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
Abstrak
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.
Topik & Kata Kunci
Penulis (10)
Carmela Maria Montone
Sara Elsa Aita
Anna Arnoldi
Anna Laura Capriotti
Chiara Cavaliere
Andrea Cerrato
Carmen Lammi
Susy Piovesana
Giulia Ranaldi
Aldo Laganà
Format Sitasi
Akses Cepat
- Tahun Terbit
- 2021
- Sumber Database
- DOAJ
- DOI
- 10.3390/molecules26216744
- Akses
- Open Access ✓