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.
出处
《中国天然药物》
SCIE
CAS
CSCD
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)~~
