迪斯特毒素 A-C，源自海绵共生曲霉突变株的新型天青菌素二聚体。
Diasteltoxins A-C, Asteltoxin-Based Dimers from a Mutant of the Sponge-Associated Emericella variecolor Fungus.
机构信息
State Key Laboratory of Natural and Biomimetic Drugs, Peking University , Beijing 100191, P. R. China.
Institute of Pharmaceutical Biology and Biotechnology, Heinrich-Heine University , 40225 Duesseldorf, Germany.
出版信息
Org Lett. 2016 Sep 16;18(18):4678-81. doi: 10.1021/acs.orglett.6b02313. Epub 2016 Aug 29.
Three novel asteltoxin-bearing dimers namely diasteltoxins A-C (1-3) along with asteltoxin were isolated from a mutated strain of a sponge-derived fungus Emericella variecolor XSA-07-2. Their structures were determined by extensive spectroscopic analyses including the computed electronic circular dichroism (ECD) data for the configurational assignment. The biogenetic formation of the dimers through [2 + 2] cycloaddition of asteltoxin was postulated. Diasteltoxins 1-3 exerted inhibitory effects against the tumor cell lines H1299 and MCF7 and exhibited significant inhibition against thioredoxin reductase (TrxR).
从海绵来源真菌Emericella variecolor XSA-07-2 的突变株中分离得到三种新型含asteltoxin 的二聚体，分别为 diasteltoxins A-C（1-3）以及 asteltoxin。通过包括计算电子圆二色性（ECD）数据在内的广泛光谱分析确定了它们的结构，用于构象分配。推测这些二聚体是通过 asteltoxin 的[2 + 2]环加成反应形成的。Diasteltoxins 1-3 对肿瘤细胞系 H1299 和 MCF7 表现出抑制作用，并对硫氧还蛋白还原酶（TrxR）表现出显著的抑制作用。
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