Microbial fermentation-derived inhibitors of efflux-pump-mediated drug resistance

被引：76

作者：

Lee, MD ^{[1
]}

Galazzo, JL ^{[1
]}

Staley, AL ^{[1
]}

Lee, JC ^{[1
]}

Warren, MS ^{[1
]}

Fuernkranz, H ^{[1
]}

Chamberland, S ^{[1
]}

Lomovskaya, O ^{[1
]}

Miller, GH ^{[1
]}

机构：

[1] Microcide Pharmaceut Inc, Mt View, CA 94043 USA

来源：

FARMACO | 2001年 / 56卷 / 1-2期

关键词：

D O I：

10.1016/S0014-827X(01)01002-3

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

A library of 85 000 microbial fermentation extracts was screened for inhibitors of multidrug resistance efflux pumps in Pseudomonas aeruginosa and Candida albicans. New compounds EA-371alpha and EA-371delta were isolated and demonstrated to be potent and specific inhibitors of the MexAB-OprM pump in P. aeruginosa. Two series of fungal metabolites, enniatins and beauvericins, were found to be ubiquitous and potent inhibitors of ABC transporters. Milbemycins were rediscovered as potent inhibitors of the CDR1 pump in C. albicans, and demonstrated to potentiate effectively the antifungal activity of fluconazole and SCH-56592 against a wide variety of Candida clinical isolates. (C) 2001 Elsevier Science S.A. All rights reserved.

引用

页码：81 / 85

页数：5

共 15 条

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