血根碱、白屈菜红碱衍生物的合成与体外抗HBV活性研究

发布时间：2018-04-23 09:00

本文选题：血根碱 + 白屈菜红碱　；参考：《中南药学》2014年06期

【摘要】：目的合成季铵类苯并菲啶生物碱血根碱(1)和白屈菜红碱(2)的衍生物,评价其体外抗HBV活性,初步探讨抗HBV活性。方法以血根碱和白屈菜红碱为原料,通过结构修饰获得衍生物,采用Hep G2.2.15细胞模型评价衍生物对HBsAg和HBeAg分泌抑制活性和HBV DNA复制的抑制活性。结果血根碱和白屈菜红碱对HBsAg、HBeAg和HBV DNA复制具有较高的抑制活性,但细胞毒性较高。氧化白屈菜红碱(6)对HBV DNA的复制具有一定的抑制作用(IC50=0.75 mmol·L-1),细胞毒性较白屈菜红碱明显降低(CC503.0 mmol·L-1)。6-乙氧基二氢血根碱(7)和6-乙氧基二氢白屈菜红碱(8)对HBsAg和HBeAg和HBV DNA复制具有一定的抑制活性。结论季铵类苯并菲啶生物碱具有显著的体外抗HBV活性,烯胺正离子结构单元对化合物的抗HBV活性产生重要的影响。
[Abstract]:Objective to synthesize the derivatives of quaternary ammonium benzophenidine alkaloids hemobase 1) and chrythrine 2) and to evaluate their anti- HBV activities in vitro and to explore their anti-HBV activities. Methods Derivatives were obtained by structural modification from root alkaloids and chrythrine. Hep G2.2.15 cell model was used to evaluate the inhibitory activity of derivatives on HBsAg and HBeAg secretion and HBV DNA replication. Results HBeAg and HBV DNA replication of HBeAg and HBV were inhibited by root alkaloids and chrythrine, but the cytotoxicity was higher. The cytotoxicity of HBV DNA was significantly lower than that of chrythrine (CC503.0 mmol L -1, 6 ethoxy dihydrohemodine 7) and 6 ethoxy dihydrocarythrine 8) on HBsAg, HBeAg and HBV DNA. Replication has certain inhibitory activity. Conclusion Quaternary ammonium benzophenidine alkaloids have significant anti- HBV activity in vitro, and enamine cationic structure unit has an important effect on the anti- HBV activity of the compounds.
【作者单位】：湖南农业大学作物种质创新与资源利用国家重点实验室培育基地;湖南中医药大学药学院;
【基金】：湖南中医药管理局科研项目(编号:201259) 湖南农业大学校青年科学基金(编号:11QN12)
【分类号】：R914;R373.21

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