南海海绵 Theonella swinhoei 中的甾醇类化合物。

Swinhoeisterols from the South China Sea Sponge Theonella swinhoei.

机构信息

School of Pharmacy , Second Military Medical University , 325 Guo-He Road , Shanghai 200433 , People's Republic of China.

Department of Organic Chemistry , University of Debrecen , POB 400, H-4002 Debrecen , Hungary.

出版信息

J Nat Prod. 2018 Jul 27;81(7):1645-1650. doi: 10.1021/acs.jnatprod.8b00281. Epub 2018 Jul 10.

DOI:10.1021/acs.jnatprod.8b00281

PMID:29989811

Abstract

Swinhoeisterols C-F (1-4), four new steroids having a rearranged 6/6/5/7 ring system, were isolated from the Xisha sponge Theonella swinhoei, together with the known analogue swinhoeisterol A (5). Their structures were determined based on spectroscopic analysis, TDDFT-ECD and optical rotation calculations, and biogenetic correlations. In an in vitro assay, compound 1 showed an inhibitory effect on (h)p300 with an IC value of 8.8 μM, whereas compounds 2-4 were not active.

摘要

从西沙海绵 Theonella swinhoei 中分离得到了具有重排的 6/6/5/7 环系统的 4 个新甾体化合物 Swinhoeisterols C-F (1-4)，同时还分离得到了已知的类似物 Swinhoeisterol A (5)。基于光谱分析、TDDFT-ECD 和旋光计算以及生物发生相关性，确定了它们的结构。在体外试验中，化合物 1 对 (h)p300 具有抑制作用，IC 值为 8.8 μM，而化合物 2-4 则没有活性。