Synthesis and biological evaluation of 6',7'-dihydroxybergamottin (6,7-DHB), a naturally occurring inhibitor of cytochrome P450 3A4

被引：18

作者：

Bellevue, FH

Woster, PM

Edwards, DJ

He, K

Hollenberg, PF

机构：

[1] WAYNE STATE UNIV, DEPT PHARMACEUT SCI, DETROIT, MI 48202 USA

[2] WAYNE STATE UNIV, DEPT PHARM PRACTICE, DETROIT, MI 48202 USA

[3] UNIV MICHIGAN, DEPT PHARMACOL, ANN ARBOR, MI 49109 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 20期

关键词：

D O I：

10.1016/S0960-894X(97)10043-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The recently isolated inhibitor of cytochrome P450 CYP3A4, 6',7'-dihydroxybergamottin (6,7-DHB), was synthesized by an efficient route that is readily adaptable to the production of analogues. The compound was evaluated as an inhibitor of 3A4 in a purified enzyme preparation, as well as against human liver microsomes and human 3A4 expressed in Escherichia coli membrane. In each case, 6,7-DHB proved to be a potent NADPH-and time dependent inactivator of 3A4. (C) 1997 Elsevier Science Ltd.

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页码：2593 / 2598

页数：6

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