2. Academic Validation
  3. Synthesis of 9-substituted derivatives of berberine as anti-HIV agents

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

  • Eur J Med Chem. 2011 Apr;46(4):1045-9. doi: 10.1016/j.ejmech.2011.01.016.
Hardik S Bodiwala 1,  Sudeep Sabde,  Debashis Mitra,  Kamlesh Kumar Bhutani,  Inder Pal Singh
Affiliations

Affiliation

  • 1 Department of Natural Products, National Institute of Pharmaceutical Education and Research, Sector 67, SAS Nagar, Punjab 160062, India.
PMID: 21295891 DOI: 10.1016/j.ejmech.2011.01.016
Abstract

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.

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