Combined effect of epigallocatechin gallate and triclosan on enoyl-ACP reductase of Mycobacterium tuberculosis

被引：21
作者：
Sharma, Shailendra Kumar [1 ]
Kumar, Gyanendra [1 ]
Kapoor, Mili [1 ]
Surolia, Avadhesha [1 ,2 ]
机构：
[1] Indian Inst Sci, Mol Biophys Unit, Bangalore 560012, Karnataka, India
[2] Natl Inst Immunol, New Delhi 110067, India
来源：
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS | 2008年 / 368卷 / 01期
关键词：
Mycobacterium tuberculosis; tuberculosis; InhA; enoyl reductase; FAS I; FAS III; tea catechins; epigallocatechin gallate; EGCG; triclosan; fluorescence titration; scatchard plot;
D O I：
10.1016/j.bbrc.2007.10.191
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Among the various inhibitors known for enoyl-acyl carrier protein (ACP) reductases, triclosan and green tea catechins are two promising candidates. in the present study, we show, for the first time that epigallocatechin gallate (EGCG), a major component of green tea catechins, inhibits InhA, the enoyl-ACP reductase of Mycobacterium tuberculosis with an IC50 of 17.4 mu M. EGCG interferes with the binding of NADH to InhA. We also demonstrate that EGCG increased the inhibitory activity of triclosan towards InhA and vice-versa. Direct binding assay using [H-3]EGCG and fluorescence titration assay support the spectrophotometric/kinetic inhibition data. The biochemical data has been explained by docking simulation studies. (C) 2007 Elsevier Inc. All rights reserved.
引用
收藏
页码：12 / 17
页数：6
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