Anti-SARS coronavirus 3C-like protease effects of Isatis indigotica root and plant-derived phenolic compounds.
Anti-SARS coronavirus 3C-like protease effects of Isatis indigotica root and plant-derived phenolic compounds.
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DOI：
10.1016/j.antiviral.2005.07.002
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发表时间：
2005-10
影响因子：
7.6
通讯作者：
Chao PD
中科院分区：
文献类型：
--
作者：
Lin CW;Tsai FJ;Tsai CH;Lai CC;Wan L;Ho TY;Hsieh CC;Chao PD
SARS冠状病毒的3C样蛋白酶（3CLpro）介导复制酶多肽1a和1ab的蛋白水解加工，成为药物开发的重要靶点。本研究对板蓝根提取物、板蓝根I.靛蓝根和七种植物来源的酚类化合物的抗SARS-CoV 3CLpro作用使用无细胞和基于细胞的裂解测定进行测试。用3CLpro进行的裂解试验表明，I.板蓝根提取物、靛蓝、黑芥子苷、芦荟大黄素、橙皮素。Sinigrin（IC50：在基于细胞的测定中，与靛蓝（IC 50：752 μM）和β-谷甾醇（IC 50：1210 μM）相比，β-谷甾醇（IC 50：217 μM）更有效地阻断3CLpro的裂解过程。只有两种酚类化合物芦荟大黄素和橙皮素剂量依赖性地抑制3CLpro的切割活性，其中在基于细胞的测定中，芦荟大黄素的IC 50为366 μM，橙皮素的IC 50为8.3 μM。
The 3C-like protease (3CLpro) of SARS-coronavirus mediates the proteolytic processing of replicase polypeptides 1a and 1ab 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 3CLpro effects using cell-free and cell-based cleavage assays. Cleavage assays with the 3CLpro demonstrated that IC50 values were in micromolar ranges for I. indigotica root extract, indigo, sinigrin, aloe emodin and hesperetin. Sinigrin (IC50: 217 μM) was more efficient in blocking the cleavage processing of the 3CLpro than indigo (IC50: 752 μM) and beta-sitosterol (IC50: 1210 μM) in the cell-based assay. Only two phenolic compounds aloe emodin and hesperetin dose-dependently inhibited cleavage activity of the 3CLpro, in which the IC50 was 366 μM for aloe emodin and 8.3 μM for hesperetin in the cell-based assay.
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影响因子：
5.4
作者：
Yi, L;Li, ZQ;Xu, XJ
通讯作者：
Xu, XJ
影响因子：
7.6
作者：
Semple, SJ;Pyke, SM;Flower, RLP
通讯作者：
Flower, RLP
DOI：
10.1016/j.bbrc.2004.04.083
发表时间：
2004-06-04
影响因子：
3.1
作者：
Yamamoto N;Yang R;Yoshinaka Y;Amari S;Nakano T;Cinatl J;Rabenau H;Doerr HW;Hunsmann G;Otaka A;Tamamura H;Fujii N;Yamamoto N
通讯作者：
Yamamoto N
DOI：
10.1111/j.1365-2672.1995.tb00931.x
发表时间：
1995-08-01
期刊：
JOURNAL OF APPLIED BACTERIOLOGY
影响因子：
--
作者：
BRABBAN, AD;EDWARDS, C
通讯作者：
EDWARDS, C
影响因子：
7.3
作者：
McGovern, SL;Shoichet, BK
通讯作者：
Shoichet, BK