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目的:研究不同剂型苦参素(肌肉注射用、静脉滴注用及口服用苦参素)体外抗乙型肝炎病毒(HBV)的作用及其作用机理。方法:以 HBsAg、HBeAg 及细胞存活率为观察指标,综合评价不同剂型苦参素体外抗2.2.15细胞 HBV 效果,进一步用荧光定量 PCR 方法测细胞内 HBV DNA、HBV RNA 及细胞上清HBV DNA 的拷贝数。结果:肌肉注射用苦参素的治疗指数(TI)>2,对 HBsAg 和 HBeAg 的 ID_(50)分别为2.5mg/ml 及3.2 mg/ml,CD_(50)为16.6 mg/ml,对细胞内、外 HBV DNA 及细胞内 HBV RNA 均有明显的剂量依赖型抑制作用(P<0.01)。结论:肌肉注射用苦参素有明显抗 HBV 作用,对 HBV 抑制位点可能在 HBVDNA 水平。
OBJECTIVE: To study the effect of different formulations of oxymatrine (intramuscular injection, intravenous infusion and oral oxymatrine) on hepatitis B virus (HBV) in vitro and its mechanism of action. Methods: HBsAg, HBeAg and cell viability were used as observation criteria to comprehensively evaluate the effect of different formulations of oxymatrine against HBV in 2.2.15 cells in vitro. HBV DNA, HBV RNA and cell supernatant HBV DNA were measured by fluorescence quantitative PCR. The number of copies. Results: The therapeutic index (TI) of oxymatrine for intramuscular injection was >2, the ID_(50) for HBsAg and HBeAg was 2.5 mg/ml and 3.2 mg/ml, and the CD_(50) was 16.6 mg/ml for cells. Internal and external HBV DNA and intracellular HBV RNA all had significant dose-dependent inhibition (P<0.01). Conclusion: The oxymatrine used for intramuscular injection has obvious anti-HBV effect, and the site of HBV inhibition may be at HBV DNA level.