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来源于产黄青霉 F375 的-verruloactone C,具有空前的双螺骨架,是一种新型金黄色葡萄球菌烯酰-ACP 还原酶抑制剂。

Verrulactone C with an unprecedented dispiro skeleton, a new inhibitor of Staphylococcus aureus enoyl-ACP reductase, from Penicillium verruculosum F375.

机构信息

Superbacteria Research Center, Korea Research Institute of Bioscience and Biotechnology, Yusong, Daejeon 305-806, Republic of Korea.

Global Research Cluster, RIKEN, Hirosawa 2-1, Wako, Saitama 351-0198, Japan.

出版信息

Bioorg Med Chem Lett. 2014 Jan 1;24(1):83-6. doi: 10.1016/j.bmcl.2013.11.071. Epub 2013 Dec 4.

Abstract

An highly quaternary and unprecedented dispiro compound, verrulactone C, with the known compound, altenuisol, were isolated from a culture broth of the fungal strain Penicillium verruculosum F375 and their structures were established by various spectral analysis. Verrulactone C and altenuisol showed FabI-selective inhibition. Especially altenuisol had the high correlation between FabI-inhibition and whole cell antibacterial activity against Staphylococcus aureus and MRSA with MICs of 8-32μg/mL.

摘要

从真菌Penicillium verruculosum F375 的发酵液中分离得到一个高度四级且前所未有的双螺环化合物 verrulactone C 和已知化合物 altenuisol,通过各种光谱分析确定了它们的结构。Verrulactone C 和 altenuisol 对 FabI 具有选择性抑制作用。特别是 altenuisol 对金黄色葡萄球菌和耐甲氧西林金黄色葡萄球菌(MRSA)的 FabI 抑制作用与全细胞抗菌活性之间具有高度相关性,MIC 值为 8-32μg/mL。

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