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
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) ac...
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| Format: | Article |
| Language: | English |
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MDPI AG
2021-11-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/26/21/6744 |
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| author | Carmela Maria Montone Sara Elsa Aita Anna Arnoldi Anna Laura Capriotti Chiara Cavaliere Andrea Cerrato Carmen Lammi Susy Piovesana Giulia Ranaldi Aldo Laganà |
| author_facet | Carmela Maria Montone Sara Elsa Aita Anna Arnoldi Anna Laura Capriotti Chiara Cavaliere Andrea Cerrato Carmen Lammi Susy Piovesana Giulia Ranaldi Aldo Laganà |
| author_sort | Carmela Maria Montone |
| collection | DOAJ |
| description | 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 inhibitory activity against the SARS-CoV-2 PLpro (IC<sub>50</sub> of 0.125 μg mL<sup>−1</sup>). 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<sub>50</sub> value equal to 11.62 ± 0.47 μg mL<sup>−1</sup>) to inhibit the PLpro target. Overall, our findings highlight the synergistic effects of the various components of the crude extract compared to isolated ECG. |
| first_indexed | 2024-03-10T05:54:28Z |
| format | Article |
| id | doaj.art-00d68b48fa254265816e1df0a9bce17c |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T05:54:28Z |
| publishDate | 2021-11-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-00d68b48fa254265816e1df0a9bce17c2023-11-22T21:26:04ZengMDPI AGMolecules1420-30492021-11-012621674410.3390/molecules26216744Characterization 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 ActivityCarmela Maria Montone0Sara Elsa Aita1Anna Arnoldi2Anna Laura Capriotti3Chiara Cavaliere4Andrea Cerrato5Carmen Lammi6Susy Piovesana7Giulia Ranaldi8Aldo Laganà9Dipartimento di Chimica, Università di Roma La Sapienza, Piazzale Aldo Moro 5, 00185 Roma, ItalyDipartimento di Chimica, Università di Roma La Sapienza, Piazzale Aldo Moro 5, 00185 Roma, ItalyDipartimento di Scienze Farmaceutiche, Università degli Studi di Milano La Statale, Via Mangiagalli, 25, 20133 Milano, ItalyDipartimento di Chimica, Università di Roma La Sapienza, Piazzale Aldo Moro 5, 00185 Roma, ItalyDipartimento di Chimica, Università di Roma La Sapienza, Piazzale Aldo Moro 5, 00185 Roma, ItalyDipartimento di Chimica, Università di Roma La Sapienza, Piazzale Aldo Moro 5, 00185 Roma, ItalyDipartimento di Scienze Farmaceutiche, Università degli Studi di Milano La Statale, Via Mangiagalli, 25, 20133 Milano, ItalyDipartimento di Chimica, Università di Roma La Sapienza, Piazzale Aldo Moro 5, 00185 Roma, ItalyCREA, Food and Nutrition Research Centre, 00100 Rome, ItalyDipartimento di Chimica, Università di Roma La Sapienza, Piazzale Aldo Moro 5, 00185 Roma, ItalyThis 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 inhibitory activity against the SARS-CoV-2 PLpro (IC<sub>50</sub> of 0.125 μg mL<sup>−1</sup>). 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<sub>50</sub> value equal to 11.62 ± 0.47 μg mL<sup>−1</sup>) to inhibit the PLpro target. Overall, our findings highlight the synergistic effects of the various components of the crude extract compared to isolated ECG.https://www.mdpi.com/1420-3049/26/21/6744Caco-2 cellscatechinsCOVID-19polyphenolshigh-resolution mass spectrometryin vitro protease assay |
| spellingShingle | Carmela Maria Montone Sara Elsa Aita Anna Arnoldi Anna Laura Capriotti Chiara Cavaliere Andrea Cerrato Carmen Lammi Susy Piovesana Giulia Ranaldi Aldo Laganà 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 Molecules Caco-2 cells catechins COVID-19 polyphenols high-resolution mass spectrometry in vitro protease assay |
| title | 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 |
| title_full | 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 |
| title_fullStr | 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 |
| title_full_unstemmed | 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 |
| title_short | 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 |
| title_sort | 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 |
| topic | Caco-2 cells catechins COVID-19 polyphenols high-resolution mass spectrometry in vitro protease assay |
| url | https://www.mdpi.com/1420-3049/26/21/6744 |
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