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Pathog Dis. 2017 Aug 31;75(6). doi: 10.1093/femspd/ftx065.

Multi-target activity of Hemidesmus indicus decoction against innovative HIV-1 drug targets and characterization of Lupeol mode of action.

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Department of Life and Environmental Sciences, University of Cagliari, 09042 Monserrato, Italy.
Department of Pharmacy and Biotechnologies, University of Bologna, 40126 Bologna, Italy.
Department of Molecular Medicine, University of Padova, 35121 Padova, Italy.
Department of Life Sciences and Biotechnology, University of Ferrara, 44100 Ferrara, Italy.
Genetics and Biomedical Research institute, National Research Council (CNR), 09042 Monserrato, Cagliari, Italy.


Despite the availability of several anti-retrovirals, there is still an urgent need for developing novel therapeutic strategies and finding new drugs against underexplored HIV-1 targets. Among them, there are the HIV-1 reverse transcriptase (RT)-associated ribonuclease H (RNase H) function and the cellular α-glucosidase, involved in the control mechanisms of N-linked glycoproteins formation in the endoplasmic reticulum. It is known that many natural compounds, such as pentacyclic triterpenes, are a promising class of HIV-1 inhibitors. Hence, here we tested the pentacyclic triterpene Lupeol, showing that it inhibits the HIV-1 RT-associated RNase H function. We then performed combination studies of Lupeol and the active site RNase H inhibitor RDS1759, and blind docking calculations, demonstrating that Lupeol binds to an HIV-1 RT allosteric pocket. On the bases of these results and searching for potential multitarget active drug supplement, we also investigated the anti-HIV-1 activity of Hemidesmus indicus, an Ayurveda medicinal plant containing Lupeol. Results supported the potential of this plant as a valuable multitarget active drug source. In fact, by virtue of its numerous active metabolites, H. indicus was able to inhibit not only the RT-associated RNase H function, but also the HIV-1 RT-associated RNA-dependent DNA polymerase activity and the cellular α-glucosidase.


Hemidesmus indicus; Lupeol; RNase H; RT; anti-HIV-1; multitarget inhibitors; α-glucosidase

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