Isolation, Identification, Quantification and Inhibitory Activity on HCV Protease of Coumarins from Viola yedoensis

Isolation, Identification, Quantification and Inhibitory Activity on HCV Protease of Coumarins from Viola yedoensis
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紫花地丁香豆素的分离、鉴定、定量及其对HCV蛋白酶的抑制活性

DOI:
10.13179/canchemtrans.2013.01.03.0025
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发表时间:
2013
期刊:
Canadian Chemical Transaction
影响因子:
--
通讯作者:
Chaomei Ma
Chaomei Ma
中科院分区:
其他
文献类型:
--
作者:
Mengyang Li;Liwei Wang;Jie Gao;Chaomei Ma

文献摘要

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相似文献

本研究以HCV蛋白酶(PR)为靶点,研究抗肝炎民族药植物紫花地丁(Viola yedoensis)的抗HCV活性,并对其活性成分进行鉴定。这导致了3个香豆素从植物中的分离和表征,使用各种色谱程序和光谱数据的解释与文献中报道的已有数据相比。其中一种化合物5,5′-二(6,7-二羟基香豆素)(一种二聚香豆素)对HCV NS 3/4A蛋白酶有很强的抑制作用,其IC 50值为0.5 μg/ml,对于非肽类蛋白结合剂来说,IC 50值非常低(预示着非常高的抑制活性)。该化合物具有抗HCV PR活性,有望成为开发新型抗HCV药物的分子模板。
This research was aimed at investigating the possible anti-HCV activity and identifying the responsible bioactive constituents of the anti-hepatitis ethnomedicinal plant Viola yedoensis, using HCV protease (PR) as target. This has led to the isolation and characterization of 3 coumarins from the plant, using various chromatographic procedures and the interpretation of spectral data in comparison with already existing data reported in literatures. One of the isolated compounds, 5, 5′-bi (6, 7dihydroxycoumarin), a dimeric coumarin, potently inhibited HCV NS3/4A protease with an IC50 value of 0.5 μg/ml, an uncommonly low IC50 value (portending an uncommonly high inhibitory activity) for a nonpeptide protein binder. This dicoumarin, hereby for the first time reported for its anti-HCV PR activity, could become a molecular template for the development of novel anti-HCV drugs.
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发表时间: 1963-10
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