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.

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, C. M.; Aita, S. E.; Arnoldi, A.; Capriotti, A. L.; Cavaliere, C.; Cerrato, A.; Lammi, C.; Piovesana, S.; Ranaldi, G.; Lagana, A.. - In: MOLECULES. - ISSN 1420-3049. - 26:21(2021). [10.3390/molecules26216744]

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 C. M.;Aita S. E.;Capriotti A. L.;Cavaliere C.;Cerrato A.;Piovesana S.;Ranaldi G.;Lagana A.
2021

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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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11573/1592040
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