HCV-NS3/4A Protease Inhibitory Iridoid Glucosides and Dimeric Foliamenthoic Acid Derivatives from Anarrhinum orientale

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• 作者：Riham Salah El Dine ; Azza R. Abdel Monem ; Ali M. El-Halawany ; Masao Hattori ; Essam Abdel-Sattar
• 刊名：Journal of Natural Products
• 出版年：2011
• 出版时间：May 27, 2011
• 年：2011
• 卷：74
• 期：5
• 页码：943-948
• 全文大小：864K
• 年卷期：v.74,no.5(May 27, 2011)
• ISSN：1520-6025

文摘

Four new compounds were isolated from the methanol extract of the aerial parts of Anarrhinum orientale: 6鈥?O-cinnamoylmussaenosidic acid (1), 6鈥?O-cinnamoyl-8-O-(6鈥测€测€?O-cinnamoylglucopyranosyl)mussaenosidic acid (2), (2E,6E)-8-{[(2E,6E)-8-hydroxy-2,6-dimethylocta-2,6-dienoyl]oxy}-2,6-dimethylocta-2,6-dienoic acid (3), and (2E,6E)-8-{[(2E,6E)-8-acetoxy-2,6-dimethylocta-2,6-dienoyl]oxy}-2,6-dimethylocta-2,6-dienoic acid (4). The known 8-O-cinnamoylmussaenosidic acid (5) was also identified. All five compounds were tested for inhibition of the hepatitis C virus (HCV) protease. Compounds 1 and 5 exhibited moderate activity, while 2 and 3 showed weak effects. No inhibitory activity on the human serine protease was observed for any of these compounds, which may infer the selectivity toward the viral protease. A computational docking study of the isolated compounds against HCV protease was used to formulate a hypothetical mechanism for the inhibitory activity of the active compounds on the enzymes tested.