Specific Plant Terpenoids and Lignoids Possess Potent Antiviral Activities against Severe Acute Respiratory Syndrome Coronavirus

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• 作者：Chih-Chun Wen ; Yueh-Hsiung Kuo ; Jia-Tsrong Jan ; Po-Huang Liang ; Sheng-Yang Wang ; Hong-Gi Liu ; Ching-Kuo Lee ; Shang-Tzen Chang ; Chih-Jung Kuo ; Shoei-Sheng Lee ; Chia-Chung Hou ; Pei-Wen Hsiao ; Shih-Chang
• 刊名：Journal of Medicinal Chemistry
• 出版年：2007
• 出版时间：August 23, 2007
• 年：2007
• 卷：50
• 期：17
• 页码：4087 - 4095
• 全文大小：314K
• 年卷期：v.50,no.17(August 23, 2007)
• ISSN：1520-4804

文摘

In this study, 221 phytocompounds were evaluated for activity against anti-severe acute respiratory syndromeassociated coronavirus (SARS-CoV) activities using a cell-based assay measuring SARS-CoV-inducedcytopathogenic effect on Vero E6 cells. Ten diterpenoids (1-10), two sesquiterpenoids (11 and 12), twotriterpenoids (13 and 14), five lignoids (15-19), curcumin (20), and reference controls niclosamide (21)and valinomycin (22) were potent inhibitors at concentrations between 3.3 and 10 M. The concentrationsof the 22 compounds to inhibit 50% of Vero E6 cell proliferation (CC₅₀) and viral replication (EC₅₀) weremeasured. The selective index values (SI = CC₅₀/EC₅₀) of the most potent compounds 1, 5, 6, 8, 14, and16 were 58, >510, 111, 193, 180, and >667, respectively. Betulinic acid (13) and savinin (16) werecompetitive inhibitors of SARS-CoV 3CL protease with K_i values = 8.2 ± 0.7 and 9.1 ± 2.4 M, respectively.Our findings suggest that specific abietane-type diterpenoids and lignoids exhibit strong anti-SARS-CoVeffects.