Zusammenfassung
Phyllanthus amarus derived preparations were previously shown to inhibit RT inhibitor-resistant HIV variants as efficiently as wildtype strains. The drugs target different steps of the HIV life cycle, thereby presenting multiple antiviral activities. Here we show that a water/alcohol extract blocks HIV-1 attachment and the HIV-1 enzymes integrase, reverse transcriptase and protease to different ...
Zusammenfassung
Phyllanthus amarus derived preparations were previously shown to inhibit RT inhibitor-resistant HIV variants as efficiently as wildtype strains. The drugs target different steps of the HIV life cycle, thereby presenting multiple antiviral activities. Here we show that a water/alcohol extract blocks HIV-1 attachment and the HIV-1 enzymes integrase, reverse transcriptase and protease to different degrees. A gallotannin containing fraction and the isolated ellagitannins geraniin and corilagin were shown to be the most potent mediators of these antiviral activities. The P amarus derived preparations blocked the interaction of HIV-1 gp120 with its primary cellular receptor CD4 at 50% inhibitory concentrations of 2.65 (water/alcohol extract) to 0.48 mug/ml (geraniin). Inhibition was also evident for the HIV-1 enzymes integrase (0.48-0.16 mug/ml), reverse transcriptase (8.17-2.53 mug/ml) and protease (21.80-6.28 mug/ml). In order to prove the in vivo relevance of these biological activities, plant material was administered orally to volunteers and a potent anti-HIV activity in blood could be demonstrated. Sera at a final concentration of 5% reduced HIV replication by more than 30%. These results support the conclusion that P amarus has inhibitory effects on HIV not only in vitro but also in vivo. (C) 2004 Elsevier B.V. All rights reserved.
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