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Phialomustin A-D, new antimicrobial and cytotoxic metabolites from an endophytic fungus, Phialophora mustea

机译:Phialomustin A-D,一种内生真菌,Philophora mustea的新的抗微生物和细胞毒性代谢产物

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摘要

Phialomustin A-D (1-4), four new bioactive metabolites, with an unprecedented azaphilone derived skeleton, were isolated and characterized from an endophytic fungus isolated from Crocus sativus. The ITS-5.8S-ITS2 ribosomal gene sequence of the endophyte displayed a sequence similarity of more than 99% with Phialophora mustea. The structural determinations of compounds (1-4) were authenticated by spectroscopic and chemical analysis. The absolute configuration of the stereogenic centers of 1, 3 and 4 were determined by electronic circular dichroism spectroscopy. Compounds 3 and 4 showed promising antifungal activities against Candida albicans, with IC50 values of 14.3 and 73.6 mu M, whereas compound 2 exhibited remarkable cytotoxic activity against the human breast cancer cell line, T47D, with an IC50 of 1 mu M.
机译:从从番红花中分离出的一种内生真菌分离并鉴定了具有新的生物活性代谢产物Phialomustin A-D(1-4),该代谢物具有空前的氮杂酚酮骨架。内生植物的ITS-5.8S-ITS2核糖体基因序列与毛霉菌的序列相似性超过99%。化合物(1-4)的结构测定通过光谱和化学分析进行鉴定。 1、3和4的立体异构中心的绝对构型是通过电子圆二色性光谱法确定的。化合物3和4对白念珠菌显示出有希望的抗真菌活性,IC50值为14.3和73.6μM,而化合物2对人乳腺癌细胞系T47D表现出显着的细胞毒性活性,IC 50为1μM.

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