These findings indicate that green tea and EGCG inhibit multiple drug transporters in vitro. Basolateral to apical transport of digoxin was significantly decreased in the presence of green tea and EGCG.

Green tea also inhibited OATP1B1- and OATP1B3-mediated atorvastatin net uptake with IC 50 values of 1.9% (v/v) and 1.0% (v/v), respectively. BSP net uptake by OATP1B1 and OATP1B3 was inhibited by green tea. OCT1-, OCT2-, MATE1- and MATE2-K-mediated metformin uptake was significantly reduced in the presence of green tea and EGCG (P < 0.05). Transcellular transport of digoxin, a typical substrate of P-gp, was measured over 4 hours in the absence and presence of green tea or EGCG in Caco-2 cell monolayers. Uptake of the typical substrates metformin for OCTs and MATEs and bromosulphophthalein (BSP) and atorvastatin for OATPs was measured in the absence and presence of a commercially available green tea and EGCG. The present study was aimed at investigating the effect of green tea and its most abundant catechin epigallocatechin gallate (EGCG) on the transport activity of several drug transporters expressed in enterocytes, hepatocytes and renal proximal tubular cells such as OATPs, organic cation transporters (OCTs), multidrug and toxin extrusion proteins (MATEs), and P-glycoprotein (P-gp).

Green tea catechins inhibit the function of organic anion transporting polypeptides (OATPs) that mediate the uptake of a diverse group of drugs and endogenous compounds into cells.

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