In Vitro Anti-HIV-1 Reverse Transcriptase and Integrase Properties of <i>Punica granatum</i> 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 <i>Punica granatum</i> L. for the inhibition of the HIV-1 reverse transcriptase (RT)-associated ribonuclease H (RNase H) and integrase (IN)...
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MDPI AG
2021-10-01
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| Online Access: | https://www.mdpi.com/2223-7747/10/10/2124 |
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| author | Cinzia Sanna Arianna Marengo Stefano Acquadro Alessia Caredda Roberta Lai Angela Corona Enzo Tramontano Patrizia Rubiolo Francesca Esposito |
| author_facet | Cinzia Sanna Arianna Marengo Stefano Acquadro Alessia Caredda Roberta Lai Angela Corona Enzo Tramontano Patrizia Rubiolo Francesca Esposito |
| author_sort | Cinzia Sanna |
| collection | DOAJ |
| description | 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 <i>Punica granatum</i> 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<sub>50</sub> 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<sub>50</sub> values in the 3.7–22 μM range), whereas luteolin 7-<i>O</i>-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 <i>P. granatum</i> organs as a valuable source of anti-HIV-1 compounds. |
| first_indexed | 2024-03-10T06:15:47Z |
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| issn | 2223-7747 |
| language | English |
| last_indexed | 2024-03-10T06:15:47Z |
| publishDate | 2021-10-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Plants |
| spelling | doaj.art-f2cab98899af4fb69f54cadd87c7c28d2023-11-22T19:44:11ZengMDPI AGPlants2223-77472021-10-011010212410.3390/plants10102124In Vitro Anti-HIV-1 Reverse Transcriptase and Integrase Properties of <i>Punica granatum</i> L. Leaves, Bark, and Peel Extracts and Their Main CompoundsCinzia Sanna0Arianna Marengo1Stefano Acquadro2Alessia Caredda3Roberta Lai4Angela Corona5Enzo Tramontano6Patrizia Rubiolo7Francesca Esposito8Laboratory of Pharmaceutical Botany, Department of Life and Environmental Sciences, University of Cagliari, Via S. Ignazio da Laconi 13, 09123 Cagliari, ItalyDepartment of Drug Science and Technology, University of Turin, Via Pietro Giuria 9, 10125 Turin, ItalyDepartment of Drug Science and Technology, University of Turin, Via Pietro Giuria 9, 10125 Turin, ItalyLaboratory of Molecular Virology, Department of Life and Environmental Sciences, University of Cagliari, Cittadella Universitaria di Monserrato, ss554, km 4500, Monserrato, 09042 Cagliari, ItalyLaboratory of Pharmaceutical Botany, Department of Life and Environmental Sciences, University of Cagliari, Via S. Ignazio da Laconi 13, 09123 Cagliari, ItalyLaboratory of Molecular Virology, Department of Life and Environmental Sciences, University of Cagliari, Cittadella Universitaria di Monserrato, ss554, km 4500, Monserrato, 09042 Cagliari, ItalyLaboratory of Molecular Virology, Department of Life and Environmental Sciences, University of Cagliari, Cittadella Universitaria di Monserrato, ss554, km 4500, Monserrato, 09042 Cagliari, ItalyDepartment of Drug Science and Technology, University of Turin, Via Pietro Giuria 9, 10125 Turin, ItalyLaboratory of Molecular Virology, Department of Life and Environmental Sciences, University of Cagliari, Cittadella Universitaria di Monserrato, ss554, km 4500, Monserrato, 09042 Cagliari, ItalyIn 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 <i>Punica granatum</i> 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<sub>50</sub> 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<sub>50</sub> values in the 3.7–22 μM range), whereas luteolin 7-<i>O</i>-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 <i>P. granatum</i> organs as a valuable source of anti-HIV-1 compounds.https://www.mdpi.com/2223-7747/10/10/2124<i>Punica granatum</i>pomegranateleavesbarkpeelHIV-1 reverse transcriptase |
| spellingShingle | Cinzia Sanna Arianna Marengo Stefano Acquadro Alessia Caredda Roberta Lai Angela Corona Enzo Tramontano Patrizia Rubiolo Francesca Esposito In Vitro Anti-HIV-1 Reverse Transcriptase and Integrase Properties of <i>Punica granatum</i> L. Leaves, Bark, and Peel Extracts and Their Main Compounds Plants <i>Punica granatum</i> pomegranate leaves bark peel HIV-1 reverse transcriptase |
| title | In Vitro Anti-HIV-1 Reverse Transcriptase and Integrase Properties of <i>Punica granatum</i> L. Leaves, Bark, and Peel Extracts and Their Main Compounds |
| title_full | In Vitro Anti-HIV-1 Reverse Transcriptase and Integrase Properties of <i>Punica granatum</i> L. Leaves, Bark, and Peel Extracts and Their Main Compounds |
| title_fullStr | In Vitro Anti-HIV-1 Reverse Transcriptase and Integrase Properties of <i>Punica granatum</i> L. Leaves, Bark, and Peel Extracts and Their Main Compounds |
| title_full_unstemmed | In Vitro Anti-HIV-1 Reverse Transcriptase and Integrase Properties of <i>Punica granatum</i> L. Leaves, Bark, and Peel Extracts and Their Main Compounds |
| title_short | In Vitro Anti-HIV-1 Reverse Transcriptase and Integrase Properties of <i>Punica granatum</i> L. Leaves, Bark, and Peel Extracts and Their Main Compounds |
| title_sort | in vitro anti hiv 1 reverse transcriptase and integrase properties of i punica granatum i l leaves bark and peel extracts and their main compounds |
| topic | <i>Punica granatum</i> pomegranate leaves bark peel HIV-1 reverse transcriptase |
| url | https://www.mdpi.com/2223-7747/10/10/2124 |
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