Evaluating the inhibitory effect of eight compounds from Daphne papyracea against the NS3/4A protease of hepatitis C virus

Evaluating the inhibitory effect of eight compounds from Daphne papyracea against the NS3/4A protease of hepatitis C virus
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DOI:
10.1080/14786419.2018.1519825
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发表时间:
2018-11
影响因子:
2.2
通讯作者:
Ying Wei;Jian Yang;Meena Kishore Sakharkar;Xia Wang;Qin Liu;Jiang Du;Jing-Jie Zhang
Ying Wei;Jian Yang;Meena Kishore Sakharkar;Xia Wang;Qin Liu;Jiang Du;Jing-Jie Zhang
中科院分区:
化学3区
文献类型:
--
作者:
Ying Wei;Jian Yang;Meena Kishore Sakharkar;Xia Wang;Qin Liu;Jiang Du;Jing-Jie Zhang

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摘要丙型肝炎病毒(HCV)感染是一个全球性的威胁人类健康的估计175万例新病例在2015年。我们前期的研究表明,纸莎草乙酸乙酯提取物对HCV NS 3/4A蛋白酶具有抑制作用,并从提取物中鉴定出8个化合物。在这项研究中,我们调查了8种化合物中的哪一种负责提取物对HCV NS 3/4A蛋白酶的抑制作用。从分子对接和酶抑制的研究,(+)-松萝酸被证明是最有效的化合物,并可用于开发新的抗HCV药物的先导化合物。图形摘要
Abstract Hepatitis C virus (HCV) infection is a global threat to human health with an estimated 1.75 million new cases in 2015. Our previous studies showed that the ethyl acetate extraction of Daphne papyracea exhibited an inhibitory effect towards the HCV NS3/4A protease and eight compounds were identified from the extract. In this study, we investigated which of the eight compounds was responsible for the inhibitory effect of the extract against the HCV NS3/4A protease. From both molecular docking and enzyme inhibition studies, (+)-usnic acid was shown to be the most active compound and could be used as a lead compound in developing novel anti-HCV agents. Graphical Abstract