Characterization of the Trans-Epithelial Transport of Green Tea (<i>C. sinensis</i>) Catechin Extracts with In Vitro Inhibitory Effect against the SARS-CoV-2 Papain-like Protease Activity

This work describes an untargeted analytical approach for the screening, identification, and characterization of the trans-epithelial transport of green tea (<i>Camellia sinensis</i>) catechin extracts with in vitro inhibitory effect against the SARS-CoV-2 papain-like protease (PLpro) ac...

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Autores principales:	Carmela Maria Montone, Sara Elsa Aita, Anna Arnoldi, Anna Laura Capriotti, Chiara Cavaliere, Andrea Cerrato, Carmen Lammi, Susy Piovesana, Giulia Ranaldi, Aldo Laganà
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	Caco-2 cells catechins COVID-19 polyphenols high-resolution mass spectrometry in vitro protease assay Organic chemistry QD241-441
Acceso en línea:	https://doaj.org/article/00d68b48fa254265816e1df0a9bce17c
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spelling	oai:doaj.org-article:00d68b48fa254265816e1df0a9bce17c2021-11-11T18:40:59ZCharacterization of the Trans-Epithelial Transport of Green Tea (<i>C. sinensis</i>) Catechin Extracts with In Vitro Inhibitory Effect against the SARS-CoV-2 Papain-like Protease Activity10.3390/molecules262167441420-3049https://doaj.org/article/00d68b48fa254265816e1df0a9bce17c2021-11-01T00:00:00Zhttps://www.mdpi.com/1420-3049/26/21/6744https://doaj.org/toc/1420-3049This work describes an untargeted analytical approach for the screening, identification, and characterization of the trans-epithelial transport of green tea (<i>Camellia sinensis</i>) catechin extracts with in vitro inhibitory effect against the SARS-CoV-2 papain-like protease (PLpro) activity. After specific catechin extraction, a chromatographic separation obtained six fractions were carried out. The fractions were assessed in vitro against the PLpro target. Fraction 5 showed the highest inhibitory activity against the SARS-CoV-2 PLpro (IC<sub>50</sub> of 0.125 μg mL<sup>−1</sup>). The untargeted characterization revealed that (−)-epicatechin-3-gallate (ECG) was the most abundant compound in the fraction and the primary molecule absorbed by differentiated Caco-2 cells. Results indicated that fraction 5 was approximately 10 times more active than ECG (IC<sub>50</sub> value equal to 11.62 ± 0.47 μg mL<sup>−1</sup>) to inhibit the PLpro target. Overall, our findings highlight the synergistic effects of the various components of the crude extract compared to isolated ECG.Carmela Maria MontoneSara Elsa AitaAnna ArnoldiAnna Laura CapriottiChiara CavaliereAndrea CerratoCarmen LammiSusy PiovesanaGiulia RanaldiAldo LaganàMDPI AGarticleCaco-2 cellscatechinsCOVID-19polyphenolshigh-resolution mass spectrometryin vitro protease assayOrganic chemistryQD241-441ENMolecules, Vol 26, Iss 6744, p 6744 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	Caco-2 cells catechins COVID-19 polyphenols high-resolution mass spectrometry in vitro protease assay Organic chemistry QD241-441
spellingShingle	Caco-2 cells catechins COVID-19 polyphenols high-resolution mass spectrometry in vitro protease assay Organic chemistry QD241-441 Carmela Maria Montone Sara Elsa Aita Anna Arnoldi Anna Laura Capriotti Chiara Cavaliere Andrea Cerrato Carmen Lammi Susy Piovesana Giulia Ranaldi Aldo Laganà Characterization of the Trans-Epithelial Transport of Green Tea (<i>C. sinensis</i>) Catechin Extracts with In Vitro Inhibitory Effect against the SARS-CoV-2 Papain-like Protease Activity
description	This work describes an untargeted analytical approach for the screening, identification, and characterization of the trans-epithelial transport of green tea (<i>Camellia sinensis</i>) catechin extracts with in vitro inhibitory effect against the SARS-CoV-2 papain-like protease (PLpro) activity. After specific catechin extraction, a chromatographic separation obtained six fractions were carried out. The fractions were assessed in vitro against the PLpro target. Fraction 5 showed the highest inhibitory activity against the SARS-CoV-2 PLpro (IC<sub>50</sub> of 0.125 μg mL<sup>−1</sup>). The untargeted characterization revealed that (−)-epicatechin-3-gallate (ECG) was the most abundant compound in the fraction and the primary molecule absorbed by differentiated Caco-2 cells. Results indicated that fraction 5 was approximately 10 times more active than ECG (IC<sub>50</sub> value equal to 11.62 ± 0.47 μg mL<sup>−1</sup>) to inhibit the PLpro target. Overall, our findings highlight the synergistic effects of the various components of the crude extract compared to isolated ECG.
format	article
author	Carmela Maria Montone Sara Elsa Aita Anna Arnoldi Anna Laura Capriotti Chiara Cavaliere Andrea Cerrato Carmen Lammi Susy Piovesana Giulia Ranaldi Aldo Laganà
author_facet	Carmela Maria Montone Sara Elsa Aita Anna Arnoldi Anna Laura Capriotti Chiara Cavaliere Andrea Cerrato Carmen Lammi Susy Piovesana Giulia Ranaldi Aldo Laganà
author_sort	Carmela Maria Montone
title	Characterization of the Trans-Epithelial Transport of Green Tea (<i>C. sinensis</i>) Catechin Extracts with In Vitro Inhibitory Effect against the SARS-CoV-2 Papain-like Protease Activity
title_short	Characterization of the Trans-Epithelial Transport of Green Tea (<i>C. sinensis</i>) Catechin Extracts with In Vitro Inhibitory Effect against the SARS-CoV-2 Papain-like Protease Activity
title_full	Characterization of the Trans-Epithelial Transport of Green Tea (<i>C. sinensis</i>) Catechin Extracts with In Vitro Inhibitory Effect against the SARS-CoV-2 Papain-like Protease Activity
title_fullStr	Characterization of the Trans-Epithelial Transport of Green Tea (<i>C. sinensis</i>) Catechin Extracts with In Vitro Inhibitory Effect against the SARS-CoV-2 Papain-like Protease Activity
title_full_unstemmed	Characterization of the Trans-Epithelial Transport of Green Tea (<i>C. sinensis</i>) Catechin Extracts with In Vitro Inhibitory Effect against the SARS-CoV-2 Papain-like Protease Activity
title_sort	characterization of the trans-epithelial transport of green tea (<i>c. sinensis</i>) catechin extracts with in vitro inhibitory effect against the sars-cov-2 papain-like protease activity
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/00d68b48fa254265816e1df0a9bce17c
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Characterization of the Trans-Epithelial Transport of Green Tea (<i>C. sinensis</i>) Catechin Extracts with In Vitro Inhibitory Effect against the SARS-CoV-2 Papain-like Protease Activity

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