合成 9-取代衍生物作为抗 HIV 药物的小檗碱。
Synthesis of 9-substituted derivatives of berberine as anti-HIV agents.
机构信息
Department of Natural Products, National Institute of Pharmaceutical Education and Research, Sector 67, SAS Nagar, Punjab 160062, India.
出版信息
Eur J Med Chem. 2011 Apr;46(4):1045-9. doi: 10.1016/j.ejmech.2011.01.016. Epub 2011 Jan 21.
Naturally occurring protoberberine alkaloids, berberine and berberrubine along with 9-substituted derivatives of berberine were assessed for the anti-human immunodeficiency virus (HIV) activity. Berberine was found to be the most active compound with an EC(50) of 0.13 μM against HIV-1 NL4.3 virus in CEM-GFP cell lines. Berberrubine and two other compounds were found to be less active than berberine, at the same time they were less toxic than berberine. Enzyme based assay suggested that the anti-HIV activity of berberine and its analogs might be due to RTase inhibitory activity and some additional mechanisms.
天然原小檗碱生物碱，小檗碱和小檗红碱以及小檗碱的 9-取代衍生物被评估了抗人类免疫缺陷病毒 (HIV) 的活性。小檗碱被发现是最具活性的化合物，在 CEM-GFP 细胞系中对 HIV-1 NL4.3 病毒的 EC(50)为 0.13 μM。小檗红碱和另外两种化合物的活性比小檗碱低，同时它们的毒性比小檗碱低。基于酶的测定表明，小檗碱及其类似物的抗 HIV 活性可能是由于 RTase 抑制活性和一些其他机制。
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