四个小檗碱类化合物的体外抗HIV-1活性  

Anti-HIV-1 Activities of Four Berberine Compounds in vitro

作　　者：杨柳萌[1] 王睿睿[1] 李晶晶[2] 李耐三[2] 郑永唐[1] 

机构地区：[1]中国科学院昆明动物研究所动物模型和人类疾病机理重点实验室分子免疫药理学实验室,昆明650223 [2]中国药科大学药理教研室,南京210009

出　　处：《中国天然药物》2007年第3期225-228,共4页

基　　金："十五"国家科技攻关计划项目(2004BA719A14);云南省科技攻关计划(2004NG12)资助课题;中国科学院知识创新工程重要方向项目(KSCX1-YW-R-24;KSCX1-YW-R-15)~~

摘　　要：目的:研究小檗碱和巴马汀母核上己基的引入对化合物抗HIV-1活性的影响,并比较结构相似的小檗碱和巴马汀抗HIV-1活性的差异。方法:考察4个化合物对重组HIV-1RT活性、HIV-1复制和细胞毒性的影响。结果:小檗碱和巴马汀有较强的体外抑制HIV-1重组逆转录酶活性,EC50分别是63.1和44.52μg.mL-1;己基巴马汀有一定的抗HIV-1活性,合胞体抑制的EC50是0.08μg.mL-1,治疗指数为11.38;巴马汀对各种细胞系的细胞毒性较其他3种化合物小。结论:己基巴马汀有一定的抗HIV-1活性,己基的引入可能改变了其作用机制,提示构效关系的研究将为寻找高效低毒的天然化合物提供实验依据。AIM： To study the effects of 13-hexyl substituted berberine and palmatine on anti-HIV-1 activities, and for the purpose of comparison, activities of these analogs were tested. METHODS： The effects of four compounds on recombirrant HIV-1 RT activity, HIV-1 replication and cytotoxicity were observed. RESULTS： Both berberine and palmatine have shown an inhibitory effect on recombinant HIV-1 RT in vitro. The EC50 of berberine and palmatine were 63.1 and 44.52μg·mL^-1, respectively. 13-hexylpalmatine showed better activity against the HIV-1 than the other compounds. Hexylpalmatine inhibited HIV-1 induced syncytium formation at an EC50 of 0.08 μg·mL^-1 and therapeutic index （TI） was 11.38; Palmatine exhibited lower cytotoxicity against various cell lines than three other compounds. CONCLUSION： 13-hexylpalmatine has been an effective anti-HIV-1 agent, and 13-hexyl substituted palmatine may change its mechanism of action. These results suggest that structure-activity relationship studies play an important role in anti-HIV-1 drug screening. The study of the structure-function relationship may help us to identify promising natural products.

关 键 词：小檗碱 巴马汀 抗HIV-1活性 构效关系 

分 类 号：R285.5[医药卫生—中药学]