Novel enoyl-ACP reductase (FabI) potential inhibitors of Escherichia coli from Chinese medicine monomers.

Jingjing Yao, Qingye Zhang, Jun Min, Jin He, Ziniu Yu

Journal: Bioorganic & medicinal chemistry letters 2010;20(1):56-9

PMID: 19959361

Full Text on Elsevier Science View on PubMed

Abstract

By structure-based virtual screening and experimental verification, two Chinese medicine monomers, luteolin and curcumin, had been proved to be uncompetitive inhibitors of enoyl-ACP reductase from Escherichia coli (EcFabI) with the inhibition constant (K(i)) of 7.1microM and 15.0microM, respectively. In particular, curcumin had apparent antibacterial activity against E. coli, and the minimum inhibition concentration (MIC(90)) was 73.7microg/mL. Importantly, fabI-overexpressing E. coli showed reduced susceptibility to the inhibitor compared with the wild-type strains, demonstrating that its antibacterial action is mediated by the inhibition of EcFabI.

Address: State Key Laboratory of Agricultural Microbiology and National Engineering Research Center of Microbial Pesticides, Huazhong Agricultural University, Wuhan 430070, PR China.

DOI: 10.1016/j.bmcl.2009.11.042