HIV-1 Reverse Transcriptase Inhibitor fromPhyllanthus niruri

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Abstract
An aqueous extract of Phyllanthus niruri (Euphorbiaceae) inhibited human immunodeficiency virus type-1 reverse transcriptase (HIV-1-RT). The inhibitor against HIV-1-RT in this plant was purified by combination of three column chromatographies, Sephadex LH-20, cellulose, and reverse-phase high-performance liquid chromatography. The inhibitor was then identified by nuclear magnetic resonance (NMR) spectra as repandusinic acid A monosodium salt (RA) which was originally isolated from Mallotus repandus. The 50% inhibitory doses (ID50) of RA on HIV-1-RT and DNA polymerase α(from HeLa cells) were 0.05 μM and 0.6 μM, respectively, representing approximately a 10-fold more sensitivity of HIV-1-RT compared with DNA polymerase α. RA was shown to be a competitive inhibitor with respect to the template-primer while it was a noncompetitive inhibitor with respect to the substrate. RA as low as 10.1 μM inhibited HIV-1-induced cytopathogenicity in MT-4 cells. In addition, 4.5 μM of RA inhibited HIV-1-induced giant cell formation of SUP-T1 approximately 50%. RA (2.5 μM) inhibited up to 90% of HIV-1 specific p24 antigen production in a Clone H9 cell system.

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