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Chemical Characterization and Anti-HIV-1 Activity Assessment of Iridoids and Flavonols from Scrophularia trifoliata

Plants are the everlasting source of a wide spectrum of specialized metabolites, characterized by wide variability in term of chemical structures and different biological properties such antiviral activity. In the search for novel antiviral agents against Human Immunodeficiency Virus type 1 (HIV-1)...

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Autores principales: Guzzo, Francesca, Russo, Rosita, Sanna, Cinzia, Celaj, Odeta, Caredda, Alessia, Corona, Angela, Tramontano, Enzo, Fiorentino, Antonio, Esposito, Francesca, D’Abrosca, Brigida
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8398805/
https://www.ncbi.nlm.nih.gov/pubmed/34443358
http://dx.doi.org/10.3390/molecules26164777
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author Guzzo, Francesca
Russo, Rosita
Sanna, Cinzia
Celaj, Odeta
Caredda, Alessia
Corona, Angela
Tramontano, Enzo
Fiorentino, Antonio
Esposito, Francesca
D’Abrosca, Brigida
author_facet Guzzo, Francesca
Russo, Rosita
Sanna, Cinzia
Celaj, Odeta
Caredda, Alessia
Corona, Angela
Tramontano, Enzo
Fiorentino, Antonio
Esposito, Francesca
D’Abrosca, Brigida
author_sort Guzzo, Francesca
collection PubMed
description Plants are the everlasting source of a wide spectrum of specialized metabolites, characterized by wide variability in term of chemical structures and different biological properties such antiviral activity. In the search for novel antiviral agents against Human Immunodeficiency Virus type 1 (HIV-1) from plants, the phytochemical investigation of Scrophularia trifoliata L. led us to isolate and characterize four flavonols glycosides along with nine iridoid glycosides, two of them, 5 and 13, described for the first time. In the present study, we investigated, for the first time, the contents of a methanol extract of S. trifoliata leaves, in order to explore the potential antiviral activity against HIV-1. The antiviral activity was evaluated in biochemical assays for the inhibition of HIV-1Reverse Transcriptase (RT)-associated Ribonuclease H (RNase H) activity and HIV-1 Integrase (IN). Three isolated flavonoids, rutin, kaempferol-7-O-rhamnosyl-3-O-glucopyranoside, and kaempferol-3-O-glucopyranoside, 8–10, inhibited specifically the HIV-1 IN activity at submicromolar concentration, with the latter being the most potent, showing an IC(50) value of 24 nM.
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spelling pubmed-83988052021-08-29 Chemical Characterization and Anti-HIV-1 Activity Assessment of Iridoids and Flavonols from Scrophularia trifoliata Guzzo, Francesca Russo, Rosita Sanna, Cinzia Celaj, Odeta Caredda, Alessia Corona, Angela Tramontano, Enzo Fiorentino, Antonio Esposito, Francesca D’Abrosca, Brigida Molecules Article Plants are the everlasting source of a wide spectrum of specialized metabolites, characterized by wide variability in term of chemical structures and different biological properties such antiviral activity. In the search for novel antiviral agents against Human Immunodeficiency Virus type 1 (HIV-1) from plants, the phytochemical investigation of Scrophularia trifoliata L. led us to isolate and characterize four flavonols glycosides along with nine iridoid glycosides, two of them, 5 and 13, described for the first time. In the present study, we investigated, for the first time, the contents of a methanol extract of S. trifoliata leaves, in order to explore the potential antiviral activity against HIV-1. The antiviral activity was evaluated in biochemical assays for the inhibition of HIV-1Reverse Transcriptase (RT)-associated Ribonuclease H (RNase H) activity and HIV-1 Integrase (IN). Three isolated flavonoids, rutin, kaempferol-7-O-rhamnosyl-3-O-glucopyranoside, and kaempferol-3-O-glucopyranoside, 8–10, inhibited specifically the HIV-1 IN activity at submicromolar concentration, with the latter being the most potent, showing an IC(50) value of 24 nM. MDPI 2021-08-06 /pmc/articles/PMC8398805/ /pubmed/34443358 http://dx.doi.org/10.3390/molecules26164777 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Guzzo, Francesca
Russo, Rosita
Sanna, Cinzia
Celaj, Odeta
Caredda, Alessia
Corona, Angela
Tramontano, Enzo
Fiorentino, Antonio
Esposito, Francesca
D’Abrosca, Brigida
Chemical Characterization and Anti-HIV-1 Activity Assessment of Iridoids and Flavonols from Scrophularia trifoliata
title Chemical Characterization and Anti-HIV-1 Activity Assessment of Iridoids and Flavonols from Scrophularia trifoliata
title_full Chemical Characterization and Anti-HIV-1 Activity Assessment of Iridoids and Flavonols from Scrophularia trifoliata
title_fullStr Chemical Characterization and Anti-HIV-1 Activity Assessment of Iridoids and Flavonols from Scrophularia trifoliata
title_full_unstemmed Chemical Characterization and Anti-HIV-1 Activity Assessment of Iridoids and Flavonols from Scrophularia trifoliata
title_short Chemical Characterization and Anti-HIV-1 Activity Assessment of Iridoids and Flavonols from Scrophularia trifoliata
title_sort chemical characterization and anti-hiv-1 activity assessment of iridoids and flavonols from scrophularia trifoliata
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8398805/
https://www.ncbi.nlm.nih.gov/pubmed/34443358
http://dx.doi.org/10.3390/molecules26164777
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