Cytotoxic Evaluation against Breast Cancer Cells of Isoliquiritigenin Analogues from Spatholobus suberectus and Their Synthetic Derivatives

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• 作者：Fu Peng ; Chun-Wang Meng ; Qin-Mei Zhou ; Jian-Ping Chen ; Liang Xiong
• 刊名：Journal of Natural Products
• 出版年：2016
• 出版时间：January 22, 2016
• 年：2016
• 卷：79
• 期：1
• 页码：248-251
• 全文大小：264K
• ISSN：1520-6025

文摘

Five isoliquiritigenin analogues, including a new methylene-bridged bischalcone (1), were isolated from Spatholobus suberectus. Cytotoxicity screening of these isolates and several synthetic derivatives indicated that the introduction, removal, position modification, or glycosylation of hydroxy groups in isoliquiritigenin did not improve the resultant cytotoxicity against the MCF-7 and MDA-MB-231 human breast cancer cell lines. In addition, cyclization of OH-2′ chalcones or reduction of the α,β-unsaturated carbonyl double bond decreased such cytotoxicity substantially. However, methylation of hydroxy groups resulted in a marked increase in such cytotoxic activity. Among these active isoliquiritigenin analogues, 3′,4′,5′,4″-tetramethoxychalcone (3h) was obtained as a compound with promising cytotoxic activity.