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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.

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.

SUBMITTER: Montone CM 

PROVIDER: S-EPMC8587865 | biostudies-literature | 2021 Nov

REPOSITORIES: biostudies-literature

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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.

Montone Carmela Maria CM   Aita Sara Elsa SE   Arnoldi Anna A   Capriotti Anna Laura AL   Cavaliere Chiara C   Cerrato Andrea A   Lammi Carmen C   Piovesana Susy S   Ranaldi Giulia G   Laganà Aldo A  

Molecules (Basel, Switzerland) 20211108 21

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 inhib  ...[more]