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

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 speci...

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Bibliographic Details
Published in:Molecules (Basel, Switzerland) Switzerland), 2021-11, Vol.26 (21), p.6744
Main Authors: Montone, Carmela Maria, Aita, Sara Elsa, Arnoldi, Anna, Capriotti, Anna Laura, Cavaliere, Chiara, Cerrato, Andrea, Lammi, Carmen, Piovesana, Susy, Ranaldi, Giulia, Laganà, Aldo
Format: Article
Language:English
Subjects:
Binding sites
Bioavailability
Caco-2 cells
Caffeine
Catechin
catechins
Cell differentiation
Chromatography
Coronaviruses
COVID-19
Drug dosages
Epicatechin
Flavonoids
Green tea
high-resolution mass spectrometry
HIV
Human immunodeficiency virus
in vitro protease assay
Investigations
Pandemics
Papain
Polyphenols
Protease
Proteinase
RNA polymerase
Severe acute respiratory syndrome
Severe acute respiratory syndrome coronavirus 2
Synergistic effect
Tea
Viruses
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Summary: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.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules26216744