Cytotoxic Lignans from Fruits of Cleistanthus indochinensis: Synthesis of Cleistantoxin Derivatives

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• 作者：Van Trinh Thi Thanh ; Van Cuong Pham ; Huong Doan Thi Mai ; Marc Litaudon ; Fran莽oise Gu茅ritte ; Pascal Retailleau ; Van Hung Nguyen ; Van Minh Chau
• 刊名：Journal of Natural Products
• 出版年：2012
• 出版时间：September 28, 2012
• 年：2012
• 卷：75
• 期：9
• 页码：1578-1583
• 全文大小：320K
• 年卷期：v.75,no.9(September 28, 2012)
• ISSN：1520-6025

文摘

Two new aryl-tetralin lignans, 1 and 2, were isolated from the fruits of Cleistanthus indochinensis by bioassay-guided purification. Their structures were determined by spectroscopic analysis including MS and 2D NMR. The absolute configurations of 1 and 2 were established from examination of their CD spectra. Compound 1 was cytotoxic against KB cells with an IC₅₀ value of 0.022 渭M, while compound 2 had weaker cytotoxicity, with an IC₅₀ value of 1.4 渭M. When tested against other cancer cell lines (MCF-7, MCF-7R, and HT29), 1 showed an IC₅₀ of 0.014 against MCF-7R cells and an IC₅₀ of 0.036 渭M against MCF-7 cells. A series of amide derivatives of a new lactone, homoderivatives of 1, were prepared. Of these derivatives, only compound 3 had weak cytotoxicity against KB cells.