Faculty of Pharmaceutical Sciences, Tokushima Bunri University, Tokushima, Japan.
Biological Resource Center (NBRC), Department of Biotechnology, National Institute of Technology and Evaluation, Chiba, Japan.
J Antibiot (Tokyo). 2014 Feb;67(2):163-6. doi: 10.1038/ja.2013.93. Epub 2013 Oct 2.
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.
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)。
