Synthesis of 9-substituted derivatives of berberine as anti-HIV agents

被引：95

作者：

Bodiwala, Hardik S. ^{[1
]}

Sabde, Sudeep ^{[2
]}

Mitra, Debashis ^{[2
]}

Bhutani, Kamlesh Kumar ^{[1
]}

Singh, Inder Pal ^{[1
]}

机构：

[1] NIPER, Dept Nat Prod, Sas Nagar 160062, Punjab, India

[2] NCCS, Pune 411007, Maharashtra, India

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2011年 / 46卷 / 04期

关键词：

Berberine; Berberrubine; Anti-HIV; Reverse transcriptase; DNA-BINDING AFFINITIES; PROTOBERBERINE ALKALOIDS; ANTIBACTERIAL ACTIVITY; DIMERS; BERBERRUBINE; INHIBITORS; ANALOGS;

D O I：

10.1016/j.ejmech.2011.01.016

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 mu M 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. (C) 2011 Elsevier Masson SAS. All rights reserved.

引用

页码：1045 / 1049

页数：5

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