Antimalarial and Antiproliferative Cassane Diterpenes of Caesalpinia sappan

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• 作者：Guoxu Ma ; Haifeng Wu ; Deli Chen ; Nailiang Zhu ; Yindi Zhu ; Zhonghao Sun ; Pengfei Li ; Junshan Yang ; Jingquan Yuan ; Xudong Xu
• 刊名：Journal of Natural Products
• 出版年：2015
• 出版时间：October 23, 2015
• 年：2015
• 卷：78
• 期：10
• 页码：2364-2371
• 全文大小：321K
• ISSN：1520-6025

文摘

Bioassay-guided fractionation of a methanol extract of the seeds of Caesalpinia sappan led to the isolation of 12 new cassane-type diterpenes, caesalsappanins A鈥揕 (1鈥?b>12). Their structures were elucidated on the basis of NMR and HRESIMS analysis, and the absolute configuration of compound 1 was determined by single-crystal X-ray crystallography. All isolated compounds were tested against a chloroquine-resistant Plasmodium falciparum strain for antiplasmodial activities and against a small panel of human cancer cell lines for antiproliferative activities. Compounds 7 and 8 displayed antimalarial activity against the chloroquine-resistant K1 strain of P. falciparum with IC₅₀ values of 0.78 and 0.52 渭M and selectivity indices of 17.6 and 16.4, respectively. Compound 10 showed antiproliferative activity against the KB cancer cell line with an IC₅₀ value of 7.4 渭M.