海洋海绵 Theonella swinhoei 中的新 4-亚甲基甾醇。

New 4-methylidene sterols from the marine sponge Theonella swinhoei.

机构信息

Research Center for Marine Drugs, State Key Laboratory of Oncogenes and Related Genes, Department of Pharmacy, Ren Ji Hospital, School of Medicine, Shanghai Jiao Tong University, Shanghai 200127, China.

出版信息

Fitoterapia. 2018 Jun;127:279-285. doi: 10.1016/j.fitote.2018.03.006. Epub 2018 Mar 11.

DOI:10.1016/j.fitote.2018.03.006

PMID:29540311

Abstract

A series of 4-methylidene sterols including three new compounds 1-3, were isolated from the marine sponge Theonella swinhoei. The structures of new compounds were determined on the basis of spectroscopic analyses. Compounds 3, 5, and 6 showed cytotoxicities against U937, MCF-7, and PC-9 cancer cells with IC in the range of 1.6-8.8 μM. The new compound 3 exhibited remarkable proapoptotic activity in breast cancer cells. Mechanically, 3 significantly triggered reactive oxygen species (ROS) accumulation resulting in apoptosis and DNA damage in breast cancer cells.

摘要

从海洋海绵 Theonella swinhoei 中分离得到了一系列 4-亚甲基甾醇，包括三个新化合物 1-3。根据光谱分析确定了新化合物的结构。化合物 3、5 和 6 对 U937、MCF-7 和 PC-9 癌细胞表现出细胞毒性，IC 范围为 1.6-8.8μM。新化合物 3 对乳腺癌细胞表现出显著的促凋亡活性。在机制上，3 显著触发活性氧 (ROS) 积累，导致乳腺癌细胞凋亡和 DNA 损伤。