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

被引：437
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.
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页码：36 / 42
页数：7
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