Anti-SARS coronavirus 3C-like protease effects of Isatis indigotica root and plant-derived phenolic compounds

被引：436

作者：

Lin, CW ^{[1
]}

Tsai, FJ

Tsai, CH

Lai, CC

Wan, L

Ho, TY

Hsieh, CC

Chao, PDL

机构：

[1] China Med Univ Hosp, Dept Med Genet & Med Res, Taichung 404, Taiwan

[2] China Med Univ, Dept Med Lab Sci & Biotechnol, Taichung 404, Taiwan

[3] China Med Univ Hosp, Dept Lab Med, Clin Virol Lab, Taichung 404, Taiwan

[4] China Med Univ, Inst Chinese Med Sci, Taichung 404, Taiwan

[5] China Med Univ, Inst Integrat Chinese & Western Med, Taichung 404, Taiwan

[6] China Med Univ, Dept Pharm, Taichung 404, Taiwan

来源：

ANTIVIRAL RESEARCH | 2005年 / 68卷 / 01期

关键词：

SARS-coronavirus; 3C-like protease; Isatis indigotica root; phenolic compounds;

D O I：

10.1016/j.antiviral.2005.07.002

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The 3C-like protease (3CL(pro),) of SARS-coronavirus mediates the proteolytic processing of replicase polypeptides 1 a and 1 ab into functional proteins, becoming an important target for the drug development. In this study, Isatis indigotica root extract, five major compounds of I indigotica root, and seven plant-derived phenolic compounds were tested for anti-SARS-CoV 3CL(pro) effects using cell-free and cell-based cleavage assays. Cleavage assays with the 3CL(pro) demonstrated that IC50 values were in micromolar ranges for I indigotica root extract, indigo, sinigrin, aloe emodin and hesperetin. Sinigrin (IC50: 217 mu M) was more efficient in blocking the cleavage processing of the 3CL(pro), than indigo (IC50: 752 mu M) and beta-sitosterol (IC50: 1210 mu M) in the cell-based assay. Only two phenolic compounds aloe emodin and hesperetin dose-dependently inhibited cleavage activity of the 3CL(pro), in which the IC50 was 366 mu M for aloe emodin and 8.3 mu M for hesperetin in the cell-based assay. (c) 2005 Elsevier B.V. All rights reserved.

引用

页码：36 / 42

页数：7

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