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马利筋中强心甾和强心甾糖苷的细胞毒性。

Cytotoxicity of cardenolides and cardenolide glycosides from Asclepias curassavica.

作者信息

Li Jun-Zhu, Qing Chen, Chen Chang-Xiang, Hao Xiao-Jiang, Liu Hai-Yang

机构信息

State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650204, PR China.

出版信息

Bioorg Med Chem Lett. 2009 Apr 1;19(7):1956-9. doi: 10.1016/j.bmcl.2009.02.045. Epub 2009 Feb 14.

Abstract

A new cardenolide, 12beta,14beta-dihydroxy-3beta,19-epoxy-3alpha-methoxy-5alpha-card-20(22)-enolide (6), and a new doubly linked cardenolide glycoside, 12beta-hydroxycalotropin (13), together with eleven known compounds, coroglaucigenin (1), 12beta-hydroxycoroglaucigenin (2), calotropagenin (3), desglucouzarin (4), 6'-O-feruloyl-desglucouzarin (5), calotropin (7), uscharidin (8), asclepin (9), 16alpha-hydroxyasclepin (10), 16alpha-acetoxycalotropin (11), and 16alpha-acetoxyasclepin (12), were isolated from the aerial part of ornamental milkweed, Asclepias curassavica and chemically elucidated through spectral analyses. All the isolates were evaluated for their cytotoxic activity against HepG2 and Raji cell lines. The results showed that asclepin (9) had the strongest cytotoxic activity with an IC(50) value of 0.02 microM against the two cancer cell lines and the new compound 13 had significant cytotoxic activity with IC(50) values of 0.69 and 1.46 microM, respectively.

摘要

从观赏马利筋(Asclepias curassavica)的地上部分分离得到一种新的强心甾内酯,12β,14β - 二羟基 - 3β,19 - 环氧 - 3α - 甲氧基 - 5α - 强心甾 - 20(22) - 烯醇内酯(6),以及一种新的双连接强心甾内酯糖苷,12β - 羟基牛角瓜苷元(13),同时还得到11种已知化合物,即科罗格劳苷元(1)、12β - 羟基科罗格劳苷元(2)、牛角瓜苷元(3)、去葡萄糖乌沙苷(4)、6'-O - 阿魏酰基 - 去葡萄糖乌沙苷(5)、牛角瓜苷(7)、乌沙毒苷(8)、马利筋苷(9)、16α - 羟基马利筋苷(10)、16α - 乙酰氧基牛角瓜苷(11)和16α - 乙酰氧基马利筋苷(12),并通过光谱分析对其进行了化学结构解析。对所有分离得到的化合物进行了针对肝癌细胞系HepG2和人Burkitt淋巴瘤细胞系Raji的细胞毒性活性评估。结果表明,马利筋苷(9)对这两种癌细胞系具有最强的细胞毒性活性,IC(50)值为0.02 μM,新化合物13也具有显著的细胞毒性活性,IC(50)值分别为0.69和1.46 μM。

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