岩白菜属中的细胞毒 clerodane 二萜。

Cytotoxic clerodane diterpenes from Casearia rupestris.

机构信息

Institute of Chemistry, Nucley of Bioassay, Biosynthesis and Ecophysiology of Natural Products (NuBBE), São Paulo State University, UNESP, C.P. 14801-970, Araraquara, SP, Brazil.

出版信息

J Nat Prod. 2011 Apr 25;74(4):776-81. doi: 10.1021/np100840w. Epub 2011 Mar 7.

DOI:10.1021/np100840w

PMID:21381705

Abstract

Four new clerodane diterpenes, casearupestrins A-D (1-4), were isolated from the leaves of Casearia rupestris. Compounds 1 and 4 were acetylated to yield 2,7-di-O-acetylcasearupestrin A (5) and 2,6-di-O-acetylcasearupestrin D (6). All compounds were evaluated for cytotoxicity against a small panel of human cancer cell lines. Casearupestrin A (1) exhibited the most potent activity against MDA/MB-435 (human melanoma) and SF-295 (human glioblastoma) cells, superior to that of the standard drug doxorubicin.

摘要

从 Casearia rupestris 的叶子中分离得到了四个新的 clerodane 二萜，分别命名为 casearupestrins A-D（1-4）。化合物 1 和 4 经乙酰化得到 2,7-二-O-乙酰基 casearupestrin A（5）和 2,6-二-O-乙酰基 casearupestrin D（6）。所有化合物均对一组人癌细胞系进行了细胞毒性评价。Casearupestrin A（1）对 MDA/MB-435（人黑色素瘤）和 SF-295（人神经胶质瘤）细胞的活性最强，优于标准药物阿霉素。