解放军医学杂志2011，Vol.36Issue(9)：893-896,4.
抗乙肝病毒新药Bay41-4109在HBV转基因小鼠中的药效学研究
Pharmacodynamic study of Bay41-4109 in HBV transgenic mouse model
摘要
Abstract
Objective To study the pharmacodynamics of Bay41-4109, a novel anti-HBV compound, in HBV transgenic mouse model. Methods specific pathogen free (SPF) level TgM(HBV Dl. 3)mice were divided into 3 groups: Bay41-4109 group [30mg/(kg · D)], lamivudine group [30mg/(kg · D)] and vehicle group (0. 5% sodium carboxymethycellulose). With 32 in each. Antiviral effect of Bay41-4109 was tested in HBV transgenic mice including the analysis of HBcAg changes in liver tissue by immunohistochemistry, and changes in HBV DNA in liver and serum by quantitative real time PCR analysis. Serum transaminase (ALT and AST) and body weight were assayed to evaluate the safety of the compound. Results Oral Bay41-4109 significantly reduced the number of HBV core antigen (HBcAg) positive cell nucleus· Average area of HBcAg positive cell nucleus and the rate of OD compared with vehicle group after 50 days treatment (P<0.05). On the 64th day, all the three indicates showed no substantial difference in these three groups. Lamivudine treatment had no obvious effect on HBcAg compared with vehicle group (P>0.05). However, Bay41-4109 could not significantly reduce HBV-specific DNA in HBV transgenic mice, both in liver and plasma. No significant impact was found on ALT, AST and body weigh of Bay41-4109-treated mice. Conclusions Bay41-4109 can more effectively reduce cytoplasmic HBcAg in liver sections than lamivudine. It is suggested that Bay41-4109, a different mode of action from lamivudine, represents a promising anti-HBV drug candidate with good antiviral effect and safety.关键词
抗病毒药/小鼠,转基因/肝炎病毒,乙型Key words
antiviral agents/ mice, transgenict Hepatitis B virus分类
医药卫生引用本文复制引用
李秀梅,陈阳述,刘光泽,黎经纬,陈媚娟,周军辉,孔祥平..抗乙肝病毒新药Bay41-4109在HBV转基因小鼠中的药效学研究[J].解放军医学杂志,2011,36(9):893-896,4.基金项目
“艾滋病和病毒性肝炎等重大传染病防治”科技重大专项“十一五”课题资助(2008ZX10002-011) （2008ZX10002-011）
