Interaction of green tea catechins with renal organic cation transporter 2
Interaction of green tea catechins with renal organic cation transporter 2
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DOI：
10.3109/00498254.2015.1107785
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发表时间：
2016-07
期刊：
影响因子：
1.8
通讯作者：
Chaliya Jaiyen;P. Jutabha;N. Anzai;A. Lungkaphin;S. Soodvilai;Chutima Srimaroeng
中科院分区：
文献类型：
--
作者：
Chaliya Jaiyen;P. Jutabha;N. Anzai;A. Lungkaphin;S. Soodvilai;Chutima Srimaroeng
摘要1.绿茶提取物(GTE)和EGCG先前已被证明能增加Caco-2细胞对MPP+的摄取。然而，GTE及其衍生物是否与对阳离子清除起关键作用的肾基底外侧有机阳离子转运蛋白2(Oct2)相互作用尚不清楚。因此，本研究使用肾皮质切片和稳定表达大鼠Oct2(S2rOct2)的S2来评估药物绿茶(GT)儿茶素及其衍生物与大鼠Oct2相互作用的可能性。2.GTE和心电均呈浓度依赖性抑制肾切片摄取MPP+(IC_(50)分别为2.71±0.360 mg/ml和0.87±0.151 mM)，且这种抑制作用是可逆的。GTE和心电均能抑制S2rOct2的[~3H]MPP+转运(IC_(50)分别为1.9±0.087 mg/ml和1.67±0.088 mM)。3.GTE和心电与rOct2的弱相互作用和可逆相互作用表明，饮用GT饮料不会干扰人体通过肾脏OCT2分泌的阳离子药物。然而，GTE和心电图治疗用途的增加可能必须考虑到药物与绿茶儿茶素相互作用的极大可能性，这可能会改变肾脏有机阳离子药物的清除。
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.