Anti-HIV-1 activity of compounds isolated from Hypericum hircinum.

SANNA, CINZIA;ESPOSITO, FRANCESCA;Del Vecchio C;Mandas D;BALLERO, MAURO;Bianco A;Parolin C;TRAMONTANO, ENZO

2012-01-01

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Abstract

Hypericum hircinum L. is an evergreen shrub belonging to the Clusiaceae family characterized by a strong smell, caused by tiny glands. It is native of southern Europe and the Mediterranean and it grows in damp, shady stations. In particular in Italy it occurs in Tuscany, Campania, Basilicata and Sardinia with the subspecies hircinum, and in Marche, Campania and Sicily with the subspecies majus (Aiton) N. Robson. This plant is widely used in Lucanian folk medicine for the treatment of cough and in Sardinian for the antiseptic properties and in treatment of burns. The ethanol extract and the chemical constituents isolated and identified of aerial part of Hypericum hircinum L. have been assayed on the two enzymatic associated activities of the human immunodeficiency virus type-1 (HIV-1) reverse transcriptase (RT), a multifunctional viral enzyme which is the most important target in the antiretroviral therapy. RT has two fundamental functions, indispensable for viral replication, the DNA polymerase activity (both RNA- and DNA- dependent) and the ribonuclease H (RNase H) activity. In biochemical assays, the extract inhibit HIV-1 RNase H function and RNA-dependent DNA polymerase activity (RDDP activity) with an IC50 value of 3,125 and 0,475 μM, respectively. Extensive studies have been carried out on the isolation and the identification of the chemical constituents of the extract assayed.