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Article

HIV-1 Integrase Inhibition Activity by Spiroketals Derived from Plagius flosculosus, an Endemic Plant of Sardinia (Italy) and Corsica (France)

by
Cinzia Sanna
1,
Brigida D’Abrosca
2,*,
Antonio Fiorentino
2,
Federica Giammarino
3,
Ilaria Vicenti
3,
Angela Corona
4,
Alessia Caredda
4,
Enzo Tramontano
4 and
Francesca Esposito
4,*
1
Department of Life and Environmental Sciences, University of Cagliari, Via Sant’Ignazio da Laconi 13, 09123 Cagliari, Italy
2
Department of Environmental Biological and Pharmaceutical Sciences and Technologies, DiSTABiF University of Campania Luigi Vanvitelli, Via Vivaldi 43, 81100 Caserta, Italy
3
Department of Medical Biotechnologies, University of Siena, Viale Bracci 16, 53100 Siena, Italy
4
Department of Life and Environmental Sciences, University of Cagliari, Cittadella Universitaria di Monserrato, SS554, 09042 Monserrato, Italy
*
Authors to whom correspondence should be addressed.
Pharmaceuticals 2023, 16(8), 1118; https://doi.org/10.3390/ph16081118
Submission received: 13 July 2023 / Revised: 28 July 2023 / Accepted: 3 August 2023 / Published: 8 August 2023
(This article belongs to the Special Issue Antiviral Compounds in Medicinal Plants 2023)
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Abstract

In this work we investigated, for the first time, the effect of Plagius flosculosus (L.) Alavi & Heywood, a Sardinian–Corsican endemic plant, on HIV-1 integrase (IN) activity. The phytochemical analysis of the leaves chloroform extract led us to isolate and characterize three compounds (SPK1, SPK2, and SPK3) belonging to the spiroketals, a group of naturally occurring metabolites of phytochemical relevance with interesting biological properties. Due to their structural diversity, these cyclic ketals have attracted the interest of chemists and biologists. SPK1, SPK2, and SPK3 were evaluated here for their ability to inhibit HIV-1 integrase activity in biochemical assays. The results showed that all the compounds inhibited HIV-1 IN activity. In particular, the most active one was SPK3, which interfered in a low molecular range (IC50 of 1.46 ± 0.16 µM) with HIV-1 IN activity in the presence/absence of the LEDGF cellular cofactor. To investigate the mechanism of action, the three spiroketals were also tested on HIV-1 RT-associated Ribonuclease H (RNase H) activity, proving to be active in inhibiting this function. Although SPK3 was unable to inhibit viral replication in cell culture, it promoted the IN multimerization. We hypothesize that SPK3 inhibited HIV-1 IN through an allosteric mechanism of action.
Keywords: Plagius flosculosus; 1H-NMR profiling; spiroketals; HIV-1 inhibitors; integrase; IN-LEDGF binding inhibitors Plagius flosculosus; 1H-NMR profiling; spiroketals; HIV-1 inhibitors; integrase; IN-LEDGF binding inhibitors

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MDPI and ACS Style

Sanna, C.; D’Abrosca, B.; Fiorentino, A.; Giammarino, F.; Vicenti, I.; Corona, A.; Caredda, A.; Tramontano, E.; Esposito, F. HIV-1 Integrase Inhibition Activity by Spiroketals Derived from Plagius flosculosus, an Endemic Plant of Sardinia (Italy) and Corsica (France). Pharmaceuticals 2023, 16, 1118. https://doi.org/10.3390/ph16081118

AMA Style

Sanna C, D’Abrosca B, Fiorentino A, Giammarino F, Vicenti I, Corona A, Caredda A, Tramontano E, Esposito F. HIV-1 Integrase Inhibition Activity by Spiroketals Derived from Plagius flosculosus, an Endemic Plant of Sardinia (Italy) and Corsica (France). Pharmaceuticals. 2023; 16(8):1118. https://doi.org/10.3390/ph16081118

Chicago/Turabian Style

Sanna, Cinzia, Brigida D’Abrosca, Antonio Fiorentino, Federica Giammarino, Ilaria Vicenti, Angela Corona, Alessia Caredda, Enzo Tramontano, and Francesca Esposito. 2023. "HIV-1 Integrase Inhibition Activity by Spiroketals Derived from Plagius flosculosus, an Endemic Plant of Sardinia (Italy) and Corsica (France)" Pharmaceuticals 16, no. 8: 1118. https://doi.org/10.3390/ph16081118

APA Style

Sanna, C., D’Abrosca, B., Fiorentino, A., Giammarino, F., Vicenti, I., Corona, A., Caredda, A., Tramontano, E., & Esposito, F. (2023). HIV-1 Integrase Inhibition Activity by Spiroketals Derived from Plagius flosculosus, an Endemic Plant of Sardinia (Italy) and Corsica (France). Pharmaceuticals, 16(8), 1118. https://doi.org/10.3390/ph16081118

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