• Title/Summary/Keyword: 약물 농도

Search Result 551, Processing Time 0.031 seconds

Effects of Tributyltin in vitro on Hepatic Monooxygenase System in Marine Fishes (유기주석화합물이 해산 어류의 간장 MFO 효소계에 미치는 영향)

  • 전중균;이미희;이지선;심원준;이수형;허형택
    • Korean Journal of Environmental Biology
    • /
    • v.21 no.1
    • /
    • pp.18-25
    • /
    • 2003
  • Effects of tributyltin chloride (TBTC) in vitro on mixed function oxygenase (MFO) system on liver microsome of eight marine fish species were investigated. To determine the effects on MFO system, cytochrome P45O (CYP) and cytochrome b5 con-tents, activities of two reductases (NADH-cytochrome b5 reductase and NADPH-cy-tochrome P450 reductase) and four dealkylation enzymes (EROD, PROD, MROD and ECOD) were measured in fish microsoms exposed to TBTC for 20 min. The WP content was reduced to 10% of the control group in 6 out of 8 species exposed to TBTC, whereas there was no significant change in the cytochrome bs content. the response of NAD(P)H dependant reductases depended on fish species. The dealkylation enzyme activities in microsome were also apparently inhibited by TBTC. The degree of inhibition was different among fish species and four enzymes. The EROD activities in eight species were decreased to the range of 1∼65% of control group.

Evaluation of short-term Hypolipidemic Effect and Safety of Simvastatin($Zocor^{(R)}$) in Patients with Hyperlipidemia (고콜레스테롤혈증 환자에서 Simvastatin($Zocor^{(R)}$) 단기 투여후 효과와 안정성 평가)

  • Kim, Min-Kyoung;Park, Yong-Ho;Park, Jong-Sun;Shin, Dong-Gu;Kim, Young-Jo;Kim, Gi-Sik
    • Journal of Yeungnam Medical Science
    • /
    • v.20 no.2
    • /
    • pp.152-159
    • /
    • 2003
  • Background : Hyperlipidemia is the one of the major risk factors causing the atherosclerosis of coronary arteries. Treatment of hyperlipidemia with drugs has been confirmed the effects of therapy showing a decreased incidence of coronary artery disease. Simvastatin is a new drug of HMG-CoA reductase inhibitors and the short-term hypolipidemic effects and safety of simvastatin is evaluated in patients with hyperlipidemia. Methods: We studied 63 patients (39 males and 24 females, mean age 58) for 12 weeks whose plasma levels of total cholesterol were higher than 240 mg/dL or higher than 220 mg/dL with ischemic heart disease. Simvastatin was administered 20 mg/day and measured lipid profile at 12 week interval. Result: 1) Simvastatin significantly reduced the level of the plasma total cholesterol(-29.3%), LDL-cholesterol(-36.9%) and triglyceride(-13%)(p<0.05) but the level of HDL-cholesterol was not changed after 12 weeks simvastatin therapy. 2) the clinical symptoms and laboratory examination before and after simvastatin treatment showed no particular abnormal findings in short term follow up. Conclusion: These results suggested that short-term simvastatin therapy in patients with hyperlipidemia seeems to be very effective and safe.

  • PDF

Evaluation of Medicinal Activity on Isolated Inhibitory Compounds against Helicobacter pylori from Cheongmoknosang Mulberry Leaves (청목노상 뽕잎에서 분리한 Helicobacter pylori 저해물질에 대한 약효평가)

  • Kim, Byong-O;Cho, Young-Je
    • Journal of Applied Biological Chemistry
    • /
    • v.54 no.4
    • /
    • pp.265-269
    • /
    • 2011
  • Inhibitory effect of useful components from Cheongmoknosang mulberry leaves extracts against Helicobacter pylori were investigated to develope them to a health functional food. It was confirmed that H. pylori bacterial infection occurred after 6 weeks over in C57BL/6 mouse which was caused the infection, and the average number of pathogens was $8{\times}10^5$ CFU/mL. Effects of the prevention and cure against H. pylori were tested by the mouth administration with Cheongmoknosang mulberry leaves extracts include the active ingredient, and number of H. pylori colony in stomach of drug groups were decreased more than control group. The result of testing immuno-glogulin isotype from the separated serum from a mouse, IgG1, IgA produced more in administered group, and it is expected to inhibit the H. pylori infection because of increasing antibody production in the mixture. These results suggest that caffeic acid, rosemarinic acid and chlorogenic acid in Cheongmoknosang mulberry leaves extracts are very effective to prevent or cure against H. pylori infection. So the ratio of infection is increasing and it is regarded to be able to prevent and cure the disease like gastritis, gastric ulcer and gastric cancer which are caused by H. pylori.

in vitro Anticancer Activity and in vivo Chronic Toxicity of Homoharringtonine (개비자나무 유효성분인 homoharringtonine의 in vitro 항암활성 및 in vivo 만성 독성)

  • Yoo, Gui-Jae;Cho, Chul-Hee;Lee, Gun-Soon;Ryoo, Zae-Young;Chae, Hee-Jeong
    • Applied Biological Chemistry
    • /
    • v.51 no.2
    • /
    • pp.124-128
    • /
    • 2008
  • Cell proliferation inhibitory effects of homoharringtonine (HHT), an active drug substance in Cephalotaxus koreana, against blood cancer cell line K562 were evaluated. In addition, in vivo chronic toxicity test with mouse was carried out. When K562 cell line was treated everyday for 9, 6, 3 days, $IC_{50}$ values of HHT were determined as 0.27, 0.37, and 1.10 mM respectively. The anticancer activity of HHT was comparable to adriamycin, a known anticancer drug compound for blood cancer treatment. in vivo chronic toxicity test of the HHT, the number of red blood cell (RBC) showed no significant difference. From the analysis of the liver-functional enzymes in blood, all of liver damage related enzymes such as glutamate-oxalate-transferase (GOT), glutamate-pyruvate-transferase (GPT), cholesterol (Chol) and alkaline phosphatase (ALP) showed no significant change. However, from the histologic test, a neutrophil of the band type in liver tissue was observed.

Interaction of Forskolin with the Effect of Oxotremorine on $[^3H]-Acetylcholine$ Release in Rabbit Hippocampus (가토 해마에서 Acetylcholine 유리에 미치는 Oxotremorine 및 Forskolin의 영향)

  • Choi, Bong-Kyu;Kim, Chong-Suhn;Yoon, Young-Bok;Kook, Young-Johng
    • The Korean Journal of Pharmacology
    • /
    • v.27 no.2
    • /
    • pp.89-97
    • /
    • 1991
  • As it has been reported that the depolarization-induced release of acetylcholine(ACh) is diminished by activation of presynaptic muscarinic autoreceptor in rabbit hippocampus and various lines of evidence indicate the involvement of adenylate cyclase system in ACh release, it was attempted to delineate the role of cAMP in the muscarinic autoreceptor-mediated control of ACh release. Slices and synaptosomal preparations from rabbit hippocampus were incubated with $[^3H]-choline$ and the release of the labelled products was evoked either by electrical stimulation or by $high-K^+$, and the influence of various agents on the evoked tritium release was investigated. Forskolin, a specific adenylate cyclase activator, in concentrations ranging from $0.1\;to\;30\;{\mu}M$, increased the $[^3H]-ACh$ release in a dose-dependent manner and also dbcAMP increased the tritium outflow. The responses to oxotremorine, a specific muscarinic agonist, were characterized by decrement of ACh release in dose range of $0.1-30\;{\mu}M$, and the oxotremorine effects were inhibited either by forskolin or by atropine. Glibenclamide, a specific $K^+-channel$ inhibitor, in concentration of $1{\sim}10\;{\mu}M$, decreased the evoked ACh release slightly and inhibited the enhancing effect of evoked ACh-release of a large dose$(10\;{\mu}M)$ of forskolin. These results indicate that the cAMP might play a role in the muscarinic ACh receptor-mediated control of ACh rlease in the rabbit hippocampus and suggest that certain potassium currents may also be participated in the post-receptor mechanism of ACh release.

  • PDF

Ginsenosides Inhibit N-, p-, arid Q-types but not L-type of $Ca^{2+}$ Channel in Bovine Chromaffin cells

  • Seok Chol;Jung, Se-Yeon;Kim, Hyun-Oh;Kim, Hack-Seang;Hyewhon Rhim;Kim, Seok-Chang;Nah, Seung-Yeol
    • Journal of Ginseng Research
    • /
    • v.24 no.1
    • /
    • pp.18-22
    • /
    • 2000
  • In previous reports we have shown that ginsenosides inhibit high threshold voltage-dependent $Ca^{2+}$ channels in neuronal cells. However, these studies did not show whether ginsenosides-induced inhibition of $Ca^{2+}$ currents discriminates among the various $Ca^{2+}$ channel subtypes, although it is known that there are at least five different $Ca^{2+}$ channel subtypes in neuronal cells. In this study we investigated the effect of ginsenosides on high threshold voltage-dependent $Ca^{2+}$ channel subtypes using their selective $Ca^{2+}$ channel blockers nimodipine (L-type), $\omega$-conotoxin GVIA (N-type), or $\omega$-agatoxin IVA (P-type) in bovine chromaffin cells. We could observe that ginsenosides inhibited high threshold voltage-dependent $Ca^{2+}$ currents in a dose-dependent manner. The $IC_{50}$/ was about 120 $\mu$g/ml. Nimodipine had no effect on ginsenosides response. However, the effect of ginsenosides on $Ca^{2+}$ currents was reduced by $\omega$-conotoxin GVIA, $\omega$-agatoxin IVA, and mixture of nimodipine, $\omega$-contoxin GVIA, and $\omega$-agatoxin IVA. These data suggest that ginsenosides are negatively coupled to three types of calcium channels in bovine chromaffin cell, including an $\omega$-conotoxin GVIA-sensitive (N-type) channel, an $\omega$-agatoxin IVA-sensitive (P-type) channel and nimodipine/$\omega$-conotoxin GVIA/$\omega$-agatoxin IVA-resistant (presumptive Q-type) channel.Q-type) channel.

  • PDF

The Effect of Magnolol on UVB-induced Inflammation Damage Control via the Nrf2-SOCS3-Jak2-STAT3 Pathway in Human Dermal Fibroblasts (마그놀롤의 HDF세포에서 Nrf2-SOCS3-Jak2-STAT3에 의한 UVB 유래 염증데미지 조절)

  • Nam, Young sun;Ji, Juree
    • Journal of Life Science
    • /
    • v.30 no.10
    • /
    • pp.867-876
    • /
    • 2020
  • This study investigated the repair of UVB-induced cell damage by magnolol. We performed a drug-repurposing screen, and, in the STAT3 reporter gene assay, magnolol was identified as a suppressor of STAT3 that improves the cell viability of HDF cells. HDF cells treated with IL-6, UVB, and IFNγ showed the highest expression of Jak2 and phosphorylated STAT3 (p-STAT3), and magnolol was able to decrease the expression of Jak2 and p-STAT3 in UVB-induced cells. Moreover, UVB-damaged cell growth increased significantly in correlation with both reactivation and with magnolol in a dose-dependent manner. Compared with AG490 (a Jak2 inhibitor) treatment of UVB-treated HDF cells, cell proliferation increased significantly. We confirmed that AG490 and magnolol reduced TNF-α concentrations, and Western blotting (protein level) showed decreases in Jak2 and p-STAT3 expression in only the magnolol-treated cells. The expression of Jak2, p-STAT3, and SOCS3 also increased only after treatment with magnolol. Cells were treated with magnolol and ML385 (an NRF2 inhibitor), and these secondary metabolites reduced cell proliferation and NRF2 expression. The amount of MMP9 was also increased by cotreatment with magnolol and ML385. Collectively, these results demonstrate the potential of magnolol for repairing cells after UVB-induced damage by regulating the expression of NRF2, SOCS3, Jak2, and STAT3.

Enhanced Antimicrobial Activities and Physicochemical Characteristics of Isoliquiritigenin Encapsulated in Hydroxypropyl-β-Cyclodextrin (아이소리퀴리티게닌을 담지한 2-하이드록시프로필-베타사이클로덱스트린의 물리화학적 특성 및 항균활성 연구)

  • Kim, Hae Soo;Im, Na Ri;Park, Soo Nam
    • Applied Chemistry for Engineering
    • /
    • v.26 no.6
    • /
    • pp.719-724
    • /
    • 2015
  • Isoliquiritigenin (ILG) is a hydrophobic component in licorice and has a variety of pharmaceutical and biological activities. In this study, we prepared an isoliquiritigenin-hydroxypropyl-${\beta}$-cyclodextrin (ILG/HP-${\beta}$-CD) complex by freeze-drying method to enhance its water solubility. The complex was characterized by phase solubility studies, DSC, SEM, and 1H NMR. Antimicrobial activities against Staphylococcus aureus (S. aureus) and Escherichia coli (E. coli) were evaluated by broth dilution method. The results showed that the stoichiometry of ILG/HP-${\beta}$-CD complex was 1 : 1. The antimicrobial activity of ILG/HP-${\beta}$-CD complex was higher than that of using free ILG against S. aureus and E. coli. Therefore, we suggest that ILG/HP-${\beta}$-CD complex may be used as a natural antiseptic and could potentially replace synthetic preservatives in cosmetic and food industries.

Effects of Nutrition Therapy and Drug Treatment on the Blood Lipid Levels in Patients with Hyperlipidemia according to Genetic Polymorphism of Apo CII (Apo CIII 유전자 다형성에 따라 영양치료 및 약물 병용치료가 고지혈증 환자의 혈중 지질 농도에 미치는 영향)

  • 조여원;임정은;김수정;김영설
    • Journal of Nutrition and Health
    • /
    • v.33 no.8
    • /
    • pp.813-823
    • /
    • 2000
  • The purpose of this study was to investigate the effects of the nutrition therapy and drug(simvastatin) treatment on the levels of blood lipids for the hyperlipidemic patients according to genetic polymorphism of apo CIII. Subjects of the study consisted of 43(male: 9, female: 34 )hyperlipidemic patients registered to Kyung Hee Medical Center, Intakes of nutrients for the subjects were determined by 24-hr recall method through a personal interviews. The subjects were instructed to take the hypolipidemic and hypocholesterolemic diets. Compliance was monitored through food records, personal interview, and body-weight measurements. The patients changed their basal diet containing 40. 1g fat(182.7mg cholesterol./day) to a diet containing 30.7g fat(139.2mg cholesterol/day) after 12 weeks of nutrition therapy. The distribution of genotypes for apo CIII by Msp I was 32.5% of TT, 50.0% of TC, and 17.5% of CC. aT the beginning of the study, the level of blood triglyceride was the highest for patients with TT and TC. Following the nutrition therapy, patients with CC exhibited the largest drop of blood triglyceride. Following simvastatin treatment with nutrition therapy, blood LDL-cholesterol decreased in most of the patiens with TT. Meanwhile the distribution of genotypes for apo CII by the Fok I was 10.0% of TT, 47.5% of TC, and 42.5% of CC. The level of blood triglyceride was the highest for patients with CC. Following the nutrition therapy, patients with TC exhibited a significant drop for the blood triglyceride. Following simvastatin treatment with nutrition therapy the level of blood LDL-cholesterol decreased in most of the patients with CC. We concluded that dietary habits and food have been changed by nutrition therapy. And blood lipid levels have been decreased by the restriction of intakes of energy, fat and cholesterol. There was variation in the levels of blood lipids according to apo CII polymorphisms. The level of blood lipids responded to nutrition therapy and drug treatment in different was according to genetic polymorphisms. Accordingly, the choice of individualized therapy based on the patient\\`s genetic polymorphism is very important for effective therapy(Korean J Nutrition 33(8) : 813-823, 2000)

  • PDF

Anti-Varicella Zoster Virus Activity of Water Soluble Components of Elfvingia applanata Alone and in Combinations with Interferons (잔나비걸상 수용성성분의 항-Varicella Zoster Virus 작용과 Interferon과의 병용효과)

  • Kim, Young-So;Lee, Seong-Kug;Lee, Young-Nam;Han, Seong-Sun
    • The Korean Journal of Mycology
    • /
    • v.27 no.3 s.90
    • /
    • pp.237-241
    • /
    • 1999
  • To search for less toxic antiviral agents from Basidiomycetes, the water soluble components (=EA), were isolated from the carpophores of Elfvingia applanata (Pers.) Karst. Anti-varicella zoster virus (Oka strain; anti-VZV/Oka) activity of EA was examined in MRC-5 cells by plaque reduction assay in vitro. And the combined antiviral effects of EA with interferon (IFN) alpha or IFN gamma were examined on the multiplication of VZV/Oka. EA exhibited a dose-dependent reduction in the plaque formation of VZV/Oka with 50% effective concentration $(EC_{50})$ of $464.14\;{\mu}g/ml$. The results of the combination assay were evaluated by the combination index (CI) that was calculated by the multiple drug effect analysis. The combination of EA with IFN alpha showed partially synergistic or additive effects with CI values of $0.83{\sim}1.09$ for 50%, 70%, 90% effective levels, and those with IFN gamma showed antagonism with CI values of $1.20{\sim}1.24$.

  • PDF