中文摘要：

目的研究黄芩苷抗丙型肝炎病毒（HCV）的活性。方法在体外无细胞系统中应用荧光共振能量转移法检测黄芩苷对HCV NS3/4A蛋白酶和NS3解旋酶的抑制活性;在Huh7.5细胞培养内分析其对野生型及临床常见耐药型HCV感染的抑制作用,并考察与目前临床应用的抗病毒药物联合抗HCV的活性。结果黄芩苷具有抑制HCV NS3/4A蛋白酶活性,但对NS3解旋酶无抑制作用。细胞培养内抗HCV活性测定显示,黄芩苷抑制野生型HCV复制的半数抑制浓度（EC（50））为（31.306±9.559）μmol/L,抑制蛋白酶抑制剂常见耐药突变A156T和D168V突变HCV复制的EC（50）分别为（53.175±19.141）μmol/L和（66.722±30.994）μmol/L,抑制多聚酶抑制剂常见耐药突变S282T突变HCV复制的EC（50）为（63.673±19.770）μmol/L。黄芩苷与多聚酶抑制剂索非布韦联用还具有协同抗病毒效果,但与具有相同作用机制的西咪匹韦联用有拮抗作用。结论黄芩苷具有抗HCV作用,其机制为抑制HCV蛋白酶,对蛋白酶抑制剂常见耐药突变病毒有效,与多聚酶抑制剂联用有协同抗病毒作用。

英文摘要：

Objective To evaluate the inhibitory activity of baicalin against hepatitis C virus（HCV） in vitro. Methods The effect of compounds against HCV NS3/4A protease and NS3 helicase was detected with fluorescence resonance energy transfer assay in cell free system. The anti-HCV activity on wild and mutant type HCV replication was evaluated in HCV-infected Huh7.5 cells at RNA and protein levels. Results Baicalin showed inhibitory activity on HCV NS3/4A protease with no effect on HCV NS3 helicase. In Huh7.5 cells, baicalin inhibited wild type of HCV replication with half maximum effective concentration（EC（50）） of（31.306 ± 9.559） μmol/L, and inhibited A156T, D168V and S282T drug-resistance mutant HCV replication with EC（50） of（53.175 ± 19.141） μmol/L,（66.722 ± 30.994） μmol/L, and（63.673 ± 19.770） μmol/L, respectively. Baicalin also showed synergistic effect against HCV with polymerase inhibitor sofosbuvir, but showed antagonistic action with protease inhibitor telaprevir. Conclusion Baicalin shows anti-HCV effect with the action mechanism of inhibiting HCV protease and it is effective for common drug-resistant mutant HCV and exerts synergistic antiviral effect with polymerase inhibitor.