. Sequential activations of caspases-depolarization of mitochondrial membrane potential and cytochrome c release. Sequential activations of caspases-9, and -3, or -7, but not of caspase 8 coincide well in a time dependent manner with mitochondrial membrane depolarization and cytochrome c release from mitochondria during apoptosis of SK-HEP-1 cells induced by treatment with panaxadiol. (omitted)
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Anticancer drug resistance occasionally occurs in malignant hematologic diseases such as acute myelocytic leukemia (AML) treated with chemotherapy and is a major problem to complete remission. Malignant cells primarily induce intrinsic resistance to treatment of anticancer drug, but gradually obtain acquired resistance to cytotoxic activities of chemotherapy. In this study, we monitored the expression profiles of doxorubicin resistance-related genes in AML-2/DX100, a doxorubicin-resistant human acute myelocytic leukemia cell line. (omitted)
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We show that panaxadiol (PD), a ginseng saponin with a dammarane skeleton, selectively interferes with the cell cycle in human cancer cell lines. PD inhibited DNA synthesis in a dose-dependent manner with
$IC_{50}$ values ranging from 0.8$\mu$ M-1.2$\mu$ M in SK-HEP-1 cells and HeLa cells. PD-treated cells were arrested at G1/S phase, shich coincided well with decreases in Cyclin A-Cdk2 activity, but not in Cyclin E-Cdk2 and Cdc2 activities. The intracellular levels of$p21^{WAF1/CIP1}$ were significantly and selectively elevated in a dose and time-dependent manners in PD-treated HeLa cells. (omitted) -
Ko, Jong-Hee;Yeon, Seung-Woo;Lee, Hong-Sub;Kim, Tae-Yong;Noh, Dong-Youn;Shin, Kyong-Soon;Hong, Soon-Kwang;Kang, Sang-Sun 168.2
Akt/Ptotein Kinase B (PKB) is a serine/threonine kinase and activated by PI3K pathway. Akt/PKB regulates a variety of cellular responses including proliferations, differentiations and insulin signaling pathway. Recent evidence also indicates that the abnormal activities or expression of Akt/PKB is closely associated with cancer, diabetes and neuro-degenerative diseases. These findings mean that Akt/PKB is likely to be a new therapeutic target for the treatment of disease. (omitted) -
The matrix metalloproteases (MMPs) play important roles in invasion, metastasis and angiogenesis in various cell types. Tissue inhibitor of metalloprotease (TIMP)-2, an endogenopus inhibitor of MMP-2, has been shown to inhibit invasion and metastasis. We have previously shown that MMP-2 is responsible for the H-ras-induced invasive and migrative phenotypes in MCF10A human breast epithelial cells. Here, we investigated the effect of TlMP-2 overexpression on invasion and migration in H-ras MCF10A cells. (omitted)
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Hwang, Hyun-Jin;Kim, Jeong-Hee;Park, Joon-Woo;Kim, Sung-Hee;Lee, Min-Jeon;Jeong, Han-Seung;Hwang, In-Hwan 169.1
Recently development of cell-based assay systems which are useful in molecular cell biology and drug discovery attracts significant attention. Here, we introduce a new technologies for monitoring enzyme activity and its inhibition inside living cells. Among various enzymes, proteases are important targets for studying various biological and disease-related processes such as viral infections, apoptosis and Alzheimer's disease. In this study, a sensitive cell-based protease detection system that enables direct fluorescence detection of a target protease and its inhibition inside living cells is introduced. (omitted) -
Lee, Sang-Min;Park, Hye-Ji;Lee, Yoot-Mo;Moon, Dong-Cheul;Kim, Kyong-Soon;Cho, Kyong-Ju;Yoon, Do-Young;Song, Suk-Gil;Hong, Jin-Tae 169.2
Erythropietin (EPO), a hematopoietic factor is also required for normal brain development, and its receptor is localized in brain. Therefore, it is possible that EPO could act as a neurotropic factor inducing differentiation of neurons. The present study, we therefore investigated whether EPO can increase differentiation of undifferentiated cortical neuron isolated from postneonatal (Day 1) rat brains and PC12 cell, undifferentiated dopaminagic cell line. EPO dose (1-100 U/ml) dependently increased cell differentiation and expression of differentiation marker gene (neurofilament and tyrosine hydroxylase) in both cells. (omitted) -
This study was performed to determine the anticarcinogenic activity of the Rhodiola Sachalinesis Extract (RS) on several microorganisms and human cancer cell lines. Among the various solvent fractions of RS, the ethylether partition layer (RSMEE) showed the strongest antimicrobial activity, ethylacetate partition layer (RSMEA) resulted in good antimicrobial activity. We also determined the effect of RS extract and fractions on cytotoxicity, and chemopreventive effect on human cancer cells. (omitted)
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Activation of MKK6 induces invasive and migrative phenotypes in MCF10A human breast epithelial cellsRas expression has been suggested as a marker for tumor aggressiveness of breast cancer, including the degrees of invasion and tumor recurrence. We previously showed that p38 MAPK is a key signaling molecule differentially regulated by H-ras and N-ras, leading to H-ras-specific cell invasive and migrative phenotypes in human breast epithelial cells (Cancer Res: 63, 5454-5461, 2003). In this study, we further investigated the role of p38 MARK pathway in the induction of metastatic potential in MCF10A cells as a "gain of function" study. (omitted)
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Lee, Yun-Jeong;Kim, Na-Young;Kim, Hyung-Jin;Park, Jung-Ho;Kim, Jung-Kwon;Hee, Chang-Kern;Kim, Jung-Hoe;Kim, Hong-Jin 170.3
An efficient Erythropoietin (EPO)-expression system in mammalian cells is required for massive production for therapeutic use. Ammonium ion is a major problem in the production of valuable recombinant proteins in cultured animal cells. Therefore, it is of importance to devise a system by which a high productivity of human therapeutic recombinant protein can be maintained or enhanced under low ammonium concentration. To reduce the ammonium ion accumulated in EPO producing Chinese Hamster Ovary (CHO) ceels, IBE, we introduced the first two genes of the urea cycle, carbamoyl phosphate synthetase (CPSI) and arnithine transcarbamoylase (OTC), into IBE using a stable transfection method. (omitted) -
·The potent antitumor activities of 3-arylisoquinolines promoted us to explore the structure-activity relationship of these compounds. A series of 3-arylisoquinoline derivatives were evaluated for antitumor cytotoxicity against human lung tumor cell (A 549). For the next stage, we decided to prepare the constrained form of 3-arylisoquinolines as indeno[1,2-c]isoquinolines. As a result, diverse spectrum against human tumor cell lines was obtained. In order to study structure-activity relationship (SAT) of these compounds the comparative molecular field analysis (CoMFA) was carried out. (omitted)
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Over the past few years, a variety of macrocyclic salicylate natural products have been isolated from both terrestrial and marine sources based on their ability to induce a particular phenotype in mammalian cells. Extracts of the myxobacterium Chondromyces showed high cytotoxicity against cultivated mammalian cells and bio-guided fractionation revealed the cytotoxicity was due to one main metabolite identified as the novel macrolide apicularen A. Beginning to understand the molecular basis for these distinct activities will require structure-function correlation studies and the development of synthetic chemistry in this area. (omitted)
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Park, Jae-Gyu;Kim, Dong-Hyun;Rahaman-A.F.M.Motiur;Chang, Hyeun-Wook;Lee, Eung-Seok;Jahng, Yurng-Dong 172.1
Luotonin A was isolated from Peganum nigellastrum Bunge (Zygophyllaceae) which was named Luo-Tuo-Hao in China and used as a Chinese traditional medicine for the treatment of rheumatism, abscess, and inflammation. The basic fractions of P. nigellastrum showed antitumor activtity, and the origin of such an activity was recently revealed by identifying its constituent luotonin A which inhibited the growth of leukemia P-388 cells ($IC_50$ = 1.8$\mu$ g/mL). Such an intriguing properties of luotonin A led developments of efficient methods for total synthesis. (omitted) -
3-Alkoxy-6-allylthiopyridazine derivatives showed the strongest protective effect against oxidative stress and their anticancer effect determined on the growth of SK-Hep-l hepatocellular carcinomar cells. The allythio group as a pharmacologically active group was introduced into pyridazine nucleus and a substituent such as halogen or alkoxy was also introduced into paraposition of allylthio group. Five kinds of 3-alkoxy-6-allylthiopyridazine derivatives were synthesized and their chemoprotective activities examined in rats exposed to aflatoxin
$B_1$ -toxicant. (omitted) -
One of attractive target for Rheumatoid Arthritis (RA) therapy is the cytokine, tumor necrosis factor-alpha (TNF-
$\alpha$ ), which has been shown to be overproduced in the joint of RA patients. The clinical success of anti- TNFR biologics has validated TNF-$\alpha$ as a drug discovery target. Thus, inhibiting of formation of TNF-$\alpha$ has been emerged to an intriguing approach for RA therapy. TNF-$\alpha$ is processed from its membrane bound precursor by the metalloprotease TNF-$\alpha$ converting enzyme (TACE), Here, biological evaluation, mode of action of natural TACE inhibitor, Gelastatin hydroxamate, are addressed. (omitted) -
Park, Hyeung-Geun;Choi, Je-Yeon;Choi, Sea-Hoon;Park, Mi-Kyung;Lee, Ji-Hye;Suh, Young-Ger;Cho, Ha-Won;Oh, Uh-Taek;Lee, Ji-Youn;Kang, Sang-Uk;Lee, Jee-Woo;Kim, Hee-Doo;Park, Young-Ho;Jeong, Yeon-Su;Choi, Jin-Kyu;Jew, Sang-Sup 173.2
Vanilloid receptor I (VR1) is a nonselective cation ion channel placed in the plasma membrane of peripheral sensory neurons that is potential target for analgesia A series of N-4-substituted-benzyl-N'-tert-butylbenzyl thioureas were prepared for the study of their agonistic/antagonistic activities to the vanilloid receptor in rat DRG. Their structure-activity relationship in reveals that not only the two oxygens and amide hydrogen of sulfonamido group but also the optimal size of methyl in methanesulfonamido group play an integral role for the antagonistic activity on vanilloid receptor. -
In recent years, olefin cross-metathesis (CM) has emerged as a powerful and convenient synthetic technique in organic chemistry; however, as a general synthetic method, CM has been limited by the lack of predictability in product selectivity and stereoselectivity. A number of excellent studies have recently appeared in the literature which have shown that with the correct catalyst and reaction conditions CM can be used to access a variety of di-and trisubstituted olefinic products in moderate to high yield with good E/Z ratios. (omitted)
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We have previously reported the synthesis and cytotoxic activities of a series of azaanthraquinone derivatives using doxorubicin as a lead compound. Doxorubicin is known to intercalate into DNA and to inhibit topoisomerase II activity. But in the case of quinone compounds like Dox, its use is limited because of systemic toxicities, primarily cardiotoxicity and myelosuppression. In this study, we discuss the synthesis of isoindolobenzoquinoxaline derivatives. The quinone group of the azaanthraquinone derivatives were removed in the target compounds. (omitted)
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Quorum sensing, a gene expression in response to population density, is regulated by chemical signals, most of which are acylated homoserine lactones (AHLs). The AHL derivatives have been reported to regulate bioluminescence, virulence factors and / or swarming motility in bacteria. It is hypothesized that higher organisms may have evolved specific means to interfere with bacterial communication as exemplified in the AHL-antagonistic activity of halogenated furanones isolated from the Australian macroalga Delisea pulchra. (omitted)
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Moon, Yoon-Soo;Kim, Eun-Kyung;Basnet, Arjun;Zhao, Long-Xuan;Kim, Dae-Ok;Kim, Nam-Hee;Chae, Whi-Gun;Jeong, Tae-Cheon;Lee, Eung-Seok 174.3
1-and 2-Bromopropane were reported as the causative agents for reproductive toxicity and immunotoxicity. The glutathione (GSH) metabolites resulting from in vitro treatment of 1- and 2-bromopropane were detected, identified and characterized. For the facile identification, expected GSH metabolites rormed by 1- and 2-bromopropane were chemically synthesized as reference materials (positive controls) and characterized by$^1H$ -NMR,$^13C$ -NMR, HPLC and LC/MS/MS. The treatment of GSH and S-9 fraction with 1- or 2-bromopropane at a physiological condition (pH 7.4,$37^\times$ ) for 1hr produced GSH metabolites, which were identified by UV, HPLC and ESI LC/MS/MS analyses. (omitted) -
Galactosyl ceramides paly important roles in biological system as immunomodulator and essential constituents of membranes and cell walls. An efficient synthesis of
$\alpha$ -galactosyl ceramide, KRN 7000, derived from marine sponge Agelas mauritianus as accomplished via a short reaction involving the coupling ceramide moiety and trichloroacetimidate as glycosylation donor. We could synthesize$\alpha$ -galactosyl ceramide stereoselectivity without$\beta$ -anomer formation on a multigram scale. -
Inhibition of the protein-modifying enzyme farnesyltransferase is considered as a major emerging strategy in cancer therapy because of the involvement of farnesylated proteins in oncogensis. We studied the structure-activity relationship of a novel class of CAAX-peptidomimetic farnesyltransferase inhibitors based on the benzophenone scaffold. FlexX docking of inhibitors confirmed reasonable fit of the molecule into the peptide binding site of farnesyltransferase. We also performed a virtual screening with LeadQuest chemical library databases to idenfity novel inhibitors of farnesyltransferase. (omitted)
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2-Phenyl-1, 8-naphthyridin-4-ones had been synthesized for their cytotoxic activity. Substituted acetophenone was treated with NaH and diethyl carbonate to give ethyl benzoylacetates, which was reacted with substituted 2-aminopyridine and PPA to yield 2-phenylpyridopyrimidine-4-ones. These compounds was heated at
$350^\times$C in liquid paraffin to afford final compounds, 2-phenyl-1 , 8-naphthyridin-4-ones. -
Our long-term research goals involve the SARs study and the synthetic procedure development of wogonin and its analogs. We investigated efficient synthetic pathways of wogonin and its bioisosteres in a large quantity to decipher the structural requirements for anti-inflammatory activities. We plan to serially delete or modify the 5,7-dihydroxyl groups of wogonin to observe the effects of the hydroxyl groups on anti-inflammatory activity. Also we modofied the 8- methoxy group on a ring since it is known to be necessary for biological activity. (omitted)
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Bradykinin is an autocoid related to acute and chronic pain and inflammation. The non-peptide bradykinin antagonists are of interest as novel anti-inflammatory therapeutics. To understand the structural basis for the bradykinin antagonistic activity and to guide the design of more potent compounds we analysed the three dimensional pharmacophore model. Seven active compounds very recently reported such as FR 167344, FR 173657, LF 160687, and bradyzide were used as our pharmacophore model analysis. (omitted)
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Transcription factors (TF) can bind tightly to specific DNA lesions formed by some anticancer agents. The formation these TF:(drug-modified DNA) complex may disrupt expression of genes critical for cell survival, and it was proved to be one of biochemical mechanisms of anticancer activity. Based on this model, we have designed programmable DNA Alkylating agents that can also attract TF, especially nuclear receptors. As a model compound, we designed drug molecules, RA-mustard and Am580-mustard, that enable to bind both retinoic acid receptor (RAR) and DNA by using molecular modeling techniques, and synthesized them by connecting chlorambucil and ligand for RAR with a linker unit. (omitted)
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Kim, Eun-Young;Lee, Eun-Jung;Lee, Min-Hee;Min, Hye-Young;Huh, Sun-Kyung;Lee, Sang-Kook;Kim, Sang-Hee 177.1
Styrylheterocycles were synthesized as a novel calss of inhibitors on nitric oxide(NO) production. Their inhibitory activities were evaluated using lipopolysaccharid-stimulated RAW264.7 macrophage cells. This series of inhibitors are suggested as lead comounds for the development of potent and selective inhibitors -
Thiazolidinediones (TZDs) are a new class of compound that increase insulin sensitivity in type 2 diabetic patients. Thiazolidinediones (TZDs) act as ligands for a member of the nuclear hormone receptor superfamily, peroxisome proliferator-activated receptor-
$\gamma$ (PPAR-$\gamma$ ), which is highly expressed in fatty tissue and, moreover, has been shown to play an important role in fat cell differentiation. The strong interaction between the antidiabetic activity ofTZDs and their ability to activate PPAR-$\gamma$ suggests that PPAR-$\gamma$ , through downstream-regulated genes, mediates the effects of TZDs. (omitted) -
Corticosteroids have been used most frequently for inflammatory bowel disease. To reduce side effects by the systemic absorption, colon-specific delivery is highly desirable. We expected that conversion of 21-hydroxyl in glucocorticoids into a sulfate ester sodium will greatly increase the hydrophilicity, which consequently restrict the gastrointestinal absorption. Once delivered to the colon, sulfate ester will be hydrolyzed by the sulfatase originated from microbes and release the parent compound, glucocorticoids. In this study, we prepared methylprednisolone 21-sulfate sodium (MPS) and investigated its suitability as a colon-specific prodrug on methylprednisolone (MP). (omitted)
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6-Arylthio-/6-arylamino-4,7-dioxobenzothiazoles were synthesized and tested for in vitro antifungal activity against Candida species and Aspergillus niger. 6-Arylamino-4,7-dioxobenzothiazoles showed, in general, more potent antifungal activity than 6-arylthio-4,7-dioxobenzothiazoles. The 6-arylamino-substituted compounds exhibited the greatest activity. In contrast, 6-arylthio-, 2-/5-methyl-or 5-methoxy-moieties of compounds did not improve their antifungal activity significantly. The results of this study suggest that 6-arylamino-4,7-dioxobenzothiazoles would be potent antifungal agents
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Naturally occurring sugar mimics with a nitrogen in the ring are classified into five structural classes: polyhydroxylated pyrrolidines, piperidines, indolizidines. pyrrolizidine, and nortropanes. Glycosidase are involved in a wide range of important biological processes, such as intestinal digestion, post-translational processing of glycoproteins and the lysosomal catabolism of glycoconjugate. The realization that alkaloidal sugar mimics might have enormous therapeutic potential in many diseases such as viral infection, cancer and diabetes has led to increasing interest and demand for these compounds. (omitted)
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P2X receptors are ligand gated cation channels activated by the binding of extracellular adenosine 5'-triphosphate (ATP) and classified into 7 subtype families.
$P2X_1$ receptors are abundantly expressed in smooth muscle mediates blood vessel and mediate constriction upon binding of neuronal ATP. The activation of$P2X_3$ receptor by ATP has been known to initiate the pain signaling in the peripheral nervous system, which is involved in chronic inflammatory nociception and neuropathic pain by nerve injury. (omitted) -
Chiral building blocks have the importance in the pharmaceutical and agrochemical industries as well as in the development of rapid and efficient syntheses of bioactive compounds and natural product. Vinylstannane contains two synthetically useful functional groups (vinylstannane and allylic alcohol). The vinylstannane functional group can be used in C-C bond formation under a variety of conditions and the allylic alcohol functional can be used in hydroxyl-directed epoxidations, cyclopropanations, and sigmatropic rearrangements. (omitted)
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We have developed the novel one-pot synthetic method for regioselective and stereoselective N-protected amines through the reaction of various ethers with chlorosulfonyl isocyanate (CSI). Also, we found a novel technique to compare directly the stability of carbocations in the solution phase and established the stability order of the various carbocations. And we reported the cleavage of benzyl and p-methoxybenzyl protecting groups of alcohols and phenols in the presence of other functional groups using CSI. (omitted)
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Natural histrionicotoxin, a substance isolated from the skins of the "arrow poison frog" and its fully hydrogenated derivative, perhydrohistrionicotoxin (pHTX), have been the subject of synthetic investigation because of their important neurophysiological activity and a unique framework. In this work, we could obtained the appropriately functionalized spiropiperidine compound as a formal precursor of perhydrohistrionicotoxin. An important feature of this synthesis is the creation of a stereogenic center by using Ireland-Claisen Rearrangement, and Ring-Closing Metathesis (RCM).sis (RCM).
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Eukaryotic DNA topoisomerase I (top I) is an essential enzyme that act to relax supercoiled DNA during the transcription, replication and mitosis. Intracellular levels of top I are elevated in a number of human solid tumors, relative to the respective normal tissues, suggesting that controlling the topI level is important to treat cancer. Top I poisons show their antitumor activities by stabilizing the cleavable ternary complex consisting of top I enzyme, DNA, and drug. Thus, top I is a promising target for the development of new cancer chemotherapeutics against a number of solid tumors. (omitted)
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Cathepsin K, a cysteine protease of the papain superfamily, is predominantly expressed in osteoclasts and has been postulated as a target for the treatment of osteoporosis. Crystallographic and structure-activity studies on a series of azepanone-based diamino and acyclic ketone derivative inhibitors of cathepsin K have led to the design and identification. X-ray structure of the cysteine protease cathepsin K (1NL6) co-crystalized with an inhibitor with 2.8
${\AA}$ resolution was used to predict the protein-ligand interactions and to estimate the binding affinity from the docking score by FlexX module. (omitted) -
This study was carried out to examine stability of biological products(BCG vaccine), freeze-dried BCG vaccine for percutaneous use and for interdermal use.1. pH tests of freeze-dried BCG vaccine for percutaneous use and for interdermal use vaccine was suited to basic range with variable temperature. freeze-dried BCG vaccine for percutaneous use was resulted with 6.2-6.7 and for interdermal use was resulted with 6.2-6.7.2. Bacterial concentration test of freeze-dried BCG vaccine for percutaneous use and for interdermal use vaccine was suited to basic range with variable temperature. (omitted)
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2-Aminoindan derivatives has been shown the serotonergic activities. In order to find new serotonergic agent, we trid to enlarge the indan ring. 3, 4-Dimethoxybenzaldehyde, used as starting material was condensed with malonic acid, piperidine to form 3, 4-dimethoxycinnamic acid. It was catalytically hydrogenated and sudsequently cyclized by Friedel-Crafts acylation reaction to yield 5, 6-dimethoxyindanone. This compound was reacted with pyrrolidine and then acrylamide to be synthesized the 3-membered ring. (omitted)
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Inosine monophosphate dehydrogenase(IMPDH) catalyzes the
$NAD^+$ -dependent oxidation of IMP to XMP, the rate limiting step in the de novo biosynthesis of guanine nucleotide. Its critical role at the metabolic branch point in purine nucleotide biosynthesis makes it a useful target in the development of drugs for antiviral and anticancer chemotherapy and in immunosupressant area. Several compound with antiviral activity have been found to be inhibitors of IMPDH. For example, ribavirin, a competitive inhibitor of IMPDH, has broad spectrum antiviral activities against DNA and RNA viruses. (omitted) -
Comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) were performed on 60 PPAR-g agonists. Partial Least Squars (PLS) analysis produced good predicted models with
$q^2$ value of 0.62 (SDEP=0.33, F value=93.22,$r^2$ =0.92) and 0.56 (SDEP=0.47 F value=27.65,$r^2$ =0.86), respectivly. The key spatial properties were detected by careful analysis of the isocontour maps. -
Jew, Sang-Sup;Park, Boon-Saeng;Lim, Doo-Yeon;Kim, Myoung-Goo;Chung, In-Kwon;Kim, Joo-Hee;Hong, Chung-Il;Kim, Joon-Kyum;Park, Hong-Jun;Lee, Jun-Hee;Park, Hong-Jun;Lee, Jun-Hee;Park, Hyeung-Geun 181.4
Telomeres are DNA-protein complexes at the ends of chromosomes, which play an essential protective role against DNA degradation and aberrant recombination during cell divisions. Several telomerase inhibitors have been reported as candidates for new antitumor drugs. Among them, 2-thiobenzylpyridines, developed by Geron. Co Ltd. as a telomerase inhibitor, were chosen as lead compounds. Twenty-one pyridine-2- carboxylate derivatives were prepared by the coupling of 6-formyl-2-carboxylic acid with the corresponding phenol, thiophenol, and aniline, substituted with various functional groups. (omitted) -
Flavonoids with oxygen atoms are known to have potent biological effect.They have been studied long as major antioxidants which protect cell membranes. Recent medical surveys show that increased intake of selenium decreases the risk of breast, colon, lung and prostrate cancer by preventing free radical generation. The flavonoids, isoflavonoids, and coumarins which form the bulk of these compounds are very polar and have limited use as drugs which have to pass through BBB(Brain Blood Barrier)The non-polar property is increased by exchange oxygen to selenium as a part of heterocyclic compound. (omitted)
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Ryu, Chung-Kyu;Chae, Mi-Jin;Han, Ja-Young;Jung, Ok-Jai;Hong, Sung-Yu;Chung, Kwang-Hoe;Choi, Ik-Hwa 182.2
The abnormal proliferation and migration of vascular smooth muscle cell (SMC) play an important role in the pathology of coronary artery atherosclerosis and restenosis. Platelet-derived growth factor (PDGF) is one of the most potent promoters of the proliferation and migration of the SMC. The heterocyclic quinones represent an important class of biologically active molecules. However, the inhibitory activity of quinone classes on the proliferation of the SMC has not been reported. (omitted) -
(-)-Antofine is phenanthroindolizidine alkaloid being isolated from Cynanchum vincetoxicum. It has powerful cytotoxicity toward drug-sensitive KB-3-1 and multidrug resistant KB-V1 cancer cell line. We have successfully accomplished stereoselective total synthesis by using palladium catalyzed Stille coupling of l0-bromomethyl-2,3 ,6-trimethoxy-phenanthrene and (R)-(E)-4-(tributylstannanyl)but-3-en-2-o1, Overmann rearrangement of imidate, and RCM(ring-closing metathesis) for construction of pyrrolidine.
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The synthesis of various cyclic carbamate compounds and amino alcohols has attracted attention in the past because of their potential as antibiotics, antitumor, analgenics, anticonvulsants. Several methods for the preparation of cyclic carbamate compounds have previously been reported including the use of heterocumulenes. We have recently described the novel synthetic method for N-protected amines from various ethers using Chlorosulfonyl isocyanate(CSI) and found that the mechanism of our CSI reaction is a competitive reaction of
$S_N1$ and $S_ Ni$ mechanisms according to the stability of carbocation intermediates. (omitted) -
We report the synthesis of 3,4-dihydro-2-oxo-4-quinolines 5a-e for the development novel flavonoid derivatives with potential antiinflammatory activity and propose a mechanism of the one-pot reaction. The various amines (la-e) for this work were commercially available. We isolated that ester (2a-e) were formed by nucleophilic attraction using ethyl benzoylacetate. The C-N bond formation proceeded at refluxing in toluene with catalytic amount of p-toluenesulfonic acid and a removal of water and ethanol was important in this reaction. (omitted)
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Phenanthroindolizidine alkaloid, (-)-antofine has attracted attention because of its extremely potent inhibition of cancer cell growth (Its
$IC_50$ values have the low nanomolar range). The frist asymmetric total synthesis of (-)-antofine is described. An important feature of this synthesis is the creation of a stereogenic center by enantioselective alkylation using the phase transfer catalyst (PTC) and ring-closing metathesis (RCM) for pyrrolidine ring construction. This synthesis is efficient to allow the asymmetric preparation of other naturally occurring phenanthroindolizidine and phenanthroquinolizidine alkaloid. -
HDAC and HAT (histone acetyltransferase) are involved in co-regulation in chromatin remodeling and the functional regulation of gene transcription. Abnormal recruitment of HDAC is related to carcinogenesis. Thus, the identification of potent histone deacetylase (HDAC) inhibitor has been considered as very intriguing approach for development for cancer chemotherapy. More recently, anti-inflammatory activity of SAHA cytokines was reported via reduction of proinflammatory cytokinres in vitro and in vivo. (omitted)
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Many naturally occurring polyhydroxylated sterols and oxysterols exhibit potent biologic activities. The role of oxycholesterol including 2, 5(R)-2, 6-hydroxycholesterol is a potent inhibitor of cholesterol biosynthesis in vitro as it is an effective inhibitor of HMG-Coa reductase. Some new polyhydroxylated sterols were showed potent cytotoxicity to cancer cells. And it has also been chown to be an inhibitor of DNA synthesis, In order to synthesize the various oxy derivatives, we tried to positionselective and reagentselective epoxidation and reduction of cholesterol derivatives. (omitted)
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Inosine 5'-monophosphate dehydrogenase (IMPDH) is a critical enzyme in the regulation of cell proliferation and differentiation. This enzyme catalyzes the
$NAD^+$ -dependent oxidation of IMP to XMP, the rate limiting step in de novo biosynthesis of guanine nucleotides. Therefore, the biochemical effect of IMPDH inhibition in sensitive cell types is decrease in intracellular guanine nucleotide levels, and the decrease in cellular GTP and deoxy GTP pool levels blocks DNA and RNA synthesis in rapidly proliferating tumor cells. (omitted) -
The 20 alkylsulfonylamido propanol derivatives had been investigated for their cytotoxic activity against HT-29 colon cancer, Caki-2 renal cancer, A549 lung cancer, PC-3 prostate cancer, HL-60 leukemia cell using MTT assay. Cytotoxic activity was strongly influenced by the substituted alkyl chain length and the optimal alkyl chain length for cytotoxicity was C11. Some of alkylsulfonylamido porpanol derivatives showed stronger activity than reference compound, B13.
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Kim, Jong-Hoon;Park, Hyun-Jung;Noh, Ji-Young;Ryu, Hyung-Chul;Park, Sang-Wook;Ko, Dong-Hyun;Chae, Myeong-Yun;Cho, Il-Hwan 185.2
The typical approach of virtual screening is to prepare a 3D database and dock each member to the receptor, and carry out a post-analysis to make a final selection of compounds to be tested. The biological test of these compounds leads to 'hit'. The size of the 3D database is rate-determining factor because the docking process is still time-consuming method. The number of compounds for biological testing is cost-determining factor because the materials used in the test are cost-consuming. The use of the representative subsets derived from the entire database help reduce runtime of docking procedure. (omitted) -
Juglone and naphthazarine derivatives were newly systhesized for the evaluation of antifungal activities. These derivatives were prepared by methylation of juglone and 2, 3-dichloro-5, 8-dihydroxy-l, 4-naphthoquinone, and by regioselective nucleophilic subsitution with arylthiols. All compounds were tested in vitro for their growth inhibitory activities against pathogenic fungi by the standard method. The MIC values were determined by comparison to flucytosine as a standard agent. (omitted)
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Bradykinin is an autocoid related to acute and chronic pain and inflammation. The non-peptide bradykinin antagonists are of interest as novel anti-inflammatory therapeutics. Some active compounds such as FR 173657, LF 160687, and bradyzide were reported very recently. In our search for the new bradykinin antagonists, we designed and synthesized the iminodiacetic acid derivatives having two or three amide bonds and lipophilic ring system in each molecule. Liquid phase combinatorial synthesis using the iminodiacetic acid template gave diverse individual compounds rapidly and efficiently on a 10-50 mg scale. (omitted)
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PPARs (peroxisome proliferator activated receptors) are member of nuclear hormone receptors superfamily. Activations of PPARs upon binding with ligands modulate glucose metabolite, differentiation of adipocyte, inflammation response, and so on. Thiazolidinedione analog is one of the potential antidiabetic drug that binds and activates PPAR selectively and enhances insulin sensitivity. In an effort to develop novel and effective antidiabetic thiazolidindione analogs, we have synthesized tetrahydroquinoline and para-substituted benzene-linked thiazolidinedione analogs by coupling reaction of the hydrophobic segments with hydroxybenzylthiazolidinedione.
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The three-dimensional quantitative structure-activity relationship (3D-QSAR) study using the comparative molecular field analysis (CoMFA) was performed on indolinones derivatives as an inhibitor of the protein tyrosine kinase of fibroblast growth factor receptor (FGFR). In the training set, twenty-four indolinone derivatives were aligned based on the indole fragment and the steric and electrostatic fields were included in the analysis. The best predicted model showed the cross-validated coefficient (r
$^2$ $\sub$ cv/) of 0.804 and bib-cross validated coefficient (r$^2$ ) of 0.942. The CoMFA study can be used to predict several new inhibitors of the FGFR. -
Acanthoside-D, one of major components of Acanthopanacis Cortex, is known as a ginseng-like substance. it has been known to possess diverse biological effects. Acanthoside-D has a furofuran lignan structure and the synthesis of which poses interesting and often unsolved proplems of stereocontrol. Although a few interesting syntheses providing this natural product have been reported, an intermolecular McMurry coupling - intramolecular Mitsunobu cyclization route has not yet been explored. We report here a short and efficient synthetic pathway to the total synthesis of Acanthoside-D from aryl aldehydes and methyl acrylates via Baylis-Hillman reaction, intermolecular McMurry coupling and intramolecular Mitsunobu cyclization as key reaction.
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Kim, Bok-Young;Ahn, Joong-Bok;Lee, Hong-Woo;Kim, Joon-Kyum;Shin, Jae-Soo;Kang, Sung-Kwon;Lee, Jung-Hwa;Ahn, Soon-Kil;Lee, Sang-Jun;Hong, Chung-Il;Yoon, Seung-Soo 187.1
Type 2 diabetes is characterized by high level of blood glucose and insulin and impaired action. In recent years, the treatment of type 2 diabetes has been revolutionized with the advent of thiazolidinedione (TZD) class of molecules that ameliorate insulin resistance and thereby normalize elevated blood glucose levels. These TZDs are synthetic, high-affinity ligands of peroxisome proliferator activated receptor-gamma (PPAR${\gamma}$ ); a member of the nuclear receptor family that controls the expression of genes in the target tissues of insulin action. (omitted) -
The cyclin-dependent kinases (CDKs), a group of serine/threonine kinases that form active heterodimeric complexes binding to cyclins, are key regulators of the cell cycle. The role of cyclin dependent kinases(CDKs) in cell cycle regulation has stimulated an interest in them as potential targets for proliferative diseases such as cancer, psoriasis, and chemotherapeutic agent-induced alopecia. Indirubin, an active ingredient of a traditional Chinese recipe Danggui Longhui Wan, are potent CDK inhibitors competing with ATP for binding to the catalytic site of the CDKs. (omitted)
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Structure-activity relationship studies of allylamine type of antimycotics were carried out to evaluate the effect of naphthyl and methyl portion of naftifine. Compounds with 4-fluorphenyl, 2-fluorophenyl, 2,4-dichlorophenyl, 2,6-dichlorophenyl, 4-nitrophenyl, and 2,3-dihydro-benzo[l,4]dioxin-6-yl instead of naphthyl group with hydrogen, methyl, and ethyl in the place of methyl in naftifine were synthesized and tested their in vitro anti-fungal activity against five different fungi. Eight compounds showed significant antifungal activity against T. mentagrophytes. (omitted)
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kim, hyung-Kyo;Jin, Cheng-Hua;Han, Jeong-Whan;Lee, Hyang-Woo;Lee, Yin-Won;Zee, Ok-Pyo;Jung, Young-Hoon 188.1
The antiparasitic agent apicidin, which was recently isolated from cultures of Fusarium Pallidoroseum, belongs to a rare group of cyclictetrapeptide fungal metabolites. Apicidin inhibits protozoal HDAC and is orally active against Plasmodium berghei malaria in mice. The biological activity of apicidin appears to be attributable to inhibition of apicomplexan HDAC at low nanomolar concentrations. In the present, we have worked about the synthesis of new apicidin derivatives and discovered that apicidin and some derivatives have mild antitumor activity. (omiited) -
Large-conductance
$Ca^{2+}$ activated potassium channels$(BK_{ca})$ are widely distributed and play key roles in various cell functions. In nerve cells, B$K_{ca}$ channels shorten the duration of action potentials and block$Ca^{2+}$ entry thereby repolarizing excitable cells after excitation.$(BK_{ca})$ channel opening has been postulated to confer neuroprotection during stroke and has attracted attention as a means for therapeutic intervention in asthma, hypertension, convulsion, and traumatic brain injury. (omitted) -
Park, Hae-Sun;Kim, Nan-Young;Choi, Hee-Jeon;Park, Eun-Hee;park, Myung-Sook;Lee, Myung-Sook;Shin, Hea-Soon;Kwon, Soon-Kyoung 188.3
Nonsteriodal antiinflammatory drugs(NSAIDs) are widely used to treat pain, fever, and inflammatory conditions including osteoarthritis. But chronic patients suffer from gastrointestinal disturbances such as discomfort, nausea, peptic ulcer and severe bleeding because NSAIDs inhibit not only COX-2 associated with anti-inflammatory activity, but also COX-l accompanied with side effects in the stomach and kidney. Therefore, in this study, we designed a new 2-thiohydantoin derivatives as selective COX-2 inhibitors is that the 5-membered heterocycle ring is substituted with two aryl groups. (omitted) -
Jung, Kwan-Young;Kim, Soo-Kyung;Gao, Zhan-Guo;Gross-Ariel-S.;Melman-Neli;Jacobson-Kenneth-A.;Kim, Yong-Chul 189.1
4-(4-Methoxyphenyl)-2-aminothiazole and 3-(4-methoxyphenyl)-5-aminothiadiazole derivatives have been synthesized and evaluated as selective antagonists for human adenosine A$_3$ receptors. A methoxy group in the 4-position of the phenyl ring and N-acetyl or propionyl substitutions of the aminothiazole and aminothiadiazole templates displayed great increases of binding affinity and selectivity for human adenosine A$_3$ receptors. The most potent A$_3$ antagonist of the present series, N-[3-(4-methoxy-phenyl)-[1,2,4]thiadiazol-5-yl]-acetamide exhibiting a K$\_$ i/ value of 0.79 nM at human adenosine A$_3$ receptors, showed antagonistic property in functional assay of cAMP biosynthesis involved in one of the signal transduction pathways of adenosine A$_3$ receptors. (omitted) -
Seeds of Euryale ferox have been used for disorder of kidney, hysterorrhea of female and a tonic. In this study, in order to investigate the efficacy of antioxidant activity, the bio-activity guided fraction and isolation of physiologically active substance were performed. Roots, stems, flowers(seeds) were extracted with MeOH and each fractions were examined antioxidant activity by DPPH method. It was revealed that flowers(seeds) fration has significantly antioxidant activity. From flowers(seeds) frction, H
$_2$ O, 30%, 60%, 100% MeOH and acetone fractions were examined antioxidant activity by DPPH method. (omitted) -
Choi, Yeon-Hee;Seo, Jee-Hee;Kim, Jung-Sook;Kim, Seong-Kie;Choi, Sang-Un;Kim, Young-Sup;Kim, Young-Kyoon;Ryu, Shi-Yong 190.1
A bioassay-guided fractionation of the stem bark extract of Eucommia ulmoides Oliver (Eucommiaceae) led to the isolation of three iridoid constituents, genipin (1), geniposide (3), geniposidic acid (4) as well as (${\pm}$ )-guaiacylglycerol (2) and fatty acid mixtures as active ingredients of the extract responsible for the antitumoral property. The EtOAc soluble part and BuOH soluble part of the extract demonstrated a significant inhibition on the proliferation of cultured human tumor cells such as A549 (non small cell lung), SK-OV-3 (ovary), SK-MEL-2 (melanoma), XF498 (central nerve system) and HCT-15 (colon) in vitro, whereas the remaining water soluble part exhibited a poor inhibition. (omitted) -
In the course of search for various bioactive compounds from marine algae, we found strong antioxidant activity of the methanolic extract of the brown alga G. elliptica. Chromatographic purification [ODS flash, gel-filtration on Sephadex LH-20, HPLC] of the BuOH layer of the methanolic extract afforded two known polyphenolic compounds, 6,6'-bieckol (1) and dieckol (2). Compound 1 showed acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities, free radical scavenging activity on DPPH (1,1-diphenyl-2-picryl-hydazyl) with IC
$\_$ 50/ values of 91.2, 45.6 and 15.5$\mu\textrm{g}$ /$m\ell$ , respectively. (omitted) -
Three new butenolides (1-3), and a new cyclopentenone derivative (4) were isolated from a marine sponge Homaxinella sp. by bioactivity guided fractionation. The gross structures were established on the basis of NMR and MS analyses. The stereochemistry of the butenolides and cyclopentenone derivative was defined on the basis of optical rotation and CD spectroscopy. The compounds were tested against a panel of five human solid tumor cell lines and displayed marginal to significant cytotoxicity.
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This study was carried out to examine the constituents of Amorpha fruticosa (Leguminosae), a shrub originated from North Africa. Dried and ground fruit of A. fruticosa were extracted with methanol and then concentrated to give the crude extracts. The crude extracts was successively fractioned with organic sovents, such as n-hexane, CH
$_2$ Cl$_2$ and EtOAc. Seven compounds were isolated from the fruits of A. fruticosa. On the basis of spectrosopic data, the structures of these compounds were determined as: kaempferol 7-O-${\alpha}$ -L-rhamnopyranoside (I), methyl 3,4,5- trihydroxybenzoate (methyl gallate, II), tephrosin (III), dalbinol (IV), gallic acid (V), 2",4",5",7-tetramethoxyisofavone (Ⅵ) and Dalbinol 2"-O-${\beta}$ -D-Glucopyranoside (Ⅶ) respectively. (omitted) -
Son , Dong-Wook;Ryu , Ji-Young;Kang , Jun-Gil;Lee, Sang-Yun;Kim, Hyun-Su;Lee, Sang-Hyun;Hoon, Jung-Sang;Lee, Yeon-Sil;Shin, Kuk-Hyun 191.1
The anti-oxidant activities of Acanthopanax senticosus stems were investigated. The n-BuOH fraction of A. senticosus stems exhibited a significant decrease in serum transaminase activities elevated by hepatic damage induced by CCl$_4$ -intoxication in rats. The n-BuOH fraction inhibited the sGPT activities by 65.79%. The n-BuOH fraction showed the increase in the anti-oxidant enzymes such as hepatic cytoso1ic superoxide dismutase, catalase and glutathione peroxidase activities by 30.31, 19.82 and 155%, respectively, in CCl$_4$ -intoxicated rats. These results suggest that the stems of A. senticosus possess not only the hepatoprotective, but also the anti-oxidant activities in rats. -
Phyllanthus ussuriensis Rupr. et Maxim. (Euphorbiaceae) has long been used in folk medicine to treat kidney and urinary bladder disturbances, intestinal infections, diabetes, and hepatitis. Reported chemical constituents of this species are one flavonoid (rutin), two gallotannins (gallic acid, methyl gallate) and two ellagitannins.An investigation of the n-BuOH fraction of P. ussuriensis led to the isolation of two new megastigmane glycosides, 10-hydroxy-4,7-megastigmadiene-3-one-9-O-b-D-glucopyranoside (1), 10- hydroxy-4,6-megastigmadiene-3-one-9-O-b-D-glucopyranoside (2) and two known compounds roseoside (3) and 3-oxo-a-ionol-9-O-b-D-glucopyranoside (4). (omitted)
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Alnus japonica (Betulaceae) has been traditionally used for purifying blood, and curing feces containing blood, enteritis, diarrhea, alcoholism and cut wounds. In the current work, activity guided isolation of the butanol fraction of the Alnus japonica bark led to the isolation of catechin-7-O-
${\beta}$ -D-apiofuranoside. Anti-inflammatory activity was determined with carrageenan-induced paw edema in mice as an acute inflammation, complete Freund's adjuvant-induced arthritis as a chronic inflammation. Carrageenan- induced paw edema in mice was significantly inhibited at 0.5, 1, 2, and 3 hr after carrageenan injection by administration of the flavonoid glycoside at the dose of 150mg/kg. (omitted) -
Lee, Jong-Pill;Lee, Dong-Mi;Cho, So-Yeon;Cho, Chang-Hee;Park, Ju-Young;Lee, Kun-Jong;Kim, Zhe-Xiong;Ze, Keum-Ryon;Lee, Song-Deuk 192.1
Acanthopanax cortex (Acanthopanax sessiliflorum, Araliaceae, KP VIII), an important herbal drug, has been used as tonic, antistress and immuno-enhancing drugs in Korea. And Peiplocae cortex(Periploca sepium, Asclepiadaceae, CP 2000) has been used as cardiotonic, anti-inflammatory, and sedative effect in china. These are called “Namogapi” of Acanthopanax cortex and “Bukogapi” of Periplocae cortex in Chinese herbal market. These herbal medicines are sometimes circulated as same herbal medicine “Ogapi”. (omitted) -
Apigenin-7-O-
${\beta}$ -D-glucoside, chrysoeriol, and luteolin were isolated from the aqueous ethanolic extract of Zostera marina L. leaves as the scavengers of reactive oxygen species (ROS) with the SC$\_$ 50/ values of 0.18 mM, 0.68 mM, and 0.18 mM against 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 0.04 mM, 0.03 mM, and 0.01 mM against superoxide radicals in the xanthine/xanthine oxidase system, respectively. The luteolin suppressed the expression of matrix metalloproteinase-1 (MMP-1) up to 44% at 4.0${\mu}$ M. (omitted) -
Lee, Sung-Ok;Choi, Sang-Zin;Yang, Min-Cheol;Nam, Jung-Hwan;Lee, Kyu-Ha;Lee, Jong-Hwa;Jang, Ki-Uk;Lee, Kang-Ro 192.3
Aster species has been used in traditional chinese medicine for treatment of a bruies and asthma. On reviewing the literatures of this species, monoterpene glycosides, diterpenoids, triterpene glycosides, cyclic pentapeptides, oligopeptides and flavonoids 1) were isolated and some pharmacological activites were investigated 2). In continuation of our search for bioative components from Korean medicinal plants, we have examined Aster spathulifolius, collected from Jeju island on August 2001. (omitted) -
Activity-guided separation for the aerial parts of Rodgersia podophylla A. Gray gave a new acylated flavonoid, quercetin 3-O-
${\alpha}$ -L-(5$^2$ -acetyl)-arabinofuranoside (1), together with six known flavonoids (2-7). Their hepatoprotective activities were determined by using the primary cultures of rat hepatocytes injured by H$_2$ O$_2$ . Quercetin 3-O-${\alpha}$ -L-(3$^2$ -acetyl)-arabinofuranoside (3), kaempferol 3-O-${\alpha}$ -L-rhamnopyranoside (5) and quercetin 3-O-${\alpha}$ -L-rhamnopyranoside (6) exhibited hepatoprotective activities comparable to silybin at the concentration of 50 mM (45.7, 50.8 and 57.3 %, respectively), and the new flavonoid 1 showed hepatoprotective activity at the concentration of 100mM (50.1%). -
Phytochemical examination of Sophorae Fructus yielded six phenolic compounds. The structures were elucidated as genistein(1), genistin(2) and genistein 7-O-
${\alpha}$ - L-rhamnopyranoside(3) by phytochemical and spectral evidences. The other compounds(4, 5, 6) are understudied by 2D-NMR. Nitric Oxide and PGE$_2$ production inhibitory activities in INF-${\gamma}$ , LPS stimulated RAW 264.7 cell were examined. Compound 2 and 4 showed significant nitrogen monoxide(NO) production inhibitory activity in IFN-${\gamma}$ , LPS stimulated RAW 264.7 cell. (omitted) -
Platelets play critical roles in both hemostasis and thrombosis. It was reported that platelet aggregation is associated with an increase in superoxide production and can be inhibited by hydroxyl radical scavengers. In the course of our search for the anti-platelet, anti-coagulant and/or anti-oxidative components from plants, the MeOH extract of Crassula cv. "Himaturi" (Crassulaceae) was observed to have both anti-aggregatory and anti-coagulant effects. A novel compound, 12-O-(4'-O-methyl-galloyl)-bergenin (1), was isolated as an active component from the EtOAC soluble fraction. (omitted)
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Ternstroemia japonica (Theaceae) is widely distributed in Korea, Japan, Taiwan and China. The tree is a useful source of lumber, dye and horticulture. Its fruits have been used as folk medicine in Japan for the treatment of chest pain or numbness. Previously, we have isolated saponins and jacaranone derivatives from the fruits. In our continuous study on the same plant, the leaves of Ternstroemia japonica were extracted with MeOH and the MeOH extract was fractionated with solvents. The n-BuOH soluble fraction was separated by repeated column chromatographies on silica gel and Sephadex LH-20, and further purified by reversed phase HPLC. (omitted)
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The inhibitors of prostaglandin biosynthesis and nitric oxide production by corresponding inducible isozyme have been considered as potential anti-inflammatory and cancer chemopreventive agents. In our continuous search for cancer chemopreventive agents from natural products, we have evaluated the inhibitory potential of PGE
$_2$ and NO production in lipopolysaccharide (LPS)-induced mouse macrophage RAW 264.7 cells. As a result, pinosylvin (3,5-dihydroxy-trans-stilbene), a stilbenoid, mainly found from the heartwood and leaves of the Pinus sylvestris, showed potential inhibitory activity of LPS-induced PGE$_2$ and NO production in a dose-dependent manner. (omitted) -
Hong, Seong-Su;Han, Xiang-Hua;Park, Seon-Soon;Lee, kyong-Soon;Lee, Myung-Koo;Hwang, Bang-Yeon;Ro, Jai-Seup 194.3
As a part of an ongoing collaborative program to discover novel bioactive components of plant origin, the stem barks of Kalopanax septemlobus were extracted with MeOH, and successively partitioned with CH$_2$ Cl$_2$ , EtOAc, BuOH and water. Repeated column chromatographic separation of the CH$_2$ Cl$_2$ fraction resulted in the isolation of four compounds. Their structures were identified as vladinol E (1), (-)-simulanol{4-[3-hydroxymethyl-5-((E)-3-hydroxypropenyl)-7-methoxy-2,3-dihydrobenzofuran-2-yl]-2,6-dimethoxy-phenol} (2), vladinol F (3), and (${\pm}$ )-secoisolariciresinol (4). This is the first report on the isolation of these compounds from Kalopanax species. -
Kim, Hyang-Rim;Jeong, Yeon-Hee;Min, Hye-Young;Park, Go-Woo-Ni;Lee, Sang-Kook;Seo, Eun-Kyoung 194.4
Two phenolic flavonoids were isolated from the traditional medicine of Eastern Asia, Caesalpinia sappan L (Leguminosae). Brazilin (1) showed a significant inhibitory activity against inducible Nitric Oxide Synthase (iNOS) in lipopolysaccharides (LPS)-induced macrophage RAW 264.7 cells with an IC$\sub$ 50/ value of 1.68 mg/ml, which is more potent than the positive control, L-N$\^$ 6/-(1-iminoethyl)lysine (IC$\sub$ 50/ 3.49 mM). On the other hand, caesalpine J (2) was found to be inactive in the present iNOS assay system despite of their structural similarities. (omitted) -
Min, Byung-Sun;Yoon, Jeong-Hyeon;Park, Bo-Young;An, Ren-Bo;Lee, Joong-Ku;Kim, Tae-Jin;Joung, Hyo-Uk;Lee, Hyeong-Kyu 195.1
Styrax japonica Sieb. et Zucc. (Styracaceae) is a deciduous tree growing in Korea, Japan, and China. The pericarps of this plant have been used as a folk medicine for treatment of cough. Jegosaponins, deacyl jegosaponins and benzofurans have been reported from the fruits and seeds of this plant, and these compounds have been shown antisweet and cytotoxic activities. As a part of a research aimed at the discovery of biological active compounds from plant sources, we have studied a chemical constituent of the stem-bark of S. japonica. (omitted) -
Ma, Choong-Je;Kim, Seung-Hyun;Kang, So-Young;Koo, Kyung-Ah;Sung, Sang-Hyun;Lee, Ki-Yong;Lee, Ho-Yeon;Kim, Young-Choong 195.2
The CH$_2$ Cl$_2$ fraction of the bark of Machilus thunbergii Sieb. et Zucc. (Lauraceae) significantly protected primary cultures of rat cortical cells exposed to the excitotoxic amino acid, L-glutamate. Several lignans including (-)-isoguaiacin, meso- dihydroguaiaretic acid, machilin A, (+)-galbelgin, licarin A, (-)-sesamin, and (+)-guaiacin were isolated from the CH$_2$ Cl$_2$ fraction using by bioactivity-guided isolation techniques. Among these lignans, (-)-isoguaiacin, meso-dihydroguaiaretic acid, licarin A and (+)-guaiacin had significant neuroprotective activities against glutamate-induced toxicity in primary cultures of rat cortical cells at concentration ranging from 0.1${\mu}$ M to 10.0${\mu}$ M. (omitted) -
In this study, we investigated the molecular pathways targeted by platycodin D, which could involve apoptosis in immortalized human keratinocytes (HaCaT). We demonstrated that platycodin D-mediated apoptosis of HaCaT cells exhibited representative features, including DNA fragmentation, caspase-3, caspase-8 activation, and upregulation of Fas and FasL expression, but not p53 activation. To investigate the events involved in activation-induced FasL upregulation, we have examined mRNA accumulation, protein expression, and NF-
$\kappa$ B activity to elucidate transcription level in the HaCaT cell line treated with platycodin D. (omitted) -
Angelica genuflexa (Umbelliferae) is a perennial herbaceous plant which has also been variously reported as A. koreana and Ostericum koreanum. The MeOH extract was reported to have strong anti-thrombotic potential in the acute thrombosis model. In our preliminary testing, the MeOH extract and one of the solvent fractions (90% MeOH fr.) were observed to have both platelet anti-aggregating and anti-coagulant effects. Five coumarins, isoimperatorin (1), pabulenol (2), isooxypeucedanin (3), oxypeucedanin hydrate (4) and osthol (5) were isolated from the MeOH extract of Angelica genuflexa in the course of searching for anti-platelet and anti-coagulant components. (omitted)
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The Barks of Ulmus davidiana (Ulmaceae) have been used for the treatment of insecticide, anti-boil and anti-fungi in Korean traditional medicine. Four phenolic compounds were isolated from 80% Acetone extracts. The structures of these compounds were elucidated as (+)-catechin, (+)-catechin 7-O-
${\beta}$ -D-glucopyranoside, (+)-catechin 7-O-${\beta}$ -D-xylopyranoside and procyanidin B-1. These phenolic compounds showed significant nitrogen monoxide(NO) production inhibitory activity in IFN-${\gamma}$ , LPS stimulated RAW 264.7 cell and also showed significant antioxidative activity on DPPH radical. (omitted) -
To investigate biological active constituents from natural products, we have studied the roots of Angelica koreana Max. (Umbelliferae). Fifteen compounds were isolated from the MeOH extract by column chromatography on a silica gel. The compounds were identified as isoimperatorin, oxypeucedanin, oxypeucedanin hydrate, osthol, nodakenin, 2-hydroxy-4-methylacetophenone, cimifugin, falcarindiol, heraclenin, pabulenol, umbelliferone, demethylsuberosin, hamaudol, sec-O-glucosylhamaudol, and prim-O-glucosylcimifugin, respectivelv, by spectroscopic means. Among these, the latter eight compounds were isolated for the first time form this plant.
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One of the consequences of hyperglycemia is the excessive nonenzymatic glycation of proteins known as Millard reaction. Under hyperglycemia the irreversibly formed advanced glycation endproducts(AGEs) do not return to normal when hyperglycemia is corrected and continue to accumulate over the lifetime of protein. AGEs are largely involved in the pathogenesis of diabetic complications. To find possible AGEs inhibitor, BSA was added to a mixture of sugars and unprocessed-, processed Coptidis Rhizoma, Berberine, its standard compound or AG(Aminoguanidine HCl: positive control). (omitted)
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From the EtOAc fraction of the MeOH extract of Albizzia julibrissin (Leguminosae), a rare 5-deoxy flavone (geraldone), a 3',4',7,8-tetrahydroxyflavanone, an isoflavone (daidzein), and five prenylated flavonoids (sophoflavescenol, kurarinone, kurarinol, kuraridin and kuraridinol) were isolated and identified based on the analysis of spectral data.(omitted)
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As an attempt to search for bioactive natural constituents exerting antinociceptive and antiinflammatory activities, we examined the potency of the extract of R. coreanus fruits by the activity-guided fractionation. The EtOAc- and BuOH fraction and those alkaline hydrolysates showed significant antinociceptive effects as assessed by writhing-, hot plate- and tail flicks tests in mice and rats as well as antiinflammatory effect in rats with carrageenan-induced edema. BuOH extract was subjected to column chromatography to obtain a large amount of niga-ichigoside F
$_1$ (1, 23-hydroxytormentic acid 28-O-glc), which was again hydrolyzed in NaOH solution to yield an aglycone 23-hydroxytormentic acid (1a). (omitted) -
Choi, Sang-Zin;Lee, Sung-Ok;Yang, Min-Cheol;Nam, Jung-Hwan;Lee, Kyu-Ha;Jang, Ki-Uk;Lee, Jong-Hwa;Lee, Kang-Ro 198.1
As part of our systematic study for Korean Compositae plants, we have studied Saussurea nutans, collected at Gangwon Province on August 2001. Phytochemical studies on various species of genus Saussurea have resulted in the isolation sesquiterpene, triterpene and flavonoid$\^$ 1)/. S. nutans has been used for the treatment of rheumatic arthritis and dysmenorrhea in the Chinese folk medicine$\^$ 2)/. However, chemical constituents of this plant have not been reported until now. The MeOH extract of the aerial parts of this source was solvent fractionated into n-hexane, methylene chloride, ethyl acetate and BuOH soluble portions. (omitted) -
The anti-oxidant activities of fucosterol isolated from the marine algae Pelvetia siliquosa were investigated. Fucosterol exhibited a significant decrease in serum transaminase activities elevated by hepatic damage induced by CCl
$_4$ -intoxication in rats. Fucosterol inhibited the sGOT and sGPT activities by 25.57 and 63.16%, respectively. Fucosterol showed the increase in the anti-oxidant enzymes such as hepatic cytosolic superoxide dismutase, catalase and glutathione peroxidase activities by 33.89, 21.56 and 39.24%, respectively, in CCl$_4$ -intoxicated rats. (omitted) -
Eok, Kwon-Oh;Lee, Seung-Woong;Chung, Mi-Yeon;Kim, Young-Ho;Kim, Koan-Hoi;Rho, Mun-Chual;Lee, Hyun-Sun;Kim, Young-Kook 199.1
In the course of our search for intercellular adhesion molecule-1 (ICAM-1)/leukocyte function-associated antigen-1 (LFA-1) mediated cell adhesion inhibitors from natural sources, new type of cell adhesion inhibitors were isolated from the MeOH extract of Saururus chinensis roots. On the basis of spectral evidence, the structures of the active compounds were identified as manassantin A and B. Manassantin A and B inhibited phorbol 12-myristate 13-acetate (PMA)-induced homotypic aggregation of the human promyelocytic leukemia HL-60 cells without cytotoxicity with MIC value of 1.0 and 5.5 nM, respectively. (omitted) -
Li-Gao;Xu , Ming-Lu;Seo, Chang-Seob;Kim, Hyo-Jin;Lee, You-Jeong;Lee, Yeun-Koung;Son, Jong-Keun;Song, Dong-Keun 199.2
The bioassay-guided fractionation of protective agents against sepsis-induced lethality from the root bark of Paeonia suffruticosa led to the isolation of ten known compounds: paeonol (1), 2,5-dihydroxy-4-methoxyacetophenone (2) methyl 3-hydroxy-4- methoxybenzoate (3), acetovanillone (4), benzoic acid (5), benzoylpaeoniflorin (6), paeonoside (7), paeoniflorin (8), oxypaeoniflorin (9) and apiopaeonoside (10). Among them, 4 exhibited the highest survival rate in a dose-dependent manner (100% with a dose of 30 mg/kg versus 16.7% for the control experiment) and showed reduction of plasma alanine aminotransferase (ALT) value on the in vivo assay model of sepsis induced by LPS/GalN. -
Lee, Dong-Mi;Cho, So-Yeon;Cho, Chang-Hee;Lee, Jong-Pill;Seong, Rack-Seon;Lee, Kun-Jong;Yook, Chang-Soo;Xiong, Jin-Zhe;Ze, Keum-Ryon 199.3
Acanthopanacis Cortex (Acanthopanax sessiliflorum, Araliaceae, KP VIII), an important Korean medicinal herbal drug, has been widely used as tonic, anti-stress and immuno-enhancing drugs. To monitor the contents of active ingredients (acanthoside D[=eleutheroside E], eleutheroside B, isofraxidin, chlorogenic acid, and caffeic acid) in Acanthopanax sp., we developed the HPLC analysis method and validated. The simultaneous determination of five active ingredients was achieved in a C$\sub$ 18/ column with an acetonitrile water (containing 1 % phosphoric acid) (15 : 85) mobile phase. (omitted) -
Cephalotaxus koreana Nakai is an endemic species in Korea. The EtOH extract of leaf and branch from the plant showed potent antitumor activity in Teruhiro's method. The tumor volume inhibition ratio value is 25.2% with 20mg/kg in the BDF1 mouse injected LLC cell. We isolated one flavone, sciadopitysin (1), two flavone O-glycosides, quercetin 3-O-
${\beta}$ -D-glucuronide 6"-ethyl ester (2), apigenin 7-neohesperidoside (3) in comparison with literatures data. Compounds 1-3 showed stronger antitumor activity than Taxol used as positive control. The inhibition ratio values of compounds 1-3 is 34.9, 31.6, 34.0%, respectively, and Taxol is 27.0 % compared with control group. -
Ryu , Ji-Young;Son , Dong-Wook;Kang , Jung-Il;Lee, Sang-Yun;Kim, Hyun-Su;Lee, Sang-Hhyun;Shin, Kuk-Hyun 200.2
Six compounds were isolated from the stems of Acanthopanax senticosus (Araliaceae). Their structures were elucidated as iso-fraxidin, H-sesamin, 5-hydroxymethylfurfural, eleutheroside B, eleutheroside E and an unknown compound by spectral analysis. Of them, 5-hydroxymethylfurfural was isolated for the first time from A. senticosus. -
Reactive oxygen species(ROS) are produced at a high rate continuously as a by-product of aerobic metabolism. Several lines of evidence provided that ROS appears to cause to develop aging and various diseases. High level of hyaluronic acid with decreased molecular weight has been detected in patients with inflammatory diseases including rheumatoid arthritis. Hyaluronidase is an endohexosaminidase that initiates the degradation of hyaluronic acid with high molecular weight. Prunus persica Batsch var. davidiana Maximowicz has been known as a korean folk medicine for treatment of neuritis and rheumatism. (omitted)
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Ten compounds were isolated from the methanolic extract of the whole plants of Diodia teres through repeated silica gel and Sephadex LH-20 column chromatography. Their chemical structures were elucidated as three iridoid glycosides, a coumarin glycoside, and six flavonoids by spectroscopic analysis. These compounds were isolated for the first time from D. teres.
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Lee, Seung-Woong;Kim , Koan-Hoi;Kim, Young-Ho;Rho, Mun-Chual;Lee, Hyun-Sun;Kim, Young-Kook 201.1
Study of Acyl-CoA:cholesterol acyltransferase (ACAT) inhibitors from medicinal plants, we found strong inhibitory activity of ACAT enzyme from rat liver microsome by the CHC1$_3$ extract of Piper longum. Bioactivity-guided fractionation led to the isolation of Guineensine (1), its structure was elucidated by spectroscopic (IR, UV, MS and NMR) means. It inhibited ACAT activity in a dose-dependent manner with IC$\sub$ 50/ values of 1.2$\mu\textrm{g}$ /ml on in vitro assay using rat liver microsome. -
A novel lanostane-type triterpene, (24E)-3,4-seco-9
${\beta}$ H-lanosta- 4(28),7,24- triene- 3,26- dioic acid was isolated from Abies koreana (Pinaceae) which is a tall evergreen tree grown indigenously in southern Korea. The structure of this compound was characterized by spectroscopic methods. Cytotoxicity of the compound was evaluated in vitro using the SRB method, and it showed marginal activity against human cancer cell lines. -
Na, Min-Kyun;Hong, Nam-Doo;Kamiryo Yuko;Senoo, Yu-Ichiro;Yokoo Seiichi;Ito Shinobu;Miwa Nobuhiko 201.3
The ethanol extract from the fruit of Terminalia chebula (Combretaceae) and the hook of Uncaria sinensis (Rubiaceae) exhibited significant inhibitory activity on oxidative stress and the age-dependent shortening of the telomeric DNA length. In the peroxidation model using t-BuOOH, human epidermal keratinocytes-neonatal foreskin (HEK-N/F) cells were treated with the T. chebula and U. sinensis extracts. The results showed a notable enhancing effect on the cell viability of 60.5${\pm}$ 3.8 and 65.0${\pm}$ 3.0%, respectively, by 50$\mu\textrm{g}$ /ml of the extracts. (omitted) -
Yoon, Jeong-Seon;Lim, Song-Won;Yang , Hye-Kyeong;Ahn , Tae-Kyeong;Kim, Eun-Sil;Sung, Sang-Hyun;Kim, Young-Choong 202.1
Six compounds were isolated from the 90% MeOH fraction of the vine stem of Spatholobus suberectus Dunn (Leguminosae) using silica gel, reverse phase column chromatography and RP-HPLC. Structures of compounds 1-6 were elucidated by spectroscopic parameters of IR, E1 MS, FAB MS, lD-NMR and 2D-NMR spectrum and identified as pseudobaptigenin (1), genistein (2), (2R)-7-hydroxy-6-methoxyflavanone (3), (3R,4R)-2",4"-dihydroxy-6,7-methylenedioxy-isoflavan-4-ol (4), (3R,4R)-7,2" -dihydroxy- 4"-methoxyisoflavan-4-ol (5), sativan (6), respectively. Compounds 3, 4 and 5 have been newly reported in nature. -
Seo, Jee-Hee;Choi, Yeon-Hee;Kim, Jung-Sook;Kim, Seong-Kie;Choi, Sang-Un;Kim, Young-Sup;Ryu, Shi-Yong;Kim, Young-Kyoon 202.2
A bioassay-guided fractionation of the whole extract of Viscum album (a parasitic plant : Loranthaceae) led to the isolation of two triterpenoidal components, oleanolic acid (1),${\beta}$ -amyrin acetate (2), homoflavoyadorinin B (3) as well as large quantity of free fatty acid mixtures as active ingredients of the extract responsible for the antitumoral property. The EtOAc soluble part and BuOH soluble part of the extract demonstrated a significant inhibition on the proliferation of cultured human tumor cells such as A549 (non small cell lung), SK-OV-3 (ovary), SK-MEL-2 (melanoma), XF498 (central nerve system) and HCT-15 (colon) in vitro, whereas the remaining water soluble part exhibited a poor inhibition. (omitted) -
Two Known compounds, syringaresinol monoglucoside(8), chimaphilin(14), together with three new compounds, (9)[mp.
$106{\sim} 111^{\circ}C$ ,C_{29}H_{44}O_{13}$ ], (10)[mp.$180{\sim}182^{\circ}C$ ,$C_{15}H_{20}O_{9}$ ] and (11)[mp.$100{\sim}105^{\circ}C$ ,$C_{18}H_{28}O_{8}$ ] were isolated from the BuOH fractionof Pyrola japonics(Pyrolaceae). The structures of the known compounds were determined by chemical and spectorscopic methods. The assignments of the$^{1}H-$ and$^{13}C-NMP$ spectra of these compounds were carried out by two-dimensional$^1H-^1H-COSY$ , NOESY and$^1H-^{13}C$ multiple-bond, multiplequantum spectroscopic correlation techniques. The characterization of the three new compounds is now in progress. -
The present study was carried out to clarify whether isoflavonoids isolated from Belamcandae Rhizoma (Iridaceae) inhibit inflammation and angiogenesis by the experimental methods in vitro and in vivo. Among the isolated isoflavonoids, such as irigenin, irisflorentine, and iristectorene B inhibited nitric oxide (NO) production, as measured by nitrite formation at 3-30
${\mu}M$ . Also these compounds reduced cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) enzyme expression in a concentration dependent manner, when measured by western blotting, at 3-30${\mu}M$ . Irigenin, irisflorentine and iristectoren B decreased angiogenesis of chick embryos in the chorioallantoic membrane assay. These compounds also reduced the proliferation of calf pulmonary arterial endothelial (CPAE) cells and found to possess relatively weak gelatinase/collagenase inhibitory activity in vitro. These compounds, when administered subcataneously at the dose of 30mg/kg for 20 days to mice implanted with murine Lewis lung carcinoma (LLC), caused a significant inhibition of tumor volume. Therefore, antiangiogenic activities of isoflavonoids from Belamcandae Rhizoma might be due to antiproliferative activities under inhibition the induction of COX-2 and iNOS enzyme. -
Cudrania tricuspidata have been used for anti-inflammatory, anti-hepatotoxic, anti-hypertensive and anti-diabetic activities. In this study, in order to investigate the efficacy of antioxidant activity, the bio-activity guided fraction and isolation of physiologically active substance were performed. H
$_2$ O, 30%, 60%, 100% MeOH and acetone fractions were examined antioxidant activity by DPPH method. It was revealed that 30%, 60%, 100% MeOH frations have significantly antioxidant activity. (omitted) -
Nitric oxide (NO) produced in large amounts by inducible nitric oxide synthase (iNOS) is known to be responsible for the vasodilation and hypotension observed in septic shock and inflammation. Inhibitors of iNOS, thus, may be useful candidate for the treatment of inflammatory diseases accompanied by the overproduction of NO. We prepared alcoholic extracts of woody plants and screened the inhibitory activity of NO production in lipopolysaccharide (LPS)-activated macrophages after the treatment of these extracts. (omitted)
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Rehmanniae Radix Preparata attributes good blood circulation and it has been used for the treatment of dizziness, men's sterility, excessive loss of blood and weakness. On the quality control of the commercial Rehmanniae Radix Preparata, quantitative determination of 5-hydroxymethyl-2-furaldehyde (5-HMF) using HPLC method has been conducted. Quantitative analysis of 5-HMF in Rehmanniae Radix Preparata showered average 0.121
${\pm}$ 0.063% in 14 samples collected throughout the regions of Korea. Contents of loss on drying, residue on ignition and residue on acid insoluble ignition showered average 14.084${\pm}$ 2.804%, 3.415${\pm}$ 0.790% and 0.807${\pm}$ 0.474% respectively. -
The aqueous extract of European mistletoe (Viscum album, L.) has been used in cancer therapy. The purified mistletoe lectins, main components of mistletoe, have demonstrated cytotoxic and immune-system-stimulating activities. Korean mistletoe (Viscum album L. coloratum), a subspecies of European mistletoe, has also been reported to possess anticancer and immunological activities. A galactose- and N-acetyl-D-galactosamine- specific lectin (Viscum album L. coloratum agglutinin, VCA) with Mr 60 kDa was isolated from Korean mistletoe. (omitted)
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Antimutagenic activity-guided fractionation of an extract prepared from the thorns of Gleditsia sinensis Lam. (Leguminosae), which is a perennial shrub widely distributed throughout China (called "Zao Jiao Ci" ) and in Gyeongju city area in Korea (called "Jo Gak Ja" ) and has been used in traditional medicine for the treatment of swelling, suppuration, carbuncle and skin diseases, led to the isolation of one triterpenoid and four steroids, which were identified as D:C-friedours-7-en-3-one (1), stigmastane-3,6-dione (2),
${\beta}$ -sitosterol (3), sigmasterol (4), and stigmast-4-en-3,6-dione (5). (omitted) -
Several lines of recent evidences have shown that several pro-inflammatory genes or mediators, such as inducible nitric oxide synthase (iNOS)are strongly expressed in the ischemic brain. Inflammation is now recognized as a significant contributing mechanism in cerebral ischemia because anti-inflammatory compounds or inhibitors of iNOS have been proven to reduce ischemic brain damage. In iNOS assay, hexane fraction of M61 inhibited NO (iNOS IC50, 0.7
${\mu}$ g/ml). In vivo study was carried out to evaluate neuroprotective effect of hexane fraction of M61 after transient global ischemia using Mongolian gerbil ischemia model. (omitted) -
As part of our program to isolate bioactive compounds from korean natural sources, we have screened traditional medicinal plants to cytotoxity on human tumor cells. Of them, the MeOH extract from rhizome of Coptis japonica Makino was found to be active against five cultured human tumor cell lines. So, the MeOH extract was subjected to successive solvent partitioning to give n-hexane, chloroform and BuOH. The activity was concentrated into the chloroform extract. The extract was chromatographied on a silica gel column and resulted in the isolation 5 alkaloids. (omitted)
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The genus Styrax (Styracaceae) is different from other genera of this family due to the production of resinous material, usually secreted when the barks and trunks are injured by sharp objects. This resin, in the past considered a miraculous remedy in several parts of Asia and America, has been used in traditional medicine to treat inflammatory diseases. The CH
$_2$ Cl$_2$ fraction of Styrax japonica showed significant cytotoxic activities by SRB method against five human tumor cell lines (A549, HCT-15, MES-SA, SK-OV-3, and SK-MEL-2). (omitted) -
Jin, Jing-Ling;Lee, Sang-Hyun;Lee, Yong-Yook;Kim, Jeong-Mi;Heo, Jung-Eun;YunChoi, Hye-Sook 206.1
From methanol extract of Acanthopnanax senticosus, six platelet anti-aggregating compounds, chiisanogenin (1), chiisanoside (2), ursolic acid (3), oleanolic acid (4), b-sitosterol (5) and daucosterol (6) were isolated. All of the isolated compounds showed dose-dependent inhibitory activities to rat platelet aggregation induced by all the agonist employed. Compound 1 showed about 50 folds higher potency than acetylsalicylic acid (ASA) on U46619 induced platelet aggregation (IC$\sub$ 50/ : 6.21${\mu}$ M) and 10 ∼ 20 folds higher effect than ASA on epinephrine and arachidonic acid (AA) induced aggregation (IC$\sub$ 50/ ; 2.50 and 4.81${\mu}$ M, respectively). (omitted) -
In continuing search for bioactive compounds from Korean marine algae, we found cholinesterase-inhibitory activity in the methanolic extract of brown alga Sargassum sagamianum. After partitioning between CHCl
$_3$ and 30% MeOH, the former layer was purified by a series of ODS flash, silica column, gel-filtration on Sephadex LH-20, and HPLC to give two farnesylacetone derivatives. Their structures were identified by comparison with the literature data. Compounds 1 and 2 showed moderate acetylcholinesterase and butyrylcholinesterase inhibitory activities with IC$\sub$ 50/ values of 65.0∼48.0${\mu}$ M and 34.0∼23.0${\mu}$ M, respectively. (omitted) -
Li Gao;Kim, Jae-Hyon;Xu, Ming-Lu;Seo, Chang-Seob;Kim, Hyo-Jin;Lee, You-Jeong;Lee, Yeun-Koung;Lee, Seung-Ho;Chang, Hyeun-Wook;Son, Jong-Keun 206.3
The bioassay-guided fractionation of the methylene chloride soluble portion of a methanol extract of Gastrodia elata tubers led to the isolation of a new furfural, 5-(4-hydroxy-benzyloxymethyl)-furan-2-carbaldehyde (2), together with four known compounds (1, 3-5), which exhibited potent inhibitory activity at the concentration of 25$\mu\textrm{g}$ /ml on melanin biosynthesis in cultured B-16 mouse melanoma cells. -
The Aster tataricus is a chinese traditional medicine called “Ziwan” which has an expectorative and remediable cough action. The anti-oxidant activities of A. tataricus were investigated. The MeOH extract of A. tataricus showed strong anti-oxidant activity in the NBT(nitroblue tetrazolium) method system, and thus fractionated with several solvents in to the EtOAc, n-BuOH, CH
$_2$ Cl$_2$ , H$_2$ O fraction. The EtOAc soluble fraction exhibiting strong anti-oxidant activity was further purified by repeated silica gel and sephadex LH-20 column chomatography. (omitted) -
To develop useful antifungal agents from essential oils in Korean plant resources, the activities of Thymus quinquecostatus and T. quinquecostatus var. japonica were evaluated against ten pathogenic fungi. Their results were compared with those of T. vulgaris, which is native to Europe.The essential oils of the tested Thymus species were obtained by steam distillation using a simultaneous steam distillation-extraction apparatus. The above ground parts of plants cultivated in the herbal garden of Duksung Women"s University were used. (omitted)
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Objectives:We have reported that oral administration of Saiko-ka-Ryukotsu-Borei-To (SRB), a traditional Chinese formulation, inhibited the intimal thickening in carotid artery after balloon injury in cholesterol-fed rats. To elucidate its mechanism, the effects of SRB on migration and proliferation of vascular smooth muscle cell (VSMC) were examined in vivo and in vitro.Methods: < In vivo-study> Rats were fed on diet containing 1% cholesterol and SRB 3 days before and 4 days after denudation. Simvastatin was used as a positive control. (omitted)
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We synthesized naphthazarin derivatives from shikonin, a major compound from Lithospermum erythrorhion Sieb et ZUCC. Of derivatives, DMNQ S64, 2-or 6-(l-hydroxyiminoalkyl) effectively showed antitumor activity on A549, human lung cancer cells (IC
$\sub$ 50/= 30${\mu}$ M). It significantly inhibited prostaglandin E$_2$ (IC$\sub$ 50/= 10${\mu}$ M). We also confirmed it selectively downregulated the expression of cyclooxygenase 2(COX-2), while it didn't affect COX-1. The induction of apoptosis by DMNQ S64 is underway. -
TCDD (2,3,7,8-tetrachlorodibenzo-p-dioxin), one of the notorious toxic environmental pollutants, damages various organs including liver and is regarded as an endocrine disrupter. To investigate the effects of Houttuynia cordata Thunb (HCT) on the biochemical parameters of function, liver and serum of TCDD-treated rats were used. After 7 days from TCDD (1
$\mu\textrm{g}$ /kg) injection, HCT (200 mg/kg) was administered into rats intraperitoneally for 4 weeks. The lipidperoxide content was examined by measuring the level of total cholesterol, HDL-cholesterol, LDL-cholesterol, total lipid and triglyceride (TG) in serum, and malondialdehyde (MDA) in liver tissue of rats. (omitted) -
Lonicerae Folium et Caulis, the folium and stem of Lonicera japonica Thunb., has been used as diuretic, stomachic, antipyretic, analgesic and anti-inflammatory agent in Korea. We isolated a main iridoid, loganin which has some important biological effects from the folium and stem of this plant. Generally, it is known that iridoid compounds have variable contents by the collecting time and a part of plant. The content of main compound is important to evaluate its quality. In order to evaluate the quality of Lonicerae Folium et Caulis, the method of quantitative determination of loganin as a reference standard compound has been developed. (omitted)
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Polygoni cuspidatum has been used as treatments of dermatitis, inflammation and hyperlipidemia, and diuretic in folk medicine. In order to evaluate the urinary effect of Polygoni cuspidati Radix, its MeOH extract was administered in rats by in vivo test. We measured urine volume, chemical parameters, and electrolytes in serum and urine of the rats.The results showed that Polygoni cuspidati Radix MeOH extract had urinary volume increase and normal level parameters in rats.
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The effects of the methanol subfraction of Pueraria radix on hydrogen peroxide-induced lipid peroxidation and Cd-induced cytotoxicity were investigated in NIH3T3 fibroblasts. After the methanol subfraction treatment, the content of MDA induced by 600
${\mu}$ M H2O2 significantly decreased in proportion to the subfraction concentrations as well as 50${\mu}$ M CdCl2-induced cytotoxicity. Especially, 200$\mu\textrm{g}$ /mg concentration of methanol subfraction was strongly shown inhibition of lipid peroxidation and detoxification of Cd. These results suggest that the methanol subfraction of Pueraria radix retains a potential antioxidant and protective effect against cadmium. -
Cordyceps species has been used as antiinflammatory, antitoxic, diuretic in folk remedies. Recent research has been reported the effect of anticancer, antidiabetic, antimutagenic, antilipid peroxidation. We examined the antidiabetic activity of cultivated Cordyceps pruinosa on streptozotocin-induced diabetic rats. The blood glucose level was recovered by treatment with Cordyceps pruinosa ethanol extract. The contents of GPT, total cholesterol and xanthine oxidase, glutathione peroxidase, catalase activities of the cytosol were significantly decreased as compared to the diabetic group. (omitted)
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Jun , Jung-Yang;Ko , Eun-Kyung;Kim, Mi-Hee;Li Xun;Kang , Tai-Hyun;Park, Sun-Guk;Kim, Youn-Chul 210.1
Keokhachukeu-tang is the one of Chinese traditional prescription used for the treatment of liver disease. This prescription consists of Carthami Flos (6g), Persicae Semen (9g), Pteropi Faeces (9g), Corydalis Tuber (9g), Moutan Radicis Cortex (6g), Paeoniae Radix rubra (9g), Angelicae gigantis Radix (9g), Cnidii Rhizoma (9g), Linderae Radix (12g), Cyperi Rhizoma (12g), Aurantii Fructus (9g), and Glycyrrhizae Radix (3g). Water extract of Keokhachukeu-tang showed a moderate hepatoprotective effect on tacrine-induced cytotoxicity in Hep G2 cells. (omitted) -
Cornis fructus were extracted by successive extractions and then fractionated with chloroform extract to get active fractions. This study was performed to determine the cytotoxic effect of chloroform extract from Cornis fructus on NIH 3T3 fibroblasts and cancer cell lines using MTT assay. All extracts did not exhibit cytotoxicity in HIH 3T3 fibroblasts. Chloroform extract exhibited antitumor activity in A549, MDA-MB-123, B16 melanoma and SNU-C4 cells. Futher fractionation with chloroform extract was performed to obtain effective fractions. (omitted)
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This study was performed to determine the cytotoxic effect of methanol extract from medicinal plants. The cell viability was determined by the MTT method. Their cytotoxic activities against three cancer cell lines such as A549, MDA-MB-231 and SNU-C4 cell line were tested. Among them, The methanol extract of Saururus Chinensis Bail showed the strongest cytotoxic effect against SNU-C4 cells. These results suggest that the methanol extract of Saururus Chinensis Bail possessed a potential antitumorous agent
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The antioxidant activity of solvent extracts of leaves, trunk and root Pueraria Radix was determined by measuring the radical scavenging effect on l.l-diphenyl-2-picrylny drazyl(DPPH) radical. Extacts prepared from root showed radical scavenging effect on DPPH radical. But, extracts prepared from leaves and trunk did not show activity. The ethyl acetate ewtract of Pueraria Radix root showed radical scavenging activity at an IC 50 value of 75.7
$\mu\textrm{g}$ /$m\ell$ . -
On the purpose of develcpement of antioxidative compound from natural sources, medicinal plants known to have antioxidant actuvity have been examined concening DPPH radical scavenging activity and SOD-liked activities. Among 8 plants exhibiting the activity, Houttuynia cordata THUNB was selected as resources to search for active compounds due to rareness of study. The antioxidative compounds from Houttuynia cordata THUNB,quercitrin was assayed using a DPPH free radical. The DPPH radical scavenging activity of quercitrin was similar to that of BHA and Ascorbic acid
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Saururus Chinensis Baill (Saururaceae) has been used as folk medicine for analgesics, beriberi, edema, hepatitis, and icterus, etc. Hepatoprotective effects of Saururus chinensis Baill (SCB) administration on function of the biochemical parameters in liver of 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) treated rats were investigated. After 7 days from TCDD(1
$\mu\textrm{g}$ /kg) injection, SCB(200mg/kg) was administered into rats intraperitoneally for 4 week.s We examined the antioxidative enzymatic activity by measuring the level of AST and ALT in serum and SOD, Catalase, GPx, GSH and GSSG in liver tissue of rats. (omitted) -
Jung, Ji-Wook;Ahn, Nam-Yoon;Oh, Hye-Rim;Park, Sung-Hwan;Oh, Jin-Kyung;Lee, Bo-Kyung;Kim, Dong-Hyun;Ryu, Jong-Hoon 211.3
Scutellaria baicalensis Georgi is one of the most important medicinal herbs in traditional chinese medicine. The object of this study was to determine the effects of water extracts of Scutellaria baicalensis (SB) and Scutellaria baicalensis metabolite (SBM) on the anxiolytic-like activities in the elevated plus-maze (EPM) test. The water extracts of SB (100, 200, or 400 mg/kg), and SBM (100 mg/kg) were orally administered to male SD rats for 3 day. All rats were subjected to behavioral tests for the anxiolytic activity at 3 days. (omitted) -
Ahn, Nam-Yoon;Jung, Ji-Wook;Oh, Hye-Rim;Lee, Bo-Kyung;Oh, Jin-Kyung;Cheng, Jae-Hoon;Ryu, Jong-Hoon 212.1
The purpose of the this study was to characterize the putative anxiolytic-like effects of the aqueous extract of Albizzia julibrissin stem bark using the elevated plus maze (EPM) in rats. The water extract of Albizzia julibrissin was orally administered at 10, 50, 100 or 200 mg/kg to adult male SD rats, 1 h before behavioral evaluation in an EPM, respectively. Control rats were treated with an equal volume of saline, and positive control rats buspirone (1 mg/kg). Single or repeated treatment (for 7 days) of the water extract of Albizzia julibrissin (at 100 or 200 mg/kg) significantly increased time-spent and arm entries into the open arms of the EPM, and decreased time-spent and arm entries in the closed arms of the EPM versus saline controls (P < 0.05). (omitted) -
In the course of searching for BACE1 (
${\beta}$ -secretase) inhibitors from natural products, the ethyl acetate soluble fraction of green tea, which was suspected to be rich in catechin content, showed potent inhibitory activity. (-)-Epigallocatechin gallate, (-)-epicatechin gallate, and (-)-gallocatechin gallate ware isolated with IC$\_$ 50/ values of 1.6${\times}$ 10$\^$ -6/ M, 4.5${\times}$ 10$\^$ -6/ M, and 1.8${\times}$ 10$\^$ -6/ M, respectively. Seven additional authentic catechins were tested for a fundamental structure-activity relationship. (-)-Catechin gallate, (-)-gallocatechin, and (-)-epigallocatechin significantly inhibited BACE1 activity with IC$\_$ 50/ values of 6.0${\times}$ 10$\^$ -6/ M, 2.5${\times}$ 10$\^$ -6/ M, and 2.4${\times}$ 10$\^$ -6/ M, respectively. (omitted) -
Sphingolipids and their metabolites are highly bioactive molecules that affect various cellular functions including differentiation, cellular senescence, apoptosis, and proliferation when added exogenously, or elevated intracellularly by turnover of complex sphingolipids or synthesis from de novo pathway. We are investigating the relationship of sphingolipids cycle in apoptosis early events. A new column liquid chromatography- tandem mass spectrometry (LC/MS/MS) in combination with multiple reaction monitoring (MRM) method was developed for the rapid, simultaneous and quantitative determination of unambiguous detecting sphingolipids in cells. (omitted)
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A simple analytical procedure using FT-NIR for the rapid determination of individual ingredients was evaluated. Direct measurements were made by reflection using a reflectance accessory, by transmittance using tablet accessory and turn table. FT-NIR spectral data were transformed to the first derivative. Partial Least Square Regression(PLSR) was applied to quantify near-infrared (NIR) spectra of 2 ingredients. These calibration models were cross-validated (leave-one-out approach). The prediction ability of the models was evaluated on ambroxol tablets and compared with the real values in manufacturing procedure. (omitted)
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Osteoporosis is the most common form of metabolic bone disease and is an important cause of morbidity and mortality in the elderly and especially in postmenopausal women. The possible beneficial action of essential fatty acids and their metabolites both in the prevention and treatment of osteoporosis needs attention. Therefore in this study, fatty acid levels of the normal groups was compared with those of patients. And then star symbol plots were drawn based on the fatty acids values of patients normalized to the corresponding normal group values to transform into visual patterns discriminating from the normal pattern. (omitted)
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Metabonomic analysis using Liquid Chromatography-Mass Spectrometry (LC-MS) was employed to test the feasibility to predict chemical-induced toxicity. Time-dependent metabolic variations were evaluated in rats treated with the model hepatotoxin,
${\alpha}$ - naphthylisothiocyanate (ANIT). Urine samples of ANIT treated group and control group were collected up to 7 days postdose. Urine samples were analyzed by gradient HPLC combined with electrospray mass spectrometry. The chromatographic results were data-reduced and analyzed using principal component analysis to show the time dependent biochemical variations induced by ANIT toxicity. (omitted) -
Ji, Hye-Young;Lee, Hye-Won;Lee, Hong-Il;Kim, Hae-Kyoung;Shim, Hyun-Joo;Kim, Soon-Hoe;Kim, Won-Bae;Lee, Hye-Suk 214.2
Eupatilin (5,7-dihydroxy-3",4",6-trimethoxyflavone) is an active ingredient of an ethanol extract of Artemisia asiatica (DA-9601) that is used in the treatment of gastritis. In vitro and in vivo metabolism of eupatilin in the rats has been studied by LC- electrospray mass spectrometry. Rat liver microsomal incubation of eupatilin in the presence of NADPH and UDPGA resulted in the formation of four metabolites (M1-M4). M1, M2, M3 and M4 were tentatively identified as 3"- or- 4"-O-demethyl-eupatilin glucuronide, eupatilin glucuronide, 6-O-demethyleupatilin and 3"-or 4"-O-demethyl- eupatilin glucuronide, eupatilin glucuronide, 6-O-demethyleupatilin and 3"-or 4"-O- demethyl-eupatilin glucuronide, eupatilin glucuronide, 6-O demethyleupatilin and 3"-or 4"-O-demethyl-eupatilin glucuronide, respectively. (omitted) -
The chiral separation of multiple
${\beta}$ -blockers is described for their accurate chiral discrimination by chiral capillary electrophoresis (CE). The cyc1odextrin-modified CE system was operated in the reversed polarity mode. In this mode, fairly good enantiomeric resolutions were achieved. Relative migration times to internal standard under optimum conditions were characteristic of each enantiomer with good precision. Therefore, in this study, the usefulness for the chiral separation and accurate identification will be discussed. -
In galactose metabolic pathway : there are three inborn metabolic disorders galactokinase deficiency (galactosemia type II), galactose-1-phosphate uridyl transferase(GALT) daficiency (galactosemia type I ), uridine diphosphate galactose-4-epimerase deficiency (galactosemia typeIII). Among these disorders GALT deficiency is the most severe and common. Infants with GALT deficiency fail to metabolize galactose-1-phosphate. As a consequence, galactose-1-phosphate and galactose are accumulated in blood in which GALS enzyme plays the role of a pathognomonic marker. (omitted)
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Min, Chung-Sik;Jang, Seung-Jae;Choi, Bo-Kyung;Kim, Young-Lim;Jung, Hae-Yun;Bak, Kyung-Min;Lee, Kyung-Hee;Jo, Keang-In;Gu, You-Ni 215.1
A various${\alpha}$ -arylmethylpropionic acids(profen) have been widely used as non-steroidal anti-inflammatory drugs for the relief of acute and chronic rheumatoid arthritis and osteoarthritis, as well as for other connective tissue disorders and pains. Example is fenoprofen, ibuprofen, ketoprofen, and naproxen. All are chiral and, except for naproxen and ibuprofen, are marketed in racemic form. Enantioseparations of profens have been of considerable interest becaus their anti-inflammatory and analgesic effects have been attirbuted almost exclusively to their (S)-enantiomer. (omitted) -
Tyrosinase is an important enzyme involved in the transition steps from tyrosine to melanin. Inhibition of the tyrosinase activity could block melanin formation from tyrosine and thus prevent melanin pigmentation on skin. This may contribute to the development of new whitening agent that would be useful in the prevention of pigmentation. in this study, we isolated tyrosinase inhibitory compound from BuOH fraction of Potentilla bifurca L. var. glabrata Lehm by activity guided fractionation method. Based on spectroscopic data, the active compound was identified as a quercetin 4"-O- glucopyranoside.
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Eupatilin is a major active component of Stillen\ulcorner(Artemisia Herba Extract) having a potent antigastritic effect. We investigated the physical properties of eupatilin using high performance liquid chromatography. Solubility, stability & partition coefficient of eupatilin were investigated. pH-stability of eupatilin was examined over the broad range through pH1-9 at 37
$^{\circ}C$ & it has good stability above the broad range pH. The solubility of eupatilin was extremely low but the value of logP was more than 2. Also, a high performance liquid chromatographic method was developed for the determination of eupatilin in rat plasma. (omitted) -
P. ginseng C.A. Meyer is one of the most widely used herbal medicine in Asia. It has been used for the treatment of many disorders. Its major constituent is known to be ginsenosides, and there are many documents about bioactivities of ginsenosides such as anti-oxidant, anti-tumorigenic, anti-fatigue, and anti-inflammatory activities. Some of these activities are supposed to have some correlation with inhibitory action of cyclooxygenase (COX). Ginsenosides from P. ginseng and sapogenins were evaluated for their inhibitory effects against both cyclooxygenase-1 and -2 (COX-1 and -2). Inhibitory activity was evaluated by measuring prostaglandin E
$_2$ (PGE$_2$ ) production from arachidonic acid with an ELISA reader. (omitted) -
Sphingolipids has been known to induce apoptosis, cell proliferation, differentiation and migration in a variety of cell types. Recently, its phosphate form was suggested that they may act both as an agonist ligand to SlPRs and a second messenger in intracellular action. Phytosphingosine(PHS) is not easily detected due to trace component of cellular lipids in mammalian and human tissues while this is a major sphingolipid in yeast and plants. We therefore developed highly sensitive and reproducible analytical method for PHS and its phosphate by oxalic acid bis(2,4,6-tri-chlorophenyl) ester(TCPO)-hydrogen peroxide(H
$_2$ O$_2$ ) chemiluminescence. (omitted) -
Jung, Da-Young;Chang , Young-Eun;Ha , Hye-Kyung;Yang , Ha-Ru;Lee, Ho-Young;Kim, Chung-Sook 217.1
Phytoestrogen has been used as supplement in order to treat osteoporosis. The representative phytoestrogen, isoflavones, are daidzein, genistein and formononetin which were present highly in legumes. We have studied the quantitative analysis of isoflavones in KUNBO by HPLC. KUNBO, a mixed herbal extract including Astragali Radix and Rhynchosiae nulubilis Semen (Leguminosae), etc., is a nutraceutical candidate for type I osteoporosis. olumn used in HPLC was LUNA 5${\mu}$ C18 (250${\times}$ 4.6mm) (Phenmenex Co.m Torroance, CA, U.S.A.). (omitted) -
Kim, Sook-Jin;Lee, Seung-Seok;Ji, Hye-Young;Lee, Hong-Il;Lee, Seon-Kyoung;Yi, Kyu-Yang;Yoo, Seong-Eun;Hwang, Jeong-Sook;Lee, Hye-Suk 217.2
A liquid chromatography-tandem mass spectrometric (LC/MS/MS) method was developed for the determination of a new anti-angiogenic drug KR-31831 in rat plasma. KR-31831 and internal standard, KR-31543 were extracted from rat plasma with dichloromethane at basic pH. A reverse-phase LC separation was performed on Luna C8 column with the mixture of acetonitrile-ammonium formate (10 mM, pH 4.5) (67:33, v/v) as mobile phase. The detection of analytes was performed using an electrospray ionization tandem mass spectrometry in the multiple-reaction-monitoring mode. (omitted) -
Acetyl-L-carnitine, a physiological component of the L-carnitine family, has been proposed for treating Alzheimer's disease in pharmacological doses. Acetyl-L-carnitine and d3-acetylcarnitine (internal standard) were analyzed by electrospray ionization / tandem mass spectrometry (ESI/MS/MS) after derivatization to their butylesters through treatment with butanolic hydrogen chloride. Acetyl-L-carnitine produced a protonated precursor ion at m/z 260 and a corresponding product ion of m/z 85. Analytes were separated on a Capcell Pak C18 (2.0
${\times}$ 150mm, 5 mm). (omitted) -
Shin, Byong-Kyu;Piao, Xiang-Lan;Yoo, Hye-Hyun;Park, Yun-Kyung;Baek, Seung-Hoon;Kim, Bak-Kwang;Park, Man-Ki;Park, Jeong-Hill 218.1
Saponins are known to be the major constituent of Panax ginseng. More than 30 kinds of ginseng saponins are reported so far. The major saponins in white ginseng (WG) or red ginseng (RG) are ginsenosides Rb1, Rb2, Rc, Rd, Rg1, and Re. HPLC method with ELSD or UV detection was used to analyze ginsenosides. Recently, a new processed ginseng with fortified activity, named as Sun Ginseng (SG), was reported. The major ginsenosides of SG are totally different from that of WG or RG, i.e., ginsenoside Rg3, Rk1, and Rg5 are the major constituents of SG. (omitted) -
Paik, Man-Jeoneg;Choi, Young-Mie;Nguyen, Duc-Toan;Kim, Ji-Yung;Kim, Jung-Han;Kim, Kyoung-Rae 218.2
An efficient method is described for the enantioseparation of urinary amino acids to determine their absolute configurations. It involves two-phase extractive ethoxycarbonylation in alkaline aqueous solution with subsequent extraction after acidification. The resulting derivatives of amino acids are converted to volatile diastereomeric esters or amides for the direct analysis by gas chromatography (GC) on achiral dual-columns with different polarities. The present method was applied to urine specimens from patients with inherited metabolic disorders. In this study, the usefulness for the chiral separation of diagnostic amino acids will be discussed. -
In this study, a FT-NIR spectroscopy was used to determine skin moisture. NIR diffuse reflectance spectra were collected from separated dorsal and abdominal hairless mouse skin. Partial least squares regression (PLSR) was applied to develop calibration models that determine the water content. The seven spectra regions, such as 833-2500, 1100-2250, 1100-1750, 1750-2250, 1200-1600, 1800-2200, and 1200-2200 except 1600-1800 nm, were investigated for the best model by PLSR. The developed model predicted skin moisture for validation set with a standard errors of prediction (SEP) of 4.43%, when used 833-2500 nm. (omitted)
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$^1$ H-NMR method for the determination of enantiomeric purity of (S)-(+)-ibuprofen was developed using (-)-cinchonidine as a chiral solvating agent. (S)-(+)-ibuprofen was prepared by optical resolution of racemic ibuprofen using preferential recrystallization method with (S)-(-)-${\alpha}$ -methylbenzylamine and (R)-(-)-ibuprofen by semi-preparative chiral HPLC using chiral OD column and n-hexane/2-propanol/trifluoroacetic acid as a mobile phase. Several concentrations of synthetic mixture of (S)-(+)-ibuprofen and (R)-(-)-ibuprofen were added to the (-)-cinchonidine disolved in CDCl$_3$ . (omitted) -
Shin, Myoung-Hee;Lee, Young-Ja;Lee, Chang-Hee;Jin, Jong-Sung;Kim, Mi-Kyeong;Jin, Sun-Kyung;Doh, Hea-Jeong;Jung, Jin-Su 219.2
We want to actively cope with technological developments by improving our drug specification in Korean Pharmaceutical Codex. Pheniramine maleate and naphazoline HCl of Pheniramine Maleate and Naphazoline Hydrochloride Ophthalmic Solution were ordained as UV spectroscopy and HPLC, respectively. Simultaneous analysis of those using HPLC has been developed. The assays of two drug products were 97.2%, 102.2% (pheniramine maleate), 96.8%, 101.3% (naphazoline HC1) respectively ; the specification rage if 90.0∼110.0%. (omitted) -
We describe here solid-extraction and derivatisation methods of
${\beta}$ -adrenoceptor blocking drugs used for the treatment of various cardiovascular disorders such as hypertension, angina pectoris and cardiac arrhythmia: propranolol, metoprolol, sotalol, timolol, oxprenolol, alpranolol, atenolol, pindolol. Solid-extraction and derivatisation methods are described involving the use of Bond Elut Certify cartridges, MSTFA and MBTFA. Gas chromatographic-mass spectrometry analysis(GC/MS) was carried out select-ion monitroing mode. (omitted) -
A sensitive and selective liquid chromatographic method for the determination of carvedilol in human plasma was developed and validated. Analytes were separated on a XTerra C18 column with acetonitrile-methanol-30 mM KH
$_2$ PO$_4$ (pH 2.5) (20 : 20 : 60, v/v/v), as mobile phase. One mL plasma were pipetted into glass tubes and spiked with 0.05 mL of internal standard solution. After adding 7 mL of diethyl ether, the plasma sample was then shacked for 15 min. A centrifuged upper layer was back-extracted with 150 uL of 0.05 M sulfuric acid. (omitted) -
Many interference in blood should be considered for non-invasive blood glucose level monitoring by near-infrared spectroscopy because blood glucose concentration is about 0.1% (w/v) in normal state. In this study, we investigated the influence of other blood components on blood glucose level monitoring by near-infrared spectroscopy. It carried out by newly developed portable type-NIR system (1100∼2200 nm). Spectrum features of NIR diffuse spectral data were investigated for some blood compnents powder such as hemoglobin, blood serum albumin, urea, uric acid, ascorbate, glucose, cholesterol and as adding glucose powder into other blood components powder mixture. (omitted)
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Enantiomers of pindolol were prepared by chromatographic method. Racemic pindolol was derivatized with S-(-)-menthyl chloroformate((-)-MCF) forming its diastereomer, R-(+)-pindolol-(-)-MCF and S-(-)-pindolol-(-)-MCF. The diastereomer mixture was then chromatographically resolved to each diastereomer. Each diastereomer was further hydrolyzed with alkali to each enantiomer quantitatively. Racemization was not occurred in this process. Pindolol enantiomers were recovered producing good yield over 30% over all process.
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Armeniacae Semen is a seed of Prunus armeniaca Linne var. ansu Maximowicz, which belongs to Rosaceae family. It contains amygdalin and fatty oil and is widely used to treat asthma, dysponea and edema. It was reported that D-amygdalin in Armeniacae Semen undergoes hydrolytic reaction by emulsin when using water, and esecially it is almost decomposed when extracting from powder type. we set up a condition where we can achieve the maximun extraction yield through the study of the methods to rstrain emulsin from causing hydrolysis of D-amygdalin in Armeniacae Semen in the aqueous solution and to prevent D-amygdalin from being converted into neoamygdalin. (omitted)
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Several Compendia are effective in relation with production and supply of pharmaceutical agents in Korea. Those compendia exists only in printed documents, which are not suitable for the analysis of their contents and inter-relationship among them when they have specifications on the same or related pharmaceutical agents. For the analysis of contents of Korean compendia, database system is desinged and all of the available data are entered into relational database system. Every specification was analyzed into several database tables, fields and relations between tables. (omitted)
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Park, Yun-Kyung;Yoo, Hye-Hyun;Baek, Seung-Hoon;Lee, Seung-Ho;Kim, Chang-Min;Lee, Kyung-Soon;Park, Man-Ki;Park, Jeong-Hill 221.3
Adenophorae Radix, the roots of Adenophora triphylla var. japonica Hara (Campanulaceae) is known to be an anti-inflammatory and antitussive drug used for the treatment of lung disease. However quality control method is not established yet. This study is to establish the quality control method of Adenophorae Radix.From the roots of this plant, we isolated (6R,7R)-E,E-tetradeca-4,12-diene-8,10-diyne-1,6,7-triol (1) as a marker compound for the quality control and determined its content by HPLC-UV detector. (omitted) -
This study was carried out to investigate the quality control of domestic and imported Puerariae Radix. It was analyzed by HPLC using
${\mu}$ -Bondapak C$\sub$ 18/ column with 35% MeOH containing 1% CH$_3$ 3CO$_2$ H system as the mobile phase at UV 254nm. Good linearity showed over the range of 10 to 200$\mu\textrm{g}$ /$m\ell$ (r$^2$ =1) for Puerarin, and 0.5 to 10$\mu\textrm{g}$ /mg(r$^2$ =0.9999) for Daidzein. The average contents of Puerarin and Daidzein were 5.5${\pm}$ 1.2%(Domestic), 5.3${\pm}$ 0.7%(Imported), and 0.05${\pm}$ 0.02%(Domestic), 0.08${\pm}$ 0.02%(Imported).The average recovery rates of Puerarin and Daidzein were 101.8${\pm}$ 1.9% and 97.2${\pm}$ 0.7%, respectively. -
Baek, Seung-Hoon;Cho, Yon-Hee;Lee, Kyung-Soon;Kim, Bak-Kwang;Park, Man-Ki;Park, Jeong-Hill 222.2
The Araliae continental is Radix is the root of Aralia continentalis Kitagawa, which belongs to the Araliaceae and is distributed in Korea, Japan, Manchuria, China and Sahalane. It is generally used as a folk medicine for its excellent medical action and efficacy in various symptoms such as headache, edema, inflammation, rheumatism and neuralgia. (-)-Pimara-8(14)-15-dien-19-oic acid (1) and l-kaur-16-en-19-oic acid have been reported as the major constituent of A. continental is Radix. Essential oils such as limonene, sabinene, myrcene, humulene and sesamin,${\beta}$ -sitosterol are also reported as constituent elements. (omitted) -
Yoo, Hye-Hyun;Baek, Seung-Hoon;Park, Yun-Kyung;Lee, Seung-Ho;Kim, Chang-Min;Lee, Kyung-Soon;Park, Man-Ki;Park, Jeong-Hill 222.3
Codonopsis radix, a root of Codonopsis lanceolata (S. et Z.) Trautv., is a source of the traditional medicine and health foods. However quality control method is not established yet. This research is to establish the standard for the quality control of Codonopsis radix. From the root of this plant, 1,2,3,4-tetrahydro-${\beta}$ -carboline -3-carboxylic acid (1) was isolated. This alkaloid was adequate as a marker compound for quality control, since it is a unique constituent of Codonopsis radix. In particular, (1) was not found in Adenophorae radix, a common adulterants of Codonopsis radix. (omitted) -
D-Amygdalin and its conversion product, neoamygdalin, were clearly separated on reverse-phase column chromatography by an optimized eluent of 10 mM sodium phosphate buffer (pH 3.5) containing 8.5% acetonitrile. Linearity for analyzing D-amygdalin and neoamygdalin was observed in the range from 0.05 to 0.5 mM. The detection limits for D-amygdalin and neoamygdalin were ca. 5 uM per injected amount. When extracting amygdalin from a whole piece of Armeniacae Semen in the boiling aqueous solution, there was almost no influence of emulsin; it resulted in higher extraction yield. (omitted)
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Lee, Hye-Won;Ji, Hye-Young;Kim, Hui-Hyun;Kim, Sook-Jin;Kim, Soon-Hoe;Kim, Won-Bae;Lee, Hye-Suk 223.2
A rapid, sensitive and selective liquid chromatography-tandem mass spectrometric (LC/MS/MS) method for the determination of eupatilin in human plasma was developed. Eupatilin and internal standard, (S)-[N-3-(4-(2-(1-methyl-5-tetrazolyl)-pyridine-5-y1)- 3-fluorophenyl)-2-oxo-5-oxazolidinyl]methyl acetamide (DA-7867) were extracted from human plasma by liquid-liquid extraction and analyzed on a phenyl-hexyl column with the mobile phase of acetonitrile-ammonium formate (10 mM, pH 3.0) (60:40, v/v). (omitted) -
Chiral discrimination of ibuprofen by
$^1$ H-NMR using several chiral solvating agents such as (-)-brucine, (-)-cinchonidine, (1R, 2S)-(-)-ephedrine, (S)-(-)-${\alpha}$ - methylbenzylamine, (-)-strychnine and L-(-)-tryptophane was investigated. Racemic ibuprofen treated with one equivalent of chiral solvating agent was preferentially crystallized. Chiral purity of each precipitates was measured by chiral HPLC and chemical shift differences(ΔΔ$\delta$ ) was calculated. Eventhough (S)-(-)-${\alpha}$ -methylbenzylamine was most effective for the preferential recrystalization of (S)-(+)-ibuprofen, chemical shift differentiation ability was weak. (omitted) -
A sensitive and selective liquid chromatographic method coupled with tandem mass spectrometry (LC-MS/MS) was developed for the determination of beraprost in human plasma. Plasma samples were transferred into 96-well OASIS HLB extraction plate using an automated sample handling system and the drugs were eluted with methanol. The eluents were then evaporated and reconstituted with water. All sample transfer and solid-phase extraction (SPE) was automated through the application of both the PerkinElmer MultiPROBE II HT and TOMTEC Quadra 96 workstation. (omitted)
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Pyrethroic acids are essential chiral intermediates of the pyrethroids, which account for about 25% of the world insecticide market and are found to be some of the most effective commercially available pesticides. It was demonstrated that polysaccharide-derived chiral stationary phases (CSPs) are very efficient for the separation of the enantiomers of pyrethroid acids. It was observed that the enantioseparation of pyrethroic methyl ester and ethyl derivatives was well accomplished on brush-type WhelkO-1. (omitted)
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Kim, Hee-Kyu;Kim, Jong-Seok;Yang, Sung-Woon;Choi, Han-Gon;Yong, Chul-Soon;Choi, Young-Wook 224.3
Purpose. To investigate the effect of different terpene enhancers on skin penetrations of prostaglandin El (PGE1) and its ethyl ester (PGE1-EE), a therapeutic agent for erectile dysfunction, external gel systems were formulated with the specific enhancers having different values in their lipophilicity (log P was ranged in 2.23-4.58). Methods. Topical gels containing PGEl (0.5 %) and PGEl-EE (0.1 %) were formulated with ethanol and propylene glycol as a vehicle, selective terpenes as a penetration enhancer, and HPC-H as a thickening agent. (omitted) -
Purpose. Paclitaxel has demonstrated significant activity in clinical trials against a wide variety of tumors. The clinical application of Taxol
$\^$ \ulcorner/, a commercial product of solubilized paclitaxel with co solvents of ethanol and Cremophor, however, has been limited largely by hypersensitivity of the excipient. The aim of this study was to formulate paclitaxel-loaded lipid nanodispersions (Px-LN) for i.v. administration without toxic excipients, and to evaluate in vitro characteristics and in vivo pharmacokinetic behaviors. (omitted) -
Choi, Woo-Sik;Kim, Hyun-Il;Kwak, Seong-Shin;Choi, Hee-Kyu;Ha, Jong-Hak;Hwang, Sun-Hwan;Lee, Dong-Beom 225.2
The prolonged mechanical grinding process may enhance the bioavailability of the drugs due to the change of solid state such as micronization and decrease of crystallinity. A series of attempts to enhance the bioavailability of insoluble drugs have been made by the fine grinding technique using a planetary mill. The objective of the present study is to investigate the possibility of improving the dissolution properties of poorly water- soluble drugs such as diphenyl hydrantoin (phenytoin) and diphenyl dimethyl dicarboxylate (DDB) based on the molecular interaction between drug and additives during pharmaceutical processing to be related with the bioavailability behavior. (omitted) -
The available period of oral pharmaceutical liquid preparations was decided according to the study of the stability of unopened preparations. But if one reuses the drug after opening the sealed cap, the major components of the drug could change in quality. In addition, there isn`t any accurate information about the available period of opened oral pharmaceutical liquid preparations. In this study, a long term test, an accelerated test and a microbial limit test are run with C (pseudoephedrine and triprolidine), D (ibuprofen) that are marketed and used frequently. (omitted)
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Chung , Ji-Eun;Lee, Jue-Yeon;Kim, Kyung-Hwa;Baek, Hyun-Jin;Ku , Young;Chung, Chong-Pyung;Lee, Seung-Jin 226.2
.The healing of a bone defect is complex, and involves a wide range of cellular, molecular, physiological, and biological processes. The main effect of bone substitute is to promote wound healing by induce cell proliferation. Bone defect sites usually are localized below the original bone surface; therefore, space production and maintenance between the membrane and the original bone surface is essential. As a result, membranes must have proper mechanical strength to prevent the collapse of the soft tissue and maintain wound space that permits membranes of poly (L-lactide) (PLLA) were fabricated to provide and maintain sufficient space for bone growth. (omitted) -
Chae, Min-Jung;Chung , Hes-Son;Kwon, Ick-Chan;Chung, Jin-Wook;Park, Jae-Hyung;Sohn, Young-Taek;Jeong, Seo-Young 226.3
A cationic lipid emulsion (o/w) containing lipiodol and 1, 2-dioleoyl-sn- glycero-3-trimethylammonium-propane (DOTAP) has been prepared as a gene delivery system. In order to increase the transfection efficiency of the lipiodol emulsion, 1 2-dioleoyl-sn-glycero-3-phospho-ethanolamine (DOPE) and polyoxyethylene sorbitan monooleate (Tween 80) were incorporated as additional lipids. By including DOPE and Tween 80, the cationic emulsion became a more potent gene carrier under in vitro condition in the presence of serum, and under in vivo condition. (omitted) -
Acetyl-L-carnitine (ALC), an endogenous component of L-Carnitine, is the acetyl ester of carnitine that has been reported to be beneficial in depressive disorders and Alzheimer's disease.ALC is so hygroscopic that deliquescence took place when it absorbed moisture by 15%(w/w) in a week and then reached steady-state at 45%(w/w) in 40
$^{\circ}C$ , 75% RH storage condition. Therefore it is necessary to prevent ALC from absorbing atmospheric moisture. For this purpose, we chose hydroxypropylmethylcellulose phthalate (HPMCP) an enteric polymer, as a film former. (omitted) -
In many biodegradable polymers recently investigated, poly(lactic acid)(PLA) or poly(lactic-co-glycolic acid)(PLGA) have extensively been utilized as drug delivery systems for sustained release drug delivery. Recently, there has been increased interest in electrospinning, which can produce fibers that are sub-micron in diameter. This technique has been applied to various micro/nano fabrication areas using numerous polymers but very few uses in the sharmaceutical area have been reported. (omitted)
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Purpose. The purpose of this study is to compare in vitro dissolution characteristics and bioavailability in beagle dog of a hard gelatine capsule containing erdosteine (Yuhan Erdosteine capsule
$\^$ TM/) with those of commercial product (Erdos capsule$\^$ TM/). Methods. Yuhan Erdosteine capsule$\^$ TM/ was prepared using erdosteine 300 mg, lactose, magnesium stearate, and others by powder filling method. The dissolution characteristics of Yuhan Erdosteine capsule$\^$ TM/ and Erdos capsule$\^$ TM/ were determined by USP dissolution apparatus 2. (omitted) -
Investigation of polymorphism has become a requirement in the pharmaceutical industry because the physical properties and bioavailabilities of crystalline drugs depend on their polymorphic form. Two polymorphic modifications and one pseudopolymorphic modification of cefotaxime sodium were prepared by recrystallization in organic solvents under variable conditions. Four polymorphic modifications of cephardine were prepared by recrystallization. Three polymorphic modifications and one pseudopolymorphic modification of ceftriaxone sodium were prepared by recrystallization. (omitted)
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Baek, Hyon-Jin;Kim, Kyung-Hwa;Jung, Ji-Eun;Lee, Ju-Yeon;Ku, young;Chung, Chong-Pyung;Lee, Seung-Jin 229.1
Recently, the barrier membranes have been applied for regenerating bone surrounding peri-implant defects in guided bone regeneration(GBR). GBR membrane should provide mechanical support sufficient to withstand in vivo forces and maintain wound space for bone regeneration. The ability to exclude unwanted tissues of cells(connective tissue and epithelium) is needed. In addition large surface area is conductive to tissue ingrowth. The search for ideal materials that biocompatible, bioresorbable and can support the growth and phenotypic expression of osteoblasts is a major challenge in the biomedical application for the repair of bone defects. (omitted) -
Lee, Myung-Hee;Shim, In-Kyong;Hwang, Jung-Hyo;Ahn, Hyun-Jung;Lee, Sang-Hoon;Lee, Myung-Chul;Lee, Seung-Jin 229.2
Extracellular matrix(ECM) is composed of the ground materials(proteoglycan) and nano size diameter fibrous proteins(ex. collagens) that together form a composite-like structure. In this study, fibrous scaffold with biomimetic architecture based on collagen nanofibers interpenetrated in PLGA/chitosan microfibrous matrix. Chitosan was selected for its structure similarity to glycosaminoglycan and neutralizing capacity for PLGA acidic metabolite. Collagen nanofiber were prepared by electrospinning. (omitted) -
In case of oral application of quinupramine, antidepressants, it may cause adverse effects such as diarrhea, nausea due to transient high blood concentration. Ethylene vinyl acetate (EVA) which is heat-processible, flexible, inexpensive material was used for transdermal drug delivery. The purpose of this study was to develop the new transdermal delivery system of quinupramine using EVA polymer matrix that can provide sustained release and avoid the side effects. The EVA matrix containing quinupramine was prepared by solvent-evaporation method. (omitted)
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Erdosteine, an expectorant, has been known to show a very poor flowability. Furthermore, high dosing amount (300mg/cap) and bulk density make it more difficult to fill in a capsule less than No. 0 size as bulk state. We have studied the possibility of dry granulation process in purpose of getting a better flowability and manufacturing efficiency. A roller compactor was introduced for this purpose and the applicability of laboratory result into commercial scale instrument was also experimented.Roller compacting process was very favorable to obtain the granules with good flowability and improved density profiles. (omitted)
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The therapeutic use of protein pharmaceuticals produced by recombinant DNA technology is increasing in recent decades. In order to investigate the quality of recombinant proteins, it is important to identify and assign the impurities produced in the process of recombination or in storage conditions. Capillary Electrophoresis is emerging technology exhibiting high sensitivity, selectivity and speed and may be most powerful tools for this application. In this study, human growth hormone (hGH) has been analyzed by various mode of capillary electrophoresis such as capillary zone electrophoresis (CZE), capillary gel electrophoresis (CGE), and capillary isoelectric focusing (cIEF) to indicate the chemically or biologically oriented variants and the degraded fragments. (omitted)
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Mucoadhesive microsphere was prepared by interpo]ymer complexation of po]y(acrylic acid) (PAA) with po]y(vinyl pyrrolidone) (PVP) using solvent diffusion method. The loading efficiency of acetaminophen into the microsphere was 91.3
${\pm}$ 6.5%. The release rate of acetaminophen from the PAA/PVP complex microspheres was slower than that from PVP microspheres at pH 2.0 and 6.8. The dissolution of microspheres made of the complex was significantly slower than those made of PVP due to H-bond between PVP and PAA. As a result, the release rate of acetaminophen from the complex microspheres was slower than that from PVP microspheres. -
One of the possible mechanisms of multi-drug resistance found in cancer cells is the over-expression of P-glycoprotein (P-gp). Studies have shown that compounds found in plants including vegetables and fruits not only have anticancer activities but may also modulate P-gp activity. The effect of flavonoids and organic isothiocyanates on P-gp activity was studied in human uterine sarcoma cell lines, MES-Sa (sensitive) and MES-SD/DX5 (resistant). The accumulation of daunomycin (DNM), a P-gp substrate, was approximately 10 times greater in the sensitive cell as compared to the resistant cells over the entire time course (up to 2 hrs). (omitted)
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Hwang, Jeong-Hyo;Lee, Jue-Yeon;Kim, Sun-Chul;Jang, Jun-Hyeog;Ku , Young;Chung, Chong-Pyoung;Lee, Seung-Jin 231.3
The biomedical applications of chitosan have been widely researched. FN mediates its biological effects through binding to the hetero-dimeric transmembrane glycoproteins, integrins, which physically couple the cytoskeleton to the ECM. FN binds to the integrin through a consensus site including the Arg-Gly-Asp (RGD) sequence within tenth type III module (Ruoslahti & Pierschbacher 1987). A short sequence Pro-His-Ser-Arg-Asn (PHSRN) has also been identified as a synergistic motif within ninth type III module for binding to${\alpha}$ 5${\beta}$ 1 integrin (Aota et al. 1994). (omitted) -
Purpose. To develop a hard gelatine capsule containing meloxicam (Yuhan Meloxam capsule
$\^$ TM/), in vitro dissolution characteristics and bioavailability in beagle dog were compared with commercial product (Mobic capsule$\^$ TM/). Methods. Meloxicam capsule$\^$ TM/ was prepared by powder filling method using meloxicam, lactose, magnesium stearate, and others. The release of Meloxicam capsule$\^$ TM/ and Mobic capsule$\^$ Tm/ were monitored by USP dissolution method under various dissolution donditions - dissolution medium (pH 1.2, 4.0, 6.8 and water). (omitted) -
Transdermal iontophoresis is a physical enhancement technique to facilitate the delivery of primarily charged molecules across the skin. Principal mechanism of iontophoresis is electrorepulsion experienced by the charged solutes under the application of a potential gradient. In this work, we have investigated several factors (concentration of NADPH, current density) that can affect the iontophoretic flux. We also studied the stability of NADPH in aqueous solution with/without various antioxidants such as butylated hydroxy toluene (BHT). (omitted)
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The available period of oral pharmaceutical liquid preparations was decided according to the study of the stability of unopened preparations. But if one reuses the drug after opening the sealed cap, the major components of the drug could change in quality. In addition, there isn`t any accurate information about the available period of opened oral pharmaceutical liquid preparations. In this study, a long term test, an accelerated test and a microbial limit test are run with A (acetaminophen), B (L-carbocysteine) that are markdted and used frequently. (omitted)
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Kim, Young-Ock;An , Deuk-Kyun;Lee, Hyun-Sun;Lee, Young-Ah;Kim, Yang-On;Song, Chang-Woo;Kim, Yang-Eon;Song, Chang-Woo 233.2
This experiment study was carried out to prove the efficacy of Cheongpajeon(CPJ) extract in ovariectomized rats. 40 rats were divided into 4 groups, administrated saline after sham operation group(sham-op), administered saline after ovariectomy group(control), administered CPJ 1g/kg after ovariectomy group and administered Livial 0.042mg/kg after ovariectomy group(positive control). We examined the water extract of CPJ that is capable of affecting osteoblast proliferation using MG-63 and HOS-TE85. (omitted) -
Electroosmotic flux during iontophoresis originates due to the net negative charge of the current passing channel (pores) in skin at physiological pH (pH 7.4). Thus, the channel is permselective to cations, and this causes the convective solvent flow, from anode to cathode direction. This solvent flow facilitates the flux of cations (from anode), inhibits that of anions (from cathode), and enables the enhanced transport of neutral, polar solutes. In this work, we have investigated the effect of a series of polyethylene glycols (PEGs) with different molecular weights on the electroosmtic flow to get more detail understanding of this phenomena. (omitted)
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The effects of vehicles and penetration enhancers on the in vitro permeation of ketorolac tromethamine (KT) across excised hairless mouse skins were investigated. Among pure vehicles examined, propylene glycol monolaurate (PGML) showed the highest permeation flux, which was 94.3
${\pm}$ 17.3 mg/cm$^2$ /hr. Even though propylene glycol monocaprylate (PGMC) alone did not show high permeation rate, the skin permeability of DT was markedly increased by the addition of diethylene glycol monoethyl ether (DGME); the enhancement factors were 19.0 and 17.1 at 20 and 40% of DGME, respectively. (omitted) -
Recently, the need for ultra-fine particles, especially nano-sized particles has increased in the fields preparing raw powders such as pharmaceutical additive and high value added products in the Nano-Technology processes. Therefore, the research in ultra-fine grinding is very important, especially, in nanometer grinding. In the previous paper, a series of wet grinding experiments using grinding aids using a stirred ball mill have been performed on grinding rate constant based on grinding kinetics. (omitted)
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The aim of this study is to evaluate the permeability of PEG-conjugated salmon calcitonin (sCT) across monolayers of Caco-2 cells that represent a model of the intestinal barrier. Caco-2 cells were grown to confluency on a permeable polycarbonate membrane to permit transport through it. Permeability experiments were performed with native-sCT and PEG-conjugated sCT (PEG M.W. 2000) at various concentrations (5uM, 10uM, 25uM, 50uM, 100uM) in the apical to basolateral direction. The barrier properties were assessed by detecting transport of markder molecules (
$^3$ H-mannitol) and by measuring transepithelial electrical resistance (TEER). (omitted) -
Yook , Yeo-Joo;Hwang, Jeong-Hyo;Shim, In-Kyung;Lee, Jue-Yeon;Lee, Sang-Young;Ahn, Hyun-Jeong;Lee, Sang-Hoon;Lee, Myung-Chul;Lee, Seung-Jin 235.1
With an aim of obtaining high efficacy in cartilage regeneration, implantable polymeric rods were fabricated. These rod-type matrices were anticipated to perform structural tissue supporting activity and enhance extracellular matrix (ECM) formation by releasing specific agent, DHEA-S, in controlled manner. It is expected that application for the drilling operation on the articular cartilage of OA patients as the implants may promote regeneration of their cartilage. Osteoarthritis (OA) is a degenerative joint disease characterized by progressive loss of articular cartilage, subchondral bone remodeling, spur formation, and synovial inflammation. (omitted) -
To develop the buccal delivery system of rhEGF for the treatment of buccal mucosal ulcer, polymer films and hydrogels were investigated. Methods: Hydrogels for thermosenstive sol/gel systems were prepared by the cold method (Schmolka, 1972). And mucoadhesive films were prepared by mixing sod. alginate/polycarbophil 974p. To find an optimum buccal mucosal adhesive gel or film, the gel strength of the poloxamer and sod. alginate/polycarbophil 974p hydrogels were determined by the Simple Rheology Method and their mucoadhesiveness were measured by the Instron (M 4400, Instron Co., U.S.A.) method. (omitted)
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Evaluation of solid surface properties is very important for formulation of solid dosage form, specially insoluble drugs. The contact angle of insoluble drugs was measured by the penetration rate into powder bed using Washburn equation and wicking method. From the measured contact angle data, the surface free energy value of pharmaceutical powders
${\gamma}$ s was divided and analysized into the polar component,${\gamma}$ s$\^$ p/ and the dispersion component,${\gamma}$ s$\^$ d/. Furthermore, the data was interpreted for acid part,${\gamma}$ s$\^$ +/ and base part,${\gamma}$ s$\^$ $\square$ / of surface free energy. (omitted) -
Skin Permeation and Crosslinking of a Biological Tissue with Hydrolyzed Product of Gardeniae FructusFor the purpose to treatment of skin disease genipoiside and hydrolyzed product of Gardeniae Fructus were studied on skin permeation and crosslinking of a biologied tissue. Geniposide was hydrolyzed to genipin by
${\beta}$ -glucosidase and the rate of hydrolysis was rapid on the condition of high temperature of medium and high concentration of${\beta}$ -glucosidase. The permeation enhancing effects of geniposide and genipin under cream and gel preparations were tested using Franz type diffusion cell and the skin of hairless mouse. (omitted) -
Fine particles of water-soluble pharmaceuticals were prepared using a new micronization method, Carbon Dioxide Assisted Nebulization in a Bubble Dryer(CAN-BD). The process utilized mixtures of CO
$_2$ in aqueous solution at supercritical conditions to form an emulsion. The aerosols were dried with pre-heated nitrogen, and the drying chamber was operated at near atmospheric pressure. The dry particles were collected on membrane filter at the bottom of the drying chamber. Several processing parameters such as flow rate, temperature, pressure, solid concentration and processing scale were accessed using NaCl, human serum albumin, and granulocyte-colony stimulating factor as model pharmaceuticals. (omitted) -
Cefuroxime axetil, a broad spectrum antibiotic, has been known to form a gelatinous mass in contact with aqueous media, which could lead to poor dissolution. Therefore, this study was conducted for removing the gelling phenomenon and thereby obtaining a favorable dissolution profile. We have found that the addition of poly (methacrylic acid, methyl methacrylate) could not only inhibit the tendency of cefuroxime axetil to form a gel but also showed the good dissolution profile compared to the formula without poly (methacrylic acid, methyl methacrylate). (omitted)
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DWP40458 is a novel human thrombopoietin mutein with two additional N-linked glycosylation site. The thermal stability of DWP40458 in both solution and lyophilized form was studied in the temperature range of 4-50
$^{\circ}C$ , compared with recombinant human TPO (rhTPO). When the aggregation or degradation pattern of DWP40458 and rhTPO solution was characterized by using SDS-PAGE, gel permeation chromatography (GPC) and reverse phase HPLC, it was found that thermostability of DWP40458 was significantly different to rhTPO in the temperature at 25, 40, 40, 50$^{\circ}C$ . (omitted) -
Shim, In-Kyong;Hwang, Jung-Hyo;Lee, Sang-Young;Cho, Hyun-Chul;Lee, Myung-Chul;Lee, Seung-Jin 237.3
Tissue engineering may be adequately defined as the science of persuading the body to regenerate or repair tissue that fail to regenerate or heal spontaneously. In the various techniques of cartilage tissue engineering, the use of 3-dimensional polymeric scaffolds implanted at a tissue defect site is usually involved. These scaffolds provided a framework for cells to attach, proliferate, and form extracellular matrix(ECM). The scaffolds may also serve as carriers for cells and/or growth factors. In the ideal case, scaffold absorb at a predefined rate so that the 3-dimensional space occupied by the initial scaffold is replaced by regenerated host tissue. (omitted) -
Hyun, Jung-Seung;Kim, Jeong-Ran;Na, Chun-Soo;Choi, Bum-Rak;Yoon, Sun-Young;Park, Young-In;Dong, Mi-Sook 238.1
Hepatic stellate cells (HSC) and the derived myofibroblasts are known to play a central role in liver fibrogenesis. Rhus verniciflua Strokes (RVS) has traditionally been used in Korea herbal medicine for a stomachic tonic. In this study, we observed the effect of RVS acetone extract (Ra) and its five major components on the proliferation, the collagen synthesis, and hepatic fibrosis related proteins mRNA levels in HSC-T6 cells which is a fully activated rat hepatic stellate cell line. Ra inhibited the proliferation and decreased the content of collagen in the HSC-T6 cells. (omitted) -
The purposes of this study were to evaluate the relationship between the genetic polymorphisms in CYP2D6*10 allele, MDR1 (exon 21 and 26) gene and risperidone pharmacokinetics in healthy male Korean subjects. A single dose of 2 mg risperidone tablet was given orally to 23 healthy male Korean volunteers. Blood samples were taken during the 12 hours after the dose. Serum concentrations of risperidone and 9-hydroxyrisperidone were measured using HPLC with UV detector. 23 subjects were genotyped for CYP2D6*10 allele, MDR1 G2677 T and C3435T by polymerase chain reaction-restriction fragment length polymorphism(PCR-RFLP). (omitted)
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This study was to develop a quantification method of lisinopril using liquid chromatography tendem mass spectrometry in human plasma. Quntitation of lisinopril by MRM(multiple reaction monitoring) in the electrospray positive mode was validated according to FDA guideline. Extraction of lisinopril and enalapril as internal standard from plasma was perfomed by means solide phase extraction. The calibration curve of lisinopril showed a good linerarity in the concentration range 2∼200ng/ml. The coefficients of variations for the inter-day and intra-day precision was less than 15%, and the inter-day and intra-day accuracy was 97.6∼101.0%. (omitted)
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The purpose of this study was to evaluate the predictability of the fraction of drug absorbed in humans using the immobilized artificial membrane phosphatidylcholine column (IAMPC) under optimized conditions in comparison with a conventional IAMPC method. Twenty commercial drugs, both acidic and basic in nature, were used in the study, Drugs were dissolved in acetonitrile:water (50:50, v/v) at a concentration of 100 mg/ml, and were injected on HPLC/UVD at a mobile phase (acetonitrile:DPBS = 10:90,v/v) with a flow rate of 0.5 ml/min equilibrated at 37
$^{\circ}C$ . (omitted) -
The purpose of this study was to investigate the effect of nifedipine (10 mg/kg) on the pharmacokinetic parameters and the bioavailability of paclitaxel (50 mg/kg) orally coadministered and pretreated in rats. The plasma concentration of paclitaxel in combination with nifedipine was significantly (p<0.05 at 10 mg/kg coadmin., p<0.01 at pretreat.) increased compared to that of control, from 2 hr to 24 hr. Area under the plasma concentration-time curve (AUC) of paclitaxel with nifedipine was significantly (p<0.05 at 10 mg/kg coadmin., p<0.01 at pretreat.) higher than that of control (omitted)
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We aimed at determining bioavailability of procainarnide HCl, an antiarrhythmic drug, and developing a simple analysis in human blood using HPLC. A rapid and sensitive HPLC method was developed and validated using reverse-phase C18 column with retension time and limit of quantification of procainamide HCl being 2.58 min and 50ng/ml, respectively. Quantification was performed at 275 nm with caffeine as internal standard. The method involved a simple extraction. In order to study blood level profile in time, eight volunteers were enrolled and orally took 250 mg procainamide HCl once. (omitted)
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The purpose of this trial was to determine pharmacokinetic parameters and to characterize bioavailability of levosulpiride after oral administration in Korean healthy male volunteers. Thirty subjects were received a single oral dose of a tablet (Isomeric
$\^$ \ulcorner/) containing 25 mg of levosulpiride. The plasma concentrations of levosulpiride were measured by a validated FLD-HPLC method and compared with those reported in the literature. Levosulpride was absorbed slowly, revealing peak concentrations between 4 and 6 hr after oral administration. (omitted) -
Noh, Hyun-Jung;Kim, Il-Hwan;Choi, Jae-Mook;Kim, Deog-Yeor;Park, Jie-Eun;Choi, Kwang-Do;Yeon, Kyu-Jeong;Lee, Sung-Hak;Kim, Taek-Rho 241.1
Purpose: The objective of the study was to elucidate the pharmacokinetics of CJ-11555, anti-cirrhotic agent, in different physical properties and vehicles. Methods: 8-week-old male intact rats were administered CJ-11555 either intravenously (20 mg/0.6 mL/kg, NMP:PEG400, 1:1) or orally (50 mg/2 mL/kg, various vehicles). Different particle sizes of CJ-11668 and various vehicles were applied to characterize CJ-11555 in vivo. Following the administration in rats, the plasma concentrations were determined by HPLC. (omitted) -
The purpose of this study was to investigate the effect of quercetin(2.0, 10, 20 mg/kg; combined or pretreated) on the pharmacokinetic parameters and the bioavailability of diltiazem(15mg/kg) orally to rabbits. The plasma concentration of diltiazem pretreated with quercetin(pretreated group) were increased significantly (p<0.01) compared to that of control, but those of diltiazem combined with quercetin(combined group) were not affected. Area under the plasma concentration-time curve (AUC) of diltiazem pretreated with quercetin was significantly ( p<0.01) higher than that of control (omitted)
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Kim, Hye-Jung;Bae, Sung-Seok;Myung, Seung-Woon;Ryu, Jae-Chun;Chung, Youn-Bok;Kwon, Oh-Seung 241.3
A simple, specific and sensitive method for the determination of methyltestosterone (MT) in human serum has been developed by gas chromatography/mass spectrometry with the purpose of conducting pharmacokinetic and bioequivalence studies of MT. This method involves the use of liquid-liquid extraction with diethyl ether and derivatization with MSTFA, using 1 ml of serum obtained from volunteers orally taken 50 mg MT. MT showed good resolutions in this conditions and no significant interfering peaks were observed. (omitted) -
The bioequivalence of two tablet formulations of 12.72 mg domperidone maleate (Shinpoong "
$\textrm{Dompi}^{?}$ " tablets vs. Janssen Korea "$\textrm{Dompi}^{?}$ " tablets) was assessed in healthy Korean volunteers after oral administration in a randomized crossover study. Blood samples were collected at specified time intervals, and plasma concentration was measured as the amount of domperidone base using a validated HPLC method. The pharmacokinetic parameters of$AUC_{0{\longrightarrow}48}$ ,$C_{max}$ ,$T_{max}$ $t\frac{1}{2}$ were determined from plasma concentration-time profile of two formulations. (omitted) -
Ha, Yong-Hwa;Cho, Sung-Hee;Hong, Sung-Je;Lee, Heon-Woo;Seo, Seong-Hoon;Rew, Jae-Hwan;Lee, Kyung-Tae 242.2
The purpose of the present study was to evaluate the bioequivalence of two Erdosteine capsules,$Erdos^{TM}$ (Dae Woong Pharmaceutical Co., Ltd.) and$Ersteine^{TM}$ (Dae Won Pharmaceutical Co., Ltd.), according to the guidelines of Korea Food and Drug Administration (KFDA). Twenty-four normal male volunteers,23.88${\pm}$ 2.89 year in age and 68.50${\pm}$ 7.71 kg in body weight, were divided into two groups and radkomied 2${\times}$ 2 cross-over study was empolyed. Ater three capsules containing 300 mg of erdosteine per capsule were orally administered, blood was taken at predetermined time intervals and concentrations of erdostene I in plasma were determined using HPLC. (omitted) -
The compound of 2"-O-benzoylcinnamaldehyde(CB-ph) is a derivative of 2"-hydroxycinnamaldehyde whcih is a methanol extract of cinnamomum cassia blume. It"s a new anti-cancer agent which has been showed to inhibit the growth of various tumor cells in vitro and in vivo. In order to investigate the effective drug concentration and bio-distribution of CB-ph, the plasma protein binding was studied. In this study, the degree of the binding of Cb-ph to various serum proteins, the binding parameters, the binding site of CB-ph in human serum albumin, and the effect of some extensive protein-binding drugs on the protein binding of CB-ph in human serum ablumin were investigated respectively by ultrafilteration and fluorescence spectrometry. (omitted)
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Jang, Ji-Myun;Park, Kyung-Jin;Kim, Dong-Goo;Shim, Hyun-Joo;Ahn, Byung-Ok;Kim, Soon-Hoe;Kim, Won-Bae 243.1
The pharmacokinetics of eupatilin (an active components of Stillen, a new antigastritic agent) were investigated using UV-HPLC method. The quantitation limit of eupatilin was 10 ng/ml in plasma. After intravenous administration of eupatiln, 30 mg/kg to rats, the plasma concentrations of unchanged eupatilin declined rapidly with the mean terminal half-life of 0.101 hr. Total body clearance was 121 ml/min/kg, and fractions of dose excreted in urine and feces for 24 hr were only 2.5% and 0.919%, respectively. (omitted) -
Kim, Il-Hwan;Noh, Hyun-Jung;Park, Jae-Mook;Kim, Deog-Yeor;Park, Jie-Eun;Lee, Sung-Hak;Kim, Taek-Rho;Kim, Jin-Wan;Kim, Young-Hoon 243.2
Purpose: This study evaluated gender differences and extents of accumulation on chronic dose of CJ-1l555 using rats. Method: 0, 10, 50 and 200 mg/kg/day of CJ-11555 (0.5% CMC) were orally administered to rats for 28 days and observed toxicokinetic parameters. Plasma concentrations were analyzed by LC-MS/MS Result: Exposure to CJ-11555 increased with the increase in dose level for both sexes. Mean concentrations at 10 and 50 mg/kg/day were generally similar an Days 1 and 28, but were generally highter on Day 28 than on Day 1 at 200 mg/kg/day. (omitted) -
We aimed at determining bioavailability of clonazepam, an anxiolytic drug, and developing a simple analysis in human blood using HPLC. A rapid and sensitive HPLC method was developed and validated using reverse-phase C18 column with retension time and limit of quantification of clonazepam being 2.58 min and 5hg/ml, respectively. Quantification was performed at 235 nm with p-hydroxybenzoic acid ethyl ester as internal standard. The method involved a simple extraction. In order to study blood level profile in time, sight volunteers were enrolled and orally took 6 mg clonazepam once. (omitted)
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The objective of this study was to characterize the absorption and pharmacokinetic disposition of novel cyclic tetrapeptide, apicidin, in rats. Apicidin was administered to SD rats by i.v. bolus injection (1,2 or 4 mg/kg) and oral gavages (10 mg/kg). Serum levels of apicidin were monitored by LC/MS over 8 hours following each administration. Upon i.v. injection, serum levels of apicidin were best fit by a multi-exponential equation. The t
$\frac{1}{2}$ . Cl$\sub$ s/ and V$\sub$ ss/ ranged from 0.9-1.1 hr, 52.8-56.5 ml/min/kg, and 2.6-2.7 L/kg, respectively. (omitted) -
Cho, Sung-Hee;Ha, Yong-Hwa;Hong, Sung-Je;Seo, Seong-Hoon;Rew, Jae-Hwan;Kim, Dong-Hyun;Lee, Kyung-Tae 244.3
ABSTRACT-The purpose of the present study was to evaluate the bioequivalence of two enalapril maleate tablest,$Renitec^{TM}$ (MSD Korea Ltd.) and$Enalace^{TM}$ (Welfide Korea Ltd.), according to the guidelines of Korea Food and Drug Administration (DFDA). Twenty-four normal male volunteers, 22.33${\pm}$ 2.55 year in age and 66.54${\pm}$ 8.30 kg in body weight, were divided into two groups and a randomized 2${\times}$ 2 cross-over study was employed. After two tablets containing 10 mg of enalapril maleate per tablet were orally administered, blood was taken at predetermined time intervals and concentrations of enalapril in plasma were determined using LC-MS-MS. (omitted) -
Park, Kyung-Jin;Ahn, Gook-Jun;Kim, Dong-Hwan;Shim, Hyun-Joo;Ahn, Byung-Ok;Kim, Soon-Hoe;Kim, Won-Bae 245.1
DA-8159 is a new PDEV (Phosphodiesterase V) inhibitor, synthesized by Dong-A Pharm., as an oral agent to treat male erectile dysfunction. To make a selection of the dosage of oral administration in carcinogenic studies, we studied preliminarily the pharmacokinetics of DA-8159 after single (at the 1$\^$ st/ day) and 1-week (at the 7$\^$ th/ day) oral administrations of the drug at doses of 15, 50 and 150 mg/kg/day, to male ICR mice. In 15mg/kg single and 1-week repeated oral administration groups, the concentrations of DA-8159 and DA-8164(the main metabolite of DA-8159) were below the limit of quantitation(LOQ:50ng/ml). (omitted) -
A rapid and reproducible high performance liquid chromatographic assay of prazosin in human plasma was developed. After addition of internal standard (IS, terazosin hydrochloride) and alkalization of the plasma, the drug and IS were extracted into t-butylmethylether. The organic phase was back-extracted with 0.05% phosphoric acid and 50
${\mu}$ l of the acid solution was injected into a reverse-phase C18 column with a mobile phase consisting of water: acetonitrile: triethylamine = 75 : 25 : 0.1 (pH 5.0). (omitted) -
The purpose of this study was to investigate the effect of quercetin(2.0, 10, 20 mg/kg; combined or pretreated) on the pharmacokinetic parameters and the bioavailability of paclitaxel(50mg/kg) orally in rats. The plasma concentration of paclitaxel pretreated with quercetin(pretreated group) were increased significantly (p<0.01) compared to that of control, but those of paclitaxel combined with quercetin(combined group) were not affected. Area under the plasma concentration-time curve (AUC) of paclitaxel pretreated with quercetin was significantly (p<0.01) higher than that of control. (omitted)
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Bioequivalence of two enalapril maleate tablets, formulation A and B, was evaluated according to the Korean Guidelines for Bioequivalence Test (KGBT 2001). Twenty healthy male volunteers (19∼27 years old) were randomly divided into two groups and a randomized 2x2 cross-over study was performed. Following oral administration of enalapril maleate tablets (20 mg dose), blood sample was taken at pre-determined time intervals and the concentrations of enalapril in plasma were determined using LC-MS. (omitted)
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Lately, soybeans have received considerable public attention for their potential roles in the prevention of the chronic diseases. Epidemiologic study showed that Asian countries have significant health benefits because of the high contents of the isoflavones in their traditional diets(soybean-rich diet). This study was carried out to determine pharmacokinetic parameters of isoflavone in Korean woman. Pharmacokinetic study of three soy products(isogen, soymilk, and fermented soybean) with different ration of aglycone/glucoside in 26 healthy female volunteers(20-30 years of age) was performed. (omitted)
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Iron deficiency is the most common nutritional problem worldwide. Oral iron supplementation programs have failed because of noncompliance and gastrointestinal toxicity. The purpose of this study was to explore the possibility of alginate gel bead as an oral controlled release system of iron supplements and increase the stability of iron succinyl casein (ISC). Alginate beads containing ISC were prepared by the gelation of sodium alginate with calcium cations. The release profiles of ISC were investigated according to the concentration of polymer, the drug/sodium alginate ratio, the concentration and type of cation, curing time and pH of calcium chloride solution. (omitted)
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To increase skin permeability of LMWH (Low Molecular Weight Heparin), ultradeformable liposomes were developed. Ultradeformable liposomes were developed by Egg phosphatidylcholine (Egg-PC) and edge activator. Entrapment efficiency, vesicle size and zeta potential of vesicles were determined and characterized for deformability and stability. Transepidermal permeation of LMWH was compared to saturated aqueous control in vitro. The steady-state flux and its maximum time were calculated from the flux curves. (omitted)
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Keloids are characterized by abnormal proliferation of fibroblasts and overproduction of collagen. Recently, it is reported that transforming growth factor beta (TGFb) and its signaling molecule, SMAD3 are related to the mitogenic effect of fibroblasts and a stimulatory factor for collagen synthesis. Cationic SLN was developed to improve the complex formation of DNA/SLN and enhance the uptake efficiency to cells. SLN was formulated by DC-Chol, DOPE, trimyristin as a solid core and other surfactant. The physical properties of the SLN and the ATS-SLN complex were characterized. (omitted)
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Kim, Bum-Soo;Cho, Due-Hyeon;Koo, Wan-Mo;Kim, Byung-Su;Kim, Ha-Na;Kim, Ki-Don;Park, Jee-Hun;Kim, Ha-Hyung 248.2
A lectin has been purified from the bark of the legume Maackia fauriei. This lectin, MFA, was found to agglutinate human ABO erythrocytes at a titer of 256. The results from electrophoretic analyses, gel-filtration chromatography, and enzyme linked lectinsorbent assay indicate that MFA is an acidic glycoprotein, and exists as a tetramer of 30 kDa subunits that are linked by noncovalent bonds. The activity of MFA is critically dependent upon CaC1$_2$ . MFA demonstrated high homogeneity with the lectins from M. amurensis, which is the only legume source of lectins that bind to sialoglycoconjugate, in its N-terminal amino acid sequence and amino acid composition, (omitted) -
Objectives: Galatosylated PEI was synthesized and characterized for gene delivery to hepatocytes. It was modified by conjugating with hydrophilic PEG to improve in vivo circulation. And we studied the possibility as an imaging modality for monitoring of gene delivery using gal-PEI derivatives. Methods: The substitution values of galactose in PEI were calculated by resorcinol/sulfuric acid method and quantity of PEG was calculated by comparing NMR peak. Cytotoxicity was determined by MTT. (omitted)
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The objective of the study was to develop an oral delivery system to increase the stability and efficacy of iron casein succinylate. Aqueous nanoparticles were prepared using complex coacervation of the oppositely charged chitosan and iron casein succinylate with polyethyleneglycol (PEG). The physicochemical properties of nanoparticles were investigated using dynamic light scattering, zeta potential and scanning electron microscopy. Chitosan-iron casein succinylate interactions were investigated in solid state by differential scanning calorimetry (DSC) and FT-IR spectrometry. (omitted)
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${\beta}$ -blockers are considered as standard therapy for patients with stable chronic heart failure (CHF) and to prolong survival and reduce hospitalizations. We examined the effects of the${\beta}$ -blocker on mortality, hospitalization and symptoms in patients with CHF and the related factors to the use of${\beta}$ -blockers. Patients in New York Heart Association class II-IV were included if they were treated for heart failure from January 2002 to June 2002. At baseline, 6 months, and 12 months, they were assessed for the change of NYHA class and all deaths and hospital admissions. (omitted) -
Background Aldosterone has an important role in the pathophysiology of heart failure. Aldosterone promotes the retention of sodium, the loss of magnesium and potassium, sympathetic activation, parasympathetic inhibition, myocardial and vascular fibrosis, baroreceptor dysfunction, and vascular damage and impairs arterial compliance. Objectives We investigated the effects of additional spironolactone to angiotensin-converting enzyme inhibitor (ACEI) / angiotensin-II receptor blocker (ARB) in patients with heart failure. (omitted)
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There are contradicting reports on the nephrotoxicity of heptaplatin, a new platinum derivative. A retrospective study was performed to compare the toxicities of heptaplatin-containing regimens with the ones not. Seventy-seven patients with advanced gastric cancer who did not receive any chemotherapy within the last 3 months before the treatment were evaluated. Among them 38 patients received heptaplatin-containing regimens (heptaplatin/epirubicin/5-FU: 26, heptaplatin/5-FU: 12) and 39 patients received other regimens (cisplatin/epirubicin/5-FU:11, epirubicin/leucovorin/5-FU: 28). (omitted)