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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.
Montone, Carmela Maria; Aita, Sara Elsa; Arnoldi, Anna; Capriotti, Anna Laura; Cavaliere, Chiara; Cerrato, Andrea; Lammi, Carmen; Piovesana, Susy; Ranaldi, Giulia; Laganà, Aldo.
  • 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.
Molecules ; 26(21)2021 Nov 08.
Article in English | MEDLINE | ID: covidwho-1512511
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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Full text: Available Collection: International databases Database: MEDLINE Main subject: Tea / Catechin / Coronavirus Papain-Like Proteases Type of study: Prognostic study Limits: Humans Language: English Journal subject: Biology Year: 2021 Document Type: Article Affiliation country: Molecules26216744

Full text: Available Collection: International databases Database: MEDLINE Main subject: Tea / Catechin / Coronavirus Papain-Like Proteases Type of study: Prognostic study Limits: Humans Language: English Journal subject: Biology Year: 2021 Document Type: Article Affiliation country: Molecules26216744