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来自毒大戟的具有选择性细胞毒性的二萜类化合物。

Selectively cytotoxic diterpenes from Euphorbia poisonii.

作者信息

Fatope M O, Zeng L, Ohayaga J E, Shi G, McLaughlin J L

机构信息

Department of Medicinal Chemistry and Pharmacognosy, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, Indiana 49707, USA.

出版信息

J Med Chem. 1996 Feb 16;39(4):1005-8. doi: 10.1021/jm950509i.

Abstract

Bioactivity-guided fractionation of the latex of Euphorbia poisonii Pax. (Euphorbiaceae) led to the isolation and characterization of a new tigliane diterpene, 12-deoxyphorbol 13-(9,10-methylene)undecanoate (3), together with five known diterpenes (1,2,4-6). When evaluated for cytotoxicity in a panel of six human solid tumor cell lines, the diterpene esters, 1-3, 5, and 6, were selectively cytotoxic for the human kidney carcinoma (A-498) cell line with potencies for 2 and 3 exceeding that of adriamycin by ten thousand times. Details of the isolations, structural analyses, and cytotoxic activities are described.

摘要

对毒大戟(大戟科)乳汁进行生物活性导向分离,得到一种新的大戟烷二萜12-脱氧佛波醇13-(9,10-亚甲基)十一烷酸酯(3)以及五种已知二萜(1、2、4 - 6),并对其进行了表征。在六种人类实体瘤细胞系中评估细胞毒性时,二萜酯1 - 3、5和6对人肾癌(A - 498)细胞系具有选择性细胞毒性,其中化合物2和3的效力比阿霉素高一万倍。本文描述了分离、结构分析及细胞毒性活性的详细情况。

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