Catalytic Inhibition of Eukaryotic Topoisomerases I and II by Flavonol Glycosides Extracted from Vicia faba and Lotus edulis

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• 作者：Maria Tselepi ; Evaggelia Papachristou ; Aikaterini Emmanouilidi ; Apostolos Angelis ; Nektarios Aligiannis ; Alexios-Leandros Skaltsounis ; Demetrios Kouretas ; Kalliopi Liadaki
• 刊名：Journal of Natural Products
• 出版年：2011
• 出版时间：November 28, 2011
• 年：2011
• 卷：74
• 期：11
• 页码：2362-2370
• 全文大小：460K
• 年卷期：v.74,no.11(November 28, 2011)
• ISSN：1520-6025

文摘

Topoisomerases are essential enzymes involved in all processes of DNA metabolism, and their inhibitors have been identified as potential anticancer agents. The present study examined the effect of nine polyphenolic compounds derived from parts of two unique varieties of the Leguminosae, Vicia faba and Lotus edulis, on the activity of eukaryotic topoisomerases. We identified polyphenolic compounds that act as catalytic inhibitors of wheat germ topoisomerase I (IC₅₀: 120鈥?50 渭M), human topoisomerase I (IC₅₀: 110鈥?60 渭M), and human topoisomerase II (IC₅₀: 240鈥?00 渭M) activities. Some compounds inhibited all enzymatic activities to a similar extent, while others exhibited specificity toward individual enzymes. The strongest catalytic inhibitor of all the examined enzymes was a kaempherol glycoside with an acetyl group linked to a sugar moiety. In addition, this compound inhibited the growth of human cancer cell lines MCF7, HeLa, and HepG2. The inhibition of topoisomerase I and II activities observed by the specific compounds possibly implies a role as potential agents in the prevention and therapy of cancer.