Dipartimento di Chimica, Università di Roma La Sapienza, Piazzale Aldo Moro 5, 00185 Roma, Italy.
Dipartimento di Scienze Farmaceutiche, Università degli Studi di Milano La Statale, Via Mangiagalli, 25, 20133 Milano, Italy.
Molecules. 2021 Nov 8;26(21):6744. doi: 10.3390/molecules26216744.
This work describes an untargeted analytical approach for the screening, identification, and characterization of the trans-epithelial transport of green tea () 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 of 0.125 μg mL). 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 value equal to 11.62 ± 0.47 μg mL) to inhibit the PLpro target. Overall, our findings highlight the synergistic effects of the various components of the crude extract compared to isolated ECG.
本研究描述了一种非靶向分析方法,用于筛选、鉴定和表征具有抗 SARS-CoV-2 木瓜蛋白酶样蛋白酶 (PLpro) 活性的绿茶()儿茶素提取物的跨上皮转运。在进行特定儿茶素提取后,对获得的六个级分进行了色谱分离。评估了各馏分对 PLpro 靶标的体外抑制活性。馏分 5 对 SARS-CoV-2 PLpro 的抑制活性最高(IC 为 0.125μg/mL)。非靶向特征分析表明,(-)-表儿茶素-3-没食子酸酯(ECG)是该馏分中含量最丰富的化合物,也是分化的 Caco-2 细胞吸收的主要分子。结果表明,与 ECG(IC 值等于 11.62±0.47μg/mL)相比,馏分 5 对 PLpro 靶标的抑制活性约高 10 倍。总体而言,我们的研究结果突出了与单独 ECG 相比,粗提物中各种成分的协同作用。