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자료유형
학술대회자료
저자정보
Lee, Sang-Kwang (College of Pharmacy, Chungang University, Seoul) Kim, Sang-Hee (Korea and Natural Products Research Institute, Seoul National Universit, Seoul) Kim, Mie-Young (Korea and Natural Products Research Institute, Seoul National Universit, Seoul) Chun, Young-Jin (Korea and Natural Products Research Institute, Seoul National Universit, Seoul)
저널정보
대한약학회 대한약학회 학술대회 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
발행연도
2002.1
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3,123 - 3,124 (2page)

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Recently we have reported that various hydroxystilbenes show strong inhibition of human P450 1 activity. A series of synthetic trans-stilbene derivatives were prepared and their inhibitory potentials were evaluated with the bacterial membrane of recombinant human P450 1A1, 1A2 or 1B1 coexpressed with human NADPH-P450 reductase to find new candidates for cancer chemoprevention, Of the compounds tested. SY-021 (3.5-dimethoxyphenyl vinyl thiophene) exhibited a potent inhibition of human P450 181 with an IC$_{50}$ value of 2 nM. SY-021 also showed the inhibitrion of P450 1A1 with IC$_{50}$ value of 61 nM and P450 1A2 with IC$_{50}$ value of 11 nM. SY-021 showed 31-fold selectivity for P450 1B1 over P450 1A1 and 6-fold selectivity for P450 1B1 over 1A2. We have further investigated the inhibition kinetics of P450 1A1. 1A2 and 1B1 by SY-021. The modes of inhibition by SY-021were non-compeitive for all three P450 1 enzymes. Effect of preincubation with NADPH on inhibition of P450 1B1 by SY-021 was determined. These results suggest that SY-021 is one of the mostj potent inhibitor of human P450 1 enzymes and may be considered as a good candidate for a cancer chemopreventive agent in human

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