小檗碱衍生物HB-13体外抗单纯疱疹病毒的研究

目的 探讨小檗碱衍生物HB-13及其前体小檗碱体外抗HSV-1和HSV-2的活性.方法 利用Vero细胞体外培养模型,以阿昔洛韦(ACV)为对照药,通过观察细胞病变效应,检测HB-13和小檗碱的细胞毒性、HSV-1和HSV-2液的病毒滴度及药物抑制病毒致细胞病变效应.结果 HB-13、小檗碱和阿昔洛韦的半数中毒质量浓度(TC50)分别为31.99,380和>800 μg/mL;对HSV-1的半数抑制质量浓度(IC₅₀)分别为1.328,>100和0.443 μg/mL,治疗指数分别为24.09,<3.80和>1805.87;对HSV-2的IC₅₀分别为1.344,>100和0.679μg/mL;治疗指数分别为23.80,<3.80和>1178.20.结论 HB-13具有明显的抗HSV作用,而小檗碱无实用抗HSV活性.

In vitro Antiviral activity of a berberine derivant HB-13 against herpes simplex virus

Objective To evaluate the in vitro antiviral activity of HB-13, a compound derivant from berberine and its prodrug berberine, against herpes simplex virus type 1 （HSV-1） and type 2 （HSV-2）. Methods Vero cells were cultured in vitro and infected with HSV. Then, various concentrations of HB-13, berberine, and aciclovir were used to treat these infected cells. The cytopathic effect was observed to determine the antiviral effects and cytotoxicity of HB-13 and berberine. Results For HB-13, berberine and acyclovir, the half toxicity concentration （TC50） to Vero cells was 31.99, 380 and more than 800 μg/mL, respectively; the average half inhibitory concentration （IC50） against HSV-1 was 1.328, more than 100, and 0.443 μg/mL, respectively, the treatment index （TI） against HSV-1 was 24.09, less than 3.80, and more than 1805.87, respectively; the IC50 against HSV-2 was 1.344, more than 100, and 0.679 μg/mL, respectively, the TI against HSV-2 was 23.80, less than 3.80 and more than 1178.20, respectively. Conclusion HB-13 possesses marked antiviral activity against HSV-1 and HSV-2 in vitro , while berberine does not.