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Research Abstract In Vitro Study

In vitro anti-HIV-1 reverse transcriptase and integrase properties of Punica granatum L. leaves, bark, and peel extracts and their main compounds.

In Vitro Anti-HIV-1 Reverse Transcriptase and Integrase Properties ofL. Leaves, Bark, and Peel Extracts and Their Main Compounds.

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Abstract

In a search for natural compounds with anti-HIV-1 activity, we studied the effect of the ethanolic extract obtained from leaves, bark, and peels ofL. for the inhibition of the HIV-1 reverse transcriptase (RT)-associated ribonuclease H (RNase H) and integrase (IN) LEDGF-dependent activities. The chemical analyses led to the detection of compounds belonging mainly to the phenolic and flavonoid chemical classes. Ellagic acid, flavones, and triterpenoid molecules were identified in leaves. The bark and peels were characterized by the presence of hydrolyzable tannins, such as punicalins and punicalagins, together with ellagic acid. Among the isolated compounds, the hydrolyzable tannins and ellagic acid showed a very high inhibition (ICvalues ranging from 0.12 to 1.4µM and 0.065 to 0.09 µM of the RNase H and IN activities, respectively). Of the flavonoids, luteolin and apigenin were found to be able to inhibit RNase H and IN functions (ICvalues in the 3.7-22μM range), whereas luteolin 7--glucoside showed selective activity for HIV-1 IN. In contrast, betulinic acid, ursolic acid, and oleanolic acid were selective for the HIV-1 RNase H activity. Our results strongly support the potential of non-edibleorgans as a valuable source of anti-HIV-1 compounds.

Affiliation

Cinzia Sanna

External References

PubMed ID:
34685933

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