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中药“升麻”(Cimicifuga dahurica)中的细胞毒性环阿尔廷三萜。

Cytotoxic cycloartane triterpenes of the traditional Chinese medicine "shengma" (Cimicifuga dahurica).

机构信息

State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, PR China.

出版信息

Planta Med. 2013 Jan;79(1):60-9. doi: 10.1055/s-0032-1328019. Epub 2012 Dec 5.

Abstract

Twelve new 9,19-cycloartane triterpenes (1-12), together with fourteen known compounds (13-26), were isolated from the roots of Cimicifuga dahurica. Their structures were determined by application of spectroscopic analyses and chemical methods. Biological evaluation of the compounds against human HL-60, SMMC-7721, A549, MCF-7, and SW-480 cell lines indicated that cimigenol-type glycosides (1-3, 19, and 20) showed broad-spectrum and moderate cytotoxicities, with IC50 values ranging from 4.2 to 14.5 µM. Meanwhile, cimigenol-type aglycones (6-8, 15, 16, and 18) exhibited broad-spectrum and week cytotoxicities, having IC50 values around 20 µM. In addition, the key points of the structure-activity relationships of aglycones with a cimigenol skeleton were discussed.

摘要

从升麻根中分离得到了 12 个新的 9,19-环阿尔廷三萜(1-12)和 14 个已知化合物(13-26)。通过光谱分析和化学方法确定了它们的结构。对这些化合物进行了对人 HL-60、SMMC-7721、A549、MCF-7 和 SW-480 细胞系的生物活性评估,结果表明,紫菀醇型糖苷(1-3、19 和 20)具有广谱和中等的细胞毒性,IC50 值范围为 4.2-14.5µM。同时,紫菀醇型苷元(6-8、15、16 和 18)具有广谱和较弱的细胞毒性,IC50 值约为 20µM。此外,讨论了具有紫菀醇骨架的苷元的结构-活性关系的要点。

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