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从红树植物角果木中提取的多酚对 HCV 的抑制作用。

Inhibitory effects of polyphenols toward HCV from the mangrove plant Excoecaria agallocha L.

机构信息

State Key Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing 100191, PR China.

出版信息

Bioorg Med Chem Lett. 2012 Jan 15;22(2):1099-102. doi: 10.1016/j.bmcl.2011.11.109. Epub 2011 Dec 4.

Abstract

Four new polyphenols namely excoecariphenols A-D (1-4) were isolated from the Chinese mangrove plant Excoecaria agallocha L. together with 23 known phenolic compounds. The structures of new compounds were elucidated on the basis of extensive spectroscopic analyses including IR, MS, NMR, and CD data. Excoecariphenols A and B presented as the unusual flavane-based 1-thioglycosides. Part of the isolated polyphenols were tested against hepatitis C NS3-4A protease and HCV RNA in huh 7.5 cells. Excoecariphenol D, corilagin, geraniin, and chebulagic acid showed potential inhibition toward HCV NS3-4A protease with IC(50) values in a range of 3.45-9.03μM, while excoecariphenol D and corilagin inhibited HCV RNA in huh 7.5 cells significantly. A primary structure-activity relationship (SAR) is discussed.

摘要

从中国红树林植物桐花树(Excoecaria agallocha L.)中分离得到了 4 种新的多酚化合物,分别为 excoecariphenols A-D(1-4),此外还分离得到了 23 种已知的酚类化合物。新化合物的结构是基于广泛的光谱分析确定的,包括 IR、MS、NMR 和 CD 数据。Excoecariphenols A 和 B 呈现出不寻常的基于黄烷的 1-硫糖苷。部分分离得到的多酚化合物在 Huh 7.5 细胞中针对丙型肝炎 NS3-4A 蛋白酶和 HCV RNA 进行了测试。Excoecariphenol D、鞣花酸、没食子酸和诃黎酸对 HCV NS3-4A 蛋白酶具有潜在的抑制作用,IC50 值在 3.45-9.03μM 范围内,而 excoecariphenol D 和鞣花酸则显著抑制 Huh 7.5 细胞中的 HCV RNA。讨论了初步的结构-活性关系(SAR)。

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