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来自昆虫病原真菌虫草头孢菌 NBRC 103832 的环二肽,cardinalisamides A-C 的体外抗变形虫活性。

In vitro antitrypanosomal activity of the cyclodepsipeptides, cardinalisamides A-C, from the insect pathogenic fungus Cordyceps cardinalis NBRC 103832.

机构信息

Faculty of Pharmaceutical Sciences, Tokushima Bunri University, Tokushima, Japan.

Biological Resource Center (NBRC), Department of Biotechnology, National Institute of Technology and Evaluation, Chiba, Japan.

出版信息

J Antibiot (Tokyo). 2014 Feb;67(2):163-6. doi: 10.1038/ja.2013.93. Epub 2013 Oct 2.

Abstract

During the search for new antitrypanosomal drug leads, three new antitrypanosomal compounds, cardinalisamides A-C (1-3), were isolated from cultures of the insect pathogenic fungus Cordyceps cardinalis NBRC 103832. Their structures were elucidated using MS analyses and extensive 2D-heteronuclear NMR. The absolute configurations of 1-3 were addressed by chemical degradation and Marfey's analysis. 1-3 showed in vitro antitrypanosomal activity against Trypanosoma brucei brucei with IC50 values of 8.56, 8.65 and 8.63 μg ml(-1), respectively.

摘要

在寻找新的抗锥虫药物先导化合物的过程中,从昆虫病原真菌虫草 NBRC 103832 的培养物中分离得到了三种新的抗锥虫化合物,即 cardinalisamides A-C(1-3)。通过 MS 分析和广泛的二维异核 NMR 确定了它们的结构。通过化学降解和 Marfey 分析确定了 1-3 的绝对构型。1-3 对 Trypanosoma brucei brucei 表现出体外抗锥虫活性,IC50 值分别为 8.56、8.65 和 8.63μg/ml(-1)。

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