Novel gold(I) phosphine compounds inhibit HIV-1 enzymes

Show simple item record Fonteh, Pascaline Nanga Meyer, Debra 2010-04-13T06:26:39Z 2010-04-13T06:26:39Z 2009-08
dc.description.abstract The increasing incidence of human immunodeficiency virus (HIV) infection and the associated acquired immune deficiency syndrome (AIDS) mortality rates as well as the sometimes severe side effects of highly active anti retroviral therapy (HAART) warrants the continuous search for new, less toxic drug candidates. The anti-HIV activity (inhibition of reverse transcriptase-RT and protease-PR in direct enzyme assays) of eleven gold(I) phosphine compounds are reported here. Uptake of the compounds by peripheral blood mononuclear cells (PBMCs) was demonstrated by inductively coupled plasma atomic emission spectroscopy (ICP-AES) while the effect of the compounds on cell viability was assessed using flow cytometry with annexin V and propidium iodide (PI). Of the 11 gold compounds tested, 7 significantly (p o 0.05) inhibited RT activity at concentrations of 25 and 250 mM while 3 compounds significantly inhibited its activity at 6.25 mM. In the anti-protease assay, 4 of the compounds significantly inhibited the enzyme (p o 0.05) at 100 mM. All of the compounds were taken up by PBMCs (demonstrated by ICP-AES) and were non toxic to these cells at clinically tolerable concentrations. The potential of these novel gold(I) phosphine compounds as anti-HIV agents is therefore promising and worthy of further investigation. en
dc.identifier.citation Fonteh, P & Meyer, D 2009, 'Novel gold(I) phosphine compounds inhibit HIV-1 enzymes', Metallomics, vol. 1, no. 5, pp. 427-433. [] en
dc.identifier.issn 1756-5901
dc.identifier.other 10.1039/b909036c
dc.language.iso en en
dc.publisher Royal Society of Chemistry en
dc.rights © The Royal Society of Chemistry 2009 en
dc.subject Novel gold(I) phosphine en
dc.subject Anti-HIV agents en
dc.subject.lcsh HIV infections en
dc.subject.lcsh AIDS (Disease) -- Treatment -- Research en
dc.subject.lcsh Highly active antiretroviral therapy -- Side effects en
dc.subject.lcsh HIV (Viruses) -- Enzymes en
dc.subject.lcsh Phosphine en
dc.title Novel gold(I) phosphine compounds inhibit HIV-1 enzymes en
dc.type Article en

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