Multi target mode of HIV-1 inhibition by the bioactive molecule Lupeol extracted from the Indian plant Hemidesmus indicus R.Br.

In the effort of identifying novel therapeutic approaches for the discovery of new anti-infective drugs, the traditional Indian medicine and the use of natural compounds active against various diseases, including viral infections, receive nowadays considerable attention. Hemidesmus indicus R.Br. is known for its ethno-botanical use and its efficacy in the treatment of bone-loss diseases, and, in the Indian traditional medicine, is widely used for the treatment of blood diseases, dyspepsia, loss of taste, dyspnea, cough, poison, menorrhagia, fever and diarrhea. In the last thirty years, many natural substances have shown antiviral activity, but very few of them showed multi target mode of action. For this reason, we assessed the Hemidesmus indicus R.Br. decoction against i) the Human Immunodeficiency Virus type 1 (HIV -1) Reverse Transcriptase (RT)-associated functions and ii) the α-glucosidase activity, with the aim to identify a molecule capable to inhibit with a multiple mode of action different promising targets. Hemidesmus indicus R.Br. decoction has been shown to be active on the inhibition of both RT-associated functions and α-glucosidase activity. Active decoction was fractionated up to obtain the bioactive components which have been isolated, tested and identified as Lupeol, Lupeol Acetate, Caffeic Acid, Chlorogenic Acid and β-amirine acetate. Among these, Lupeol inhibited the HIV-1 RT -associated RNase H function, and the α -glucosidase activity. Our results suggest that this bioactive molecule is a potential lead for further development of drugs with multi target mechanism of action.