Hypericum hircinum L. components as new single‐molecule inhibitors of both HIV‐1 reverse transcriptase‐associated DNA polymerase and ribonuclease H activities

In this study, we have tested the ethanolic extracts obtained by the Hypericum hircinum L. (Hypericaceae) growing in Sardinia (Italy) on the HIV‐1 RT‐associated RNase H function and found that they have inhibitory effects. Active extracts were fractionated up to obtain the main components that have been isolated, tested, and identified to be betulinic acid, shikimic acid, chlorogenic acid, quercetin, 5,7,3′,5′‐tetrahydroxyflavanone, and 5,7,3′,5′‐tetrahydroxyflavanone 7‐O‐glucoside. Betulinic acid and 5,7,3′,5′‐tetrahydroxyflavanone 7‐O‐glucoside were active on both RT‐associated activities, and betulinic acid was also active on HIV‐1 mutant RTs resistant to efavirenz. Overall, our results suggest that some of these compounds inhibit the HIV‐1 RT binding to an allosteric site previously described for other natural compounds and are potential leads for further drug development of a single molecules having dual inhibitory activity.
Source: FEMS Immunology and Medical Microbiology - Category: Microbiology Authors: Tags: Research Article Source Type: research