• Proceedings of the PSK Conference
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• 2002.10a
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• pp.253.1-253.1
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• 2002

DA-8159 is a new PDEV inhibitor, synthesized by Dong-A Pharm, as an oral agent to treat male erectile dysfunction. DA-8159 and sildenafil are mainly metabolized by cytochrome P450 enzyme CYP 3A4. In this study. we compared the metabolism of DA-8159 with sildenafil in vitro and in vivo. First, we quantified the remaining gatio of original compound, DA-8159 and sidenafil., after we incubated drugs for 30 minutes with human liver microsome cytochrome P 450 3A4. (omitted)

• Korean Journal of Medicinal Crop Science
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• v.24 no.1
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• pp.7-13
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• 2016

Background : Ginger has been extensively used in foods and traditional medicines in Asian countries. Despite its frequent consumption in daily life, the mechanism of potential interactions between ginger components-drug has not been examined. To elucidate the mechanism of governing the effects of 6-shogaol, a primary constituent of dried ginger, on human cytochrome P450 (CYP) isoenzymes an incubation studies were carried out using pooled human liver microsome (HLM). Methods and Results : CYP isoenzyme specific substrate was incubated with multiple concentrations of inhibitor, HLM and cofactors. 6-shogaol showed a potent inhibitory effect on CYP2C9, CYP1A2 and CYP2C19 with half maximal inhibitory concentration ($IC_{50}$) values of 29.20, 20.68 and $18.78{\mu}M$ respectively. To estimate the value of the inhibition constant ($K_i$) and the mode of inhibition, an incubation study with varying concentrations of each CYP isoenzyme-specific probe was performed. 6-shogaol inhibited CYP2C9 and CYP2C19 noncompetitively ($K_i=29.02$ and $19.26{\mu}M$ respectively), in contrast, the inhibition of CYP1A2 was best explained by competitive inhibition ($K_i=6.33{\mu}M$). Conclusions : These findings suggest that 6-shogaol may possess inhibitory effects on metabolic activities mediated by CYP1A2, CYP2C9 and CYP2C19 in humans.

• Journal of the Korean Society of Tobacco Science
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• v.13 no.1
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• pp.19-26
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• 1991

Ames test using special strains which are histidine requiring mutant of Salmonella typhimufium , is widely utilized as short-term bioassay to evaluate the genotoxicity of chemicals. This method requires the liver microsome(5-9 fraction) to provide mammalian metabolism of the compounds, Therefore, the mutagenic potency of the chemicals is affected by not only the intrinsic properties of them but also the efficiency of the in vitro microsomal activation system. For this reason, the complex mixtures such as environmental pollutants from occupational sources, natural products or cigarette smoke condensates(CSC) , might be often appeared the false results. Induction of sister chromatid exchange(SCE) in cultured cells is known as another sensitive and powerful tool for the measurement of genotoxicity and the method has also an advantage which is able to apply to the in vitro and in vivo systems. In the present study, the inducibilities of revertant colonies in tester strain TA98 and SCE in human Iymphocytes by positive controls and total particulated materials(TPM) obtained from various brand(domastic and imported) cigarettes were compared in order to investigate whether the results in Ames test are in agreement with those in SCE analysis. The mutagenic activities of well known mutagens such as B(a)P showed excellent dose-response in the both methods although the induction mechanism was different each other, but cyclophosphamide resulted such effect only in SCE analysis. Most TPM tested showed a similar pattern in the mutagenic activities in those methods. However, only two(one imported brand and one domestic sample cigarettes) among the TMP obtained from various cigarettes appeared the higher induction in SCE than Ames test.

• Journal of the Korean Society of Food Science and Nutrition
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• v.36 no.11
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• pp.1365-1370
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• 2007

The inhibitory effects of the water and methanol extracts of Jakwangdo and Honghyangmi on the rat microsome lipid peroxidation and growth of four human cancer cells such as HepG2 (liver cancer), SNU-1 (stomach cancer) MCF-7 (breast cancer) and SNU-C4 (colon cancer) were examined. The methanol extracts of red colored rices showed the antioxidant activity and growth inhibitory effects of cancer cells. However, water extracts did not show the activities. Inhibitory activities of methanol extracts of Jakwangdo and Honghyangmi against lipid peroxidation of rat microsome was 80% and 68%, respectively, at the concentration of 1 mg/assay. Jakwangdo methanol extracts showed the highest growth inhibitory activity in MCF-7 cells among the cancer cells tested. The methanol extracts of red colored rices were further fractionated with hexane, chloroform, ethyl acetate and butanol. Both chloroform and hexane fractions showed strong growth inhibitory activity in HepG2 and MCF-7 cells.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.20 no.1
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• pp.1-13
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• 1994

An antioxidative compound was isolated from pine needles. This compound was identified as 4-hydroxy-5-methyl-3[2H]-furanone on the basis of spectroscopic evidences. It scavenged 1,1-diphenyl-2-picrylhydrazyl free radicals more efficiently than maltol and tocopherol did. It exhibited an inhibitory effect on the lipid peroxidation of rat liver microsome induced by Fe(ll)/ascorbate, and the protective effect against UV cytotoxicity in cultured human fibroblasts. In addition, HMF appeared to prevent the cellular melanogenesis in the cultured murine melanoma cells, more effectively than kojic acid, a well known inhibitor of melanogenesis, while the former was not so effective as the latter for the inhibilion of the tyrosinase. Considering that cellular melanogenesis is a metabolic process triggered by oxidative stress, it was tentatively deduced that the antioxidative property of HMF may afford the effect against cellular pigmentation by alleviating the causative stress. This study provided a novel inhibitor of melanogenesis, that might be useful for the cosmetic applications.

• Korean Journal of Food Science and Technology
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• v.31 no.3
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• pp.831-837
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• 1999

Ochratoxin A (OA), a naturally occurring mycotoxin, has been known to cause renal and hepatic lesion in human and animals. This study was carried out to investigate the modulation effects of antioxidant vitamins on OA-induced lipid peroxidation associated with oxidative damage. Vitamin C (10 mg/kg/day) and vitamin E (63.8 mg/kg/day) were administered by intraperitoneal (i.p.) injection to male ICR mice, and 1 hr later, OA which was dissolved in 0.1 M $NaHCO_3$, treated 4 mg/kg/day by i.p. injection. During 4 days repeated, and then measured superoxide dismutase (SOD) activity, catalase activity and malondialdehyde (MDA) formation in microsomes of liver and kidney. Additionally, the relationship between cell damage and modulation effects of antioxidant vitamins was evaluated by comet assay. Results were as followed; i) SOD, catalase activity and MDA level were significantly increased by OA treated, ii) SOD, catalase activity and MDA formation were significantly decreased by antioxidant vitamins combine treated, iii) blood cell damage associated with lipid peroxidation, induced by OA, also modulated by antioxidant vitamins. These results indicated that antioxidant vitamins might be used for prevention of renal and hepatic damage due to ochratoxicosis.