학술논문
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.
Document Type
Academic Journal
Author
Montone CM; Dipartimento di Chimica, Università di Roma La Sapienza, Piazzale Aldo Moro 5, 00185 Roma, Italy.; Aita SE; Dipartimento di Chimica, Università di Roma La Sapienza, Piazzale Aldo Moro 5, 00185 Roma, Italy.; Arnoldi A; Dipartimento di Scienze Farmaceutiche, Università degli Studi di Milano La Statale, Via Mangiagalli, 25, 20133 Milano, Italy.; Capriotti AL; Dipartimento di Chimica, Università di Roma La Sapienza, Piazzale Aldo Moro 5, 00185 Roma, Italy.; Cavaliere C; Dipartimento di Chimica, Università di Roma La Sapienza, Piazzale Aldo Moro 5, 00185 Roma, Italy.; Cerrato A; Dipartimento di Chimica, Università di Roma La Sapienza, Piazzale Aldo Moro 5, 00185 Roma, Italy.; Lammi C; Dipartimento di Scienze Farmaceutiche, Università degli Studi di Milano La Statale, Via Mangiagalli, 25, 20133 Milano, Italy.; Piovesana S; Dipartimento di Chimica, Università di Roma La Sapienza, Piazzale Aldo Moro 5, 00185 Roma, Italy.; Ranaldi G; CREA, Food and Nutrition Research Centre, 00100 Rome, Italy.; Laganà A; Dipartimento di Chimica, Università di Roma La Sapienza, Piazzale Aldo Moro 5, 00185 Roma, Italy.; CNR NANOTEC, Campus Ecotekne, University of Salento, Via Monteroni, 73100 Lecce, Italy.
Source
Publisher: MDPI Country of Publication: Switzerland NLM ID: 100964009 Publication Model: Electronic Cited Medium: Internet ISSN: 1420-3049 (Electronic) Linking ISSN: 14203049 NLM ISO Abbreviation: Molecules Subsets: MEDLINE
Subject
Language
English
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 (IC 50 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 (IC 50 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.