Identification of natural compounds with antiviral activities against SARS-associated coronavirus.

Identification of natural compounds with antiviral activities against SARS-associated coronavirus.
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DOI:
10.1016/j.antiviral.2005.02.007
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发表时间:
2005-07
期刊:
影响因子:
7.6
通讯作者:
Tan X
Tan X
中科院分区:
医学2区
文献类型:
--
作者:
Li SY;Chen C;Zhang HQ;Guo HY;Wang H;Wang L;Zhang X;Hua SN;Yu J;Xiao PG;Li RS;Tan X

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采用3-(4,5-二甲基噻唑-2-基)-5-(3-羧基甲氧基苯基)-2-(4-磺基苯基)-2H-四氮唑内盐(MTS)法对200多种中草药提取物进行抗SARS冠状病毒活性筛选。其中4种提取物对SARS-CoV具有中等至强的抗病毒活性,半数有效浓度(EC 50)为2.4 ± 0.2 ~ 88.2 ± 7.7 μg/ml。四种植物中,石蒜的药效最强。为了识别活性组分,L.辐射提取物进行进一步的分级分离、纯化和CPE/MTS测定。该过程导致鉴定出单一物质石蒜碱作为抗SARS-CoV组分,其EC 50值为15.7 ± 1.2 nM。该化合物在细胞毒性试验中的CC 50值为14980.0 ± 912.0 nM,选择性指数(SI)大于900。结果表明,4种中药提取物和复方石蒜碱有可能成为抗SARS病毒新药的候选药物。
More than 200 Chinese medicinal herb extracts were screened for antiviral activities against Severe Acute Respiratory Syndrome-associated coronavirus (SARS-CoV) using 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium inner salt (MTS) assay for virus-induced cytopathic effect (CPE). Four of these extracts showed moderate to potent antiviral activities against SARS-CoV with 50% effective concentration (EC50) ranging from 2.4 ± 0.2 to 88.2 ± 7.7 μg/ml. Out of the four, Lycoris radiata was most potent. To identify the active component, L. radiata extract was subjected to further fractionation, purification, and CPE/MTS assays. This process led to the identification of a single substance lycorine as an anti-SARS-CoV component with an EC50 value of 15.7 ± 1.2 nM. This compound has a CC50 value of 14980.0 ± 912.0 nM in cytotoxicity assay and a selective index (SI) greater than 900. The results suggested that four herbal extracts and the compound lycorine are candidates for the development of new anti-SARS-CoV drugs in the treatment of SARS.
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