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.
引用
收藏
页码：2593 / 2598
页数：6
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