密花豆茎中的拓扑异构酶II抑制成分

Topoisomerase-II-inhibitory principles from the stems of Spatholobus suberectus.

作者信息

Han Ah-Reum, Park Hyen Joo, Chen Daofeng, Jang Dae Sik, Kim Hwa-Jung, Lee Sang Kook, Seo Eun-Kyoung

机构信息

College of Pharmacy, Ewha Womans University, Seoul 120-750, Korea.

出版信息

Chem Biodivers. 2007 Jul;4(7):1487-91. doi: 10.1002/cbdv.200790127.

DOI:10.1002/cbdv.200790127

PMID:17638329

Abstract

Bioassay-guided fractionation of the stems of Spatholobus suberectus led to the isolation of procyanidin B4 (= (+)-catechin-(4-->8)-(-)-epicatechin) (1) and (+)-catechin-(4-->8)-(+)-catechin-(4-->8)-(-)-epicatechin (2). These compounds, isolated before from other sources, were found to be highly potent inhibitors of DNA-topoisomerase-II (Topo-II)-mediated KDNA decatenation, with IC50 values of 22.5+/-2.3 and 21.9+/-2.2 nM, resp.

摘要

对密花豆茎进行生物测定导向的分级分离，得到了原花青素B4（=（+）-儿茶素-（4→8）-（-）-表儿茶素）（1）和（+）-儿茶素-（4→8）-（+）-儿茶素-（4→8）-（-）-表儿茶素（2）。这些之前从其他来源分离得到的化合物，被发现是DNA拓扑异构酶-II（Topo-II）介导的线粒体DNA解连环反应的高效抑制剂，IC50值分别为22.5±2.3和21.9±2.2 nM。