Proceedings of the PSK Conference (대한약학회:학술대회논문집)

The Pharmaceutical Society of Korea (대한약학회)
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Potent inhibition of human cytochrome P450 1 enzymes by SY-081

  • Kim, Yong-Mo (Department of Immunology, College of Pharmacy, Chung-Ang University) ;
  • Lee, Sang-Kwang (Natural Products Research Institute, Seoul National University) ;
  • Kim, Mie-Young (Natural Products Research Institute, Seoul National University) ;
  • Kim, Sang-Hee (Natural Products Research Institute, Seoul National University) ;
  • Jin, Chun-Young (Natural Products Research Institute, Seoul National University)
  • Published : 2003.10.01
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Abstract

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)

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