Using Caffeine and Free Amino Acids To Enhance the Transepithelial Transport of Catechins in
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Using Caffeine and Free Amino Acids To Enhance the Transepithelial

Transport of Catechins in Caco?2 Cells


Yafang Wang, Yanqiu Zuo, Siyu Deng,  Feng Zhu, Qin Liu,  Ruru Wang, Tao Li, Huimei Cai, Xiaochun Wan,  Zijian Xie,  Zhongwen Xie,*  Daxiang Li*



Journal of Agricultural and Food Chemistry




Catechins are well-known to possess health-promoting functions. The interaction of the catechins with other components in tea could alter their absorption and efflux. This study investigated whether the absorption of catechins is affected by caffeine and amino acids using the Caco-2 monolayer cell model. We found that ()-epigallocatechin gallate (EGCG), ()-epicatechin gallate (ECG), and ()-epicatechin (EC) were all actively effluxed. Co-transportation of EGCG, ECG, or EC with caffeine, theanine, serine, or glycine increased their apparent permeability coefficient [Papp(APBL)] value by 3.425.40- fold, 1.195.75-fold, and 1.558.01-fold, respectively. Meanwhile, their efflux ratio values were significantly decreased. Moreover, the expression of multi-drug resistance protein 2 (MRP2) after 3 h of incubation with either 50 μM EGCG or 50 μM EC was elevated by 1.58- and 2.98-fold, respectively, while 50 μM ECG had no significantly effects. In addition, the expression of Pglycoprotein (P-gp) after treatment with either 50 μM EGCG, 50 μM ECG, or 50 μM EC was enhanced by 1.53-, 1.63-, and 1.80-fold, respectively. The addition of either caffeine or any one of the three amino acids decreased the expression of both MRP2 and P-gp induced by EGCG, and the expression of P-gp induced by ECG or EC also decreased. In contrast, only glycine decreased the expression of MRP2 induced by EC. Taken together, our data indicated that caffeine and theanine, glycine, or serine in tea might increase the absorption of catechins by the selectively suppressed expression of the efflux transporters induced by catechins.

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