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来源于与 Cryptosphaeria 属相关的海洋来源的子囊菌的细胞毒性 Mcl-1 抑制剂 Cryptosphaerolide。

Cryptosphaerolide, a cytotoxic Mcl-1 inhibitor from a marine-derived ascomycete related to the genus Cryptosphaeria.

机构信息

Center for Marine Biotechnology and Biomedicine, Scripps Institution of Oceanography, University of California-San Diego, La Jolla, California 92093-0204, USA.

出版信息

J Nat Prod. 2010 May 28;73(5):998-1001. doi: 10.1021/np1000889.

DOI:10.1021/np1000889
PMID:20462271
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2901504/
Abstract

Examination of the saline fermentation products from the marine-derived ascomycete fungal strain CNL-523 (Cryptosphaeria sp.) resulted in the isolation of cryptosphaerolide (1). The new compound is an ester-substituted sesquiterpenoid related to the eremophilane class. The structure of the new compound was assigned by spectroscopic and chemical methods. Cryptosphaerolide was found to be an inhibitor of the protein Mcl-1, a cancer drug target involved in apoptosis. It also showed significant cytotoxicity against an HCT-116 human colon carcinoma cell line, indicating that the compound may be of value in exploring the Mcl-1 pathway as a target for cancer chemotherapy.

摘要

从海洋来源的子囊菌真菌菌株 CNL-523(Cryptosphaeria 属)的盐发酵产物中分离得到 cryptosphaerolide(1)。该新化合物是一种酯取代的倍半萜烯,与埃罗菲兰类有关。通过光谱和化学方法确定了新化合物的结构。Cryptosphaerolide 被发现是蛋白 Mcl-1 的抑制剂,Mcl-1 是一种参与细胞凋亡的癌症药物靶点。它对 HCT-116 人结肠癌细胞系也表现出显著的细胞毒性,表明该化合物可能在探索 Mcl-1 途径作为癌症化疗靶点方面具有价值。

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