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

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 of L. for the inhibition of the HIV-1 reverse transcriptase (RT)-associated ribonuclease H (RNase H) and integrase (IN) LEDGF-dependent activities. The che...

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Bibliographic Details
Published in:Plants (Basel) 2021-10, Vol.10 (10), p.2124
Main Authors: Sanna, Cinzia, Marengo, Arianna, Acquadro, Stefano, Caredda, Alessia, Lai, Roberta, Corona, Angela, Tramontano, Enzo, Rubiolo, Patrizia, Esposito, Francesca
Format: Article
Language:English
Subjects:
Acids
Antiviral activity
Bark
Betulinic acid
DNA polymerase
Drug resistance
Ellagic acid
Enzymes
Flavones
Flavonoids
Fruits
HIV
HIV-1 reverse transcriptase
Human immunodeficiency virus
Integrase
Leaves
Oleanolic acid
Organs
peel
Phenolic compounds
Phenols
Phytochemicals
Plant extracts
pomegranate
Punica granatum
Ribonuclease H
RNA-directed DNA polymerase
Severe acute respiratory syndrome coronavirus 2
Tannins
Ursolic acid
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Summary: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 of L. 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 (IC values ranging from 0.12 to 1.4 µM 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 (IC values in the 3.7-22 μM 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-edible organs as a valuable source of anti-HIV-1 compounds.
ISSN:2223-7747
2223-7747
DOI:10.3390/plants10102124