• Title/Summary/Keyword: 약물 농도

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Evaluation on Skin Irritation and Sensitization of Oxyresveratrol and Oxyresveratrol-3-O-glucoside Produced by Biotransformation of Morus alba Extract (상백피 추출물을 효소전환 하여 생성한 oxyresveratrol 및 oxyresveratrol-3-O-glucoside의 피부 자극성 및 감작성 평가)

  • Park, Keun-Tae;Kim, Jeong-Keun;Lim, Young-Hee
    • Korean Journal of Food Science and Technology
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    • v.44 no.2
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    • pp.251-256
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    • 2012
  • Stilbenes are known as antioxidants and some of them demonstrate anti-pigmentation activity. The purpose of the present study was to investigate whether two stilbene compounds produced by biotransformation of the extract of $Morus$ $alba$ root show skin irritation and sensitization. In skin irritation test, 1% oxyresveratrol (OXY), and 5% OXY, and 1% oxyresveratrol-3-$O$-glucoside (OXY-3) showed a P.I.I score of 0, 0.04, and 0, respectively. Accordingly, the two stilbenes were evaluated to be virtually 'non-irritant' materials. In a skin sensitization study by GPMT, 1% OXY, 5% OXY, and 1% OXY-3 did not cause edema and erythema at 24 h and 48 h after topical application and exhibited a sensitization score of 0 and a rate of 0%. Consequently, it was confirmed that OXY and OXY-3 had no contact allergic sensitization in GPMT. Therefore, OXY and OXY-3 might be potential candidates as skin-whitening agents without posing any serious side effects.

Antihyperlipidemic Effect of Ginsenoside Rg1 in Type 2 Diabetic Mice (제2형 당뇨병 모델 마우스에서 ginsenoside Rg1의 항당뇨 효과)

  • Park, Jae-Hong;Lee, Ji-Youn;Yeo, Ji-Young;Nam, Jeong-Su;Jung, Myeong-Ho
    • Journal of Life Science
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    • v.21 no.7
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    • pp.932-938
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    • 2011
  • Ginsenoside Rg1 is a pharmacologically active component isolated from ginseng. The goal of this study was to clarify the beneficial effects of Rg1 on glucose and lipid metabolism in diabetic animals (db/db mice). To accomplish this, ten week old db/db mice were administered 10 mg/kg of Rg1 for 15 days. Rg1 did not influence the weight of db/db mice when compared with vehicle-treated db/db mice. The administration of Rg1 lowered fasting plasma glucose, and improved glucose tolerance. Importantly, Rg1 markedly reduced both plasma triglyceride and free fatty acids, and increased high-density lipoprotein cholesterol (HDL-C) concentrations in db/db mice. Rg1 activated promoter activity of chimeric GAL4-PPAR${\alpha}$ reporter and increased expression of peroxisome proliferator-activated receptor alpha (PPAR${\alpha}$) target genes such as carnitine palmitoyltransferase-1 (CPT-1) and acyl-CoA oxidase (ACO), which are involved in fatty acid oxidation. These findings indicated that improvement of lipid profiles by Rg1 may be associated with increased fatty acid oxidation via PPAR${\alpha}$ activation. Taken together, these results suggest that Rg1 could have beneficial effects for controlling hyperglycemia and hyperlipidemia associated with type 2 diabetes.

Case report : The Bisphosphonate-associated Osteonecrosis of the Jaw(BONJ) (증례 보고: 악골에 발생한 비스포스포네이트 관련 골괴사증 (BONJ))

  • Kim, Kyun-Yo;Ko, Yu-Jung;Hur, Yun-Kyung;Choi, Jae-Kap
    • Journal of Oral Medicine and Pain
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    • v.34 no.3
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    • pp.295-301
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    • 2009
  • Recently, bisphosphonate-associated osteonecrosis of the jaw(BONJ) is added to the list of diseases of the oromaxillofacial region. BONJ is defined as exposed bone in the jaw that does not heal within 8 weeks after identification, in a patient who has been received to bisphosphonates and has not taken radiation therapy to the craniofacial region. Bisphosphonates binded to bone mineral are concentrated in highly active remodeling site, reside in the skeleton for a long time, and do a role as powerful inhibitors of bone resorption. As the patients receiving bisphosphonates therapy grow in number, the patients of BONJ would go on increasing in Korea. We would like to present two patients who were suspected to BONJ, describe the outline of BONJ, and mention importance of our understanding about BONJ. BONJ is rare disease, but once it develops, its prognosis is very poor. Our adequate understanding of BONJ is necessary to prevent it and cope with it properly.

A COMPARATIVE STUDY ON THE VITAL SIGN AND BEHAVIOR APPEARANCE DEPENDING ON THE ROUTE OF FLUMAZENIL ADMINISTRATION IN CONSCIOUS SEDATION BY MIDAZOLAM (Midazolam을 이용한 의식진정시 flumazenil의 투여경로에 따른 생징후 및 행동양상의 비교 연구)

  • Kim, Hyun-Sik;Lee, Chang-Seop;Lee, Sang-Ho
    • Journal of the korean academy of Pediatric Dentistry
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    • v.29 no.2
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    • pp.159-167
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    • 2002
  • The purpose of this study was to evaluate the efficacy and safety depending on the route of flumazenil, as an antagonist against midazolam. The subjects of this study were 15 volunteers of $22{\sim}24$ years old. They were sedated with midazolam 0.2mg/Kg intranasal spray, and then 40 minutes after midazolam administration, they were given flumazenil 0.2mg intranasal spray for their reversal. For evaluation of the efficacy and safety of intranasal spray for flumazenil, they were monitored with pulse-oxymeter(Nellcor symphony N-3000, Nellcor Puritan CO. USA) and electric sphygmomanometer (Heartcare 200, National CO. Japan), and were assessed themselves using visual analogue scale(VAS) for tranquilization, sleep, fatigue and attitude. All of these subjects were reduced completely without any undesired situations. The results from this study can be summarized as follows ; 1. Nasaly administered flumazenil using spray device produced much more rapid reduction than intravenously administered flumazenil, but soon after fell in more deep sedated state than intravenously administered flumazenil. 2. There were no considerable side effects or bad influence on vital signs of both nasaly administered flumazenil and intravenously administered flumazenil. These results suggested that the flumazenil administered nasaly using spray device for reversal, we could treat patients safely and effectively under conscious sedation using midazolam administration. But, We will have to research about its optimal dosages for flumazenil, used as intranasal spray for reversal agents against the midazolam by evaluating the blood plasma concentration of midazolam and flumazenil.

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The Effect of Hair Growth and Distribution by Sophorae Radix, Panax ginseng, Salvia miltiorrhiza BUNGE Water Extracts (고삼, 인삼 및 단삼 혼합물에 의한 모발의 성장과 분포에 미치는 영향)

  • Hwang, Cho-Won;Hwang, Jae-Wan;Kim, Sang-Tae
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.36 no.3
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    • pp.215-219
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    • 2010
  • In this study, we investigated effects of Monegy (mixture of Sophorae Radix, Panax ginseng, Salvia miltiorrhiza BUNGE) on epilate-induced hair-loss in dorsal region of C57/BL6 mice and external structure of human hair. For morphological and histological analysis in scalp of epilate-induced hair-loss animal model, we utilized several microscopic techniques, such as confocal laser scanning microscopy (CLSM) and LAS 4000. Confocal analysis showed the distribution of FITC-conjugated Monegy and penetration depth compared with normal and control group. Furthermore, when Monegy was topically administrated onto a C57BL6 mouse, it penetrated very well. The fluorescence intensity was increased upto 205 and 113 folds compared to normal and control group, respectively. Also, area of fluorescence was increased to upto 255 to 127 folds compared to normal and control group. Broad scale area of fluorescence in dermis region was observed in the Monegy-treated mice. Furthermore, Monegy induced upto 75% hair repair against depilation. It might be promoted via the induction of growth factors in hair follicle.

Effect of Molecular Weight of PLGA on Release Behavior of Doxorubicin for Double-Layered PLGA Microspheres (PLGA 분자량에 따른 이중층 독소루비신 미립구의 방출거동)

  • Park, Jung-Soo;Yang, Jae-Chan;Yuk, Soon-Hong;Shin, Hyung-Shik;Rhee, John-M.;Kim, Moon-Suk;Lee, Hai-Bang;Khang, Gil-Son
    • Polymer(Korea)
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    • v.31 no.3
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    • pp.189-193
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    • 2007
  • We developed the doxorubicin-loaded PLGA double-layered microspheres using relatively simple oil-in-water (O/W) solvent evaporation method for sustained release of doxorubicin and investigated the release behavior according to PLGA molecular weight and initial drug loading. The double-layered microsphere was characterized on the surface, the cross-section morphology, the behavior of doxorubicin release for 5 weeks by SEM and fluorescence spectrophotometer. Double-layered microspheres showed smooth surfaces and clear difference between core and outer-shell. As the PLGA molecular weight increased, the release rate of doxorubicin-loaded, double-layered microspheres decreased. These results showed that the release behaviors can be controlled by the variation of molecular weight of PLGA.

Analysis of Differentially Expressed Genes by Sulindac Sulfide in Human Colorectal Cells (인간 대장암 세포주에서 sulindac sulfide 처리에 의해 차별적으로 발현되는 유전자 군의 분석)

  • Shin, Seung-Hwa;Kim, Jong-Sik
    • Journal of Life Science
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    • v.17 no.7 s.87
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    • pp.996-1001
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    • 2007
  • To investigate whether sulindac, sulindac sulfone, and sulindac sulfide could affect cancer cell viabilities, human colorectal HCTl16 cells were treated with 10 ${\mu}M$ of each NSAID. Among treated NSAms, sulindac sulfide dramatically decreased the cell viabilities detected by MTS and the cytotoxic effect showed dose-dependent manner. To understand the molecular mechanism of cell death in response to sulindac sulfide treatment, we performed oligo DNA microarray analysis. We found that 23 genes were up-regulated more than 2 folds, whereas 33 genes were down-regulated more than 2 folds by treatment of 10 ${\mu}M$ sulindac sulfide. Among the up-regulated genes, we selected 3 genes (NAG-1, DDIT3, PCK2) and performed RT-PCR and quantitative real-time PCR to cofirm microarray data. The results of RT-PCR and real-time PCR were highly accorded with those of microarray experiment. As NAG-1 is well-known gene as tumor suppressor, we detected changes of NAG-1 expression by 10 ${\mu}M$ of sulindac, sulindac sulfone, and sulindac sulfide. The results of RT-PCR and quantitacve real-time PCR indicated that sulindac sulfide was the strongest inducer of NAG-1 among treated NSAIDS. This result implies that induction of NAG-1 by sulindac sulfide plays important role in cell death of colorectal cancer. Overall, we speculate that these results may be helpful in understanding the molecular mechanism of the cancer chemoprevention by sulindac sulfide in human colorectal cancer.

Anti-cancer Effects and Molecular Mechanisms of Withaferin A (Withaferin A의 다양한 항암 효과 및 분자생화학적 기전)

  • Woo, Seon Min;Min, Kyoung-Jin;Kwon, Taeg Kyu
    • Journal of Life Science
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    • v.23 no.3
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    • pp.462-469
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    • 2013
  • Withaferin A is a steroidal lactone purified from the Indian medicinal plant Withania somnifera. It exhibits a wide variety of activities, including anti-tumor, anti-inflammation, and immunomodulation properties. In this review, we focused on the anti-cancer effects of withaferin A. Withaferin A inhibits cell proliferation, metastasis, invasion, and angiogenesis in cancer cells. Furthermore, it sensitized irradiation, tumor necrosis factor-related apoptosis-inducing ligand (TRAIL)-, and doxorubicin-mediated apoptosis. The results showed that multiple mechanisms were involved in withaferin A-mediated anti-cancer effects. First, withaferin A increased intracellular reactive oxygen species (ROS) production and induced ER stress- and mitochondria-mediated apoptosis. Second, withaferin A inhibited the signaling pathways (Jak/STAT, Akt, Notch, and c-Met), which are important in cell survival, proliferation, and metastasis. Third, it induced apoptosis and inhibited cancer cell migration through the up-regulation of prostate apoptosis protein-4 (Par-4). Finally, withaferin A up-regulated pro-apoptotic protein expression levels through the inhibition of proteasome activity. Our findings suggested that withaferin A is a potential, potent therapeutic agent.

Hyaluronidase Inhibitory Activity of Extracts from Doenjang, Chungkookjang and Miso (된장, 청국장 및 미소추출물의 Hyaluronidase 저해활성)

  • Ahn, Sun-Kyung;Hong, Kwang-Won
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.34 no.8
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    • pp.1119-1123
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    • 2005
  • The inhibitory effects of water and methanol extracts of Doenjang, Chungkookjang and Miso on bovine hyaluronidase were examined. The extracts were vacuum-dried and the resulting pellets were dissolved with 0.1 M acetate buffer with 1$\%$ DMSO to a final concentration of 50 mg/mL. The water extracts of Doenjang, Chungkookjang and Miso inhibited 62$\%$, 70$\% $, 56$\%$ of hyaluronidase activity, respectively, while the extract of crushed soybean inhibited 24$\%$ of the activity. Under the same condition, disodiumcromoglycate known as an anti-allergic drug inhibited 46$\%$ of hyaluronidase activity at the concentration of 0.35 mg/mL as a positive control. Also the methanol extracts of Doenjang, Chungkookjang and Miso inhibited 48$\%$, 52$\%$, 70$\%$ of hvaluronidase activity, respectively, while the extract of crushed soybean inhibited 46$\%$ of the activity. After heat treatment of the water extracts of Doenjang, Chungkookjang and Miso at 100"C for 10 min, hyaluronidase inhibitory effects of them were reduced approximately to half. However, hyaluronidase inhibitory effects of methanol extracts were maintained well even after heat treatment.

Apoptotic Response of Human Oral Squamous Carcinoma Cells to Etoposide (Etoposide에 대한 사람구강편평상피암종세포의 세포자멸사 반응)

  • Kim, Gyoo-Cheon;Lee, Kyoung-Duk;Park, Jae-Hyun;Kim, Duk-Han;Park, Jeong-Kil;Park, June-Sang;Park, Bong-Soo
    • Journal of Oral Medicine and Pain
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    • v.30 no.2
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    • pp.231-238
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    • 2005
  • Anti-cancer drugs have been shown to target diverse cellular functions in mediation cell death in chemosensitive tumors. Most antineoplastic drugs used in chemotherapy of leukemias and solid tumors induce apoptosis in drug-sensitive target cells. However, the precise molecular requirements that are central for drug-induced cell death are largely unknown. Etoposide is used for the treatment of lung and testicular cancer. This study was performed to examine whether etoposide promote apoptosis in human oral squamous carcinoma cells (OSC9) as well as in lung and testicular cancer. Etoposide had a significant dose- and time-dependent inhibitory effect on the viability of OSC9 cells. TUNEL assay showed the positive reaction on condensed nuclei. Hoechst stain demonstrated that etoposide induced a change in nuclear morphology. The expression of p53 was increased at 48 hour, suggesting that the nuclear of OSC9 cell was damaged, thereby inducing apoptosis. Etoposide treatment induced caspase-3 cleavage and activation. Intact PARP protein 116-kDa and 85-kDa cleaved product were observed. The activated caspase-3 led cleavage of the PARP. These results demonstrate that etoposide-induced apoptosis in OSC9 cells is associated with caspase-3 activation.