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Xenobiotica
the fate of foreign compounds in biological systems
Volume 46, 2016 - Issue 7
344
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Xenobiotic Transporters

Interaction of green tea catechins with renal organic cation transporter 2

, , , , &
Pages 641-650 | Received 09 Aug 2015, Accepted 10 Oct 2015, Published online: 17 Nov 2015
 

Abstract

1. Green tea extract (GTE) and EGCG have previously shown to increase the uptake of MPP+ into Caco-2 cells. However, whether GTE and its derivatives interact with renal basolateral organic cation transporter 2 (Oct2) which plays a crucial role for cationic clearance remains unknown. Thus, this study assessed the potential of drug-green tea (GT) catechins and its derivatives interactions with rat Oct2 using renal cortical slices and S2 stably expressing rat Oct2 (S2rOct2).

2. Both GTE and ECG inhibited MPP+ uptake in renal slices in a concentration-dependent manner (IC50 = 2.71 ± 0.360 mg/ml and 0.87 ± 0.151 mM), and this inhibitory effect was reversible. Inhibition of [3H]MPP+ transport in S2rOct2 by either GTE or ECG (IC50 = 1.90 ± 0.087 mg/ml and 1.67 ± 0.088 mM) was also observed.

3. The weak and reversible interactions of GTE and ECG with rOct2 indicate that consumption of GT beverages could not interfere with cationic drugs secreted via renal OCT2 in humans. However, the rise of therapeutic use of GTE and ECG might have to take into account the significant possibility of adverse drug–green tea catechins interactions which could alter renal organic cation drug clearance.

Acknowledgements

The authors thank Ms. RattanabhornJunthip for extraction method assistance and Mr. ChayaVaddhanaphuti for the assistance with manuscript preparation.

Declaration of interest

This work was supported by the Faculty of Medicine Research Fund, Chiang Mai University, Chiang Mai, Thailand (72/2556 to CS) and the Japanese Ministry of Education, Culture, Sports, Science and Technology for Monbukagakusho scholarship (CJ). The authors are responsible for the content and writing of this article and report no declarations of interest.

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