Characterization of the Trans-Epithelial Transport of Green Tea (C. sinensis) Catechin Extracts with In Vitro Inhibitory Effect against the SARS-CoV-2 Papain-like Protease Activity |
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| Authors: | Carmela Maria Montone Sara Elsa Aita Anna Arnoldi Anna Laura Capriotti Chiara Cavaliere Andrea Cerrato Carmen Lammi Susy Piovesana Giulia Ranaldi Aldo Lagan |
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| Institution: | 1.Dipartimento di Chimica, Università di Roma La Sapienza, Piazzale Aldo Moro 5, 00185 Roma, Italy; (C.M.M.); (S.E.A.); (C.C.); (A.C.); (S.P.); (A.L.);2.Dipartimento di Scienze Farmaceutiche, Università degli Studi di Milano La Statale, Via Mangiagalli, 25, 20133 Milano, Italy;3.CREA, Food and Nutrition Research Centre, 00100 Rome, Italy;4.CNR NANOTEC, Campus Ecotekne, University of Salento, Via Monteroni, 73100 Lecce, Italy |
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| Abstract: | This work describes an untargeted analytical approach for the screening, identification, and characterization of the trans-epithelial transport of green tea (Camellia sinensis) 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 (IC50 of 0.125 μg mL−1). 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 (IC50 value equal to 11.62 ± 0.47 μg mL−1) to inhibit the PLpro target. Overall, our findings highlight the synergistic effects of the various components of the crude extract compared to isolated ECG. |
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| Keywords: | Caco-2 cells catechins COVID-19 polyphenols high-resolution mass spectrometry in vitro protease assay C sinensis |
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