Inhibitory Effects of Green Tea and (–)-Epigallocatechin Gallate on Transport by OATP1B1, OATP1B3, OCT1, OCT2, MATE1, MATE2-K and P-Glycoprotein

• DOI: 10.1371/journal.pone.0139370
• Publication Date: 2015-10-01T17:53:54Z
• Authors: Jana Knop; Shingen Misaka; Katrin Singer; Eva Hoier; Fabian Müller; Hartmut Glaeser; Jörg König; Martin F. Fromm
• Keywords: Green tea extract; P-glycoprotein; Rhodamine 123; Epicatechin gallate; IC50

Green tea catechins inhibit the function of organic anion transporting polypeptides (OATPs) that mediate uptake a diverse group drugs and endogenous compounds into cells. The present study was aimed at investigating effect green its most abundant catechin epigallocatechin gallate (EGCG) on transport activity several drug transporters expressed in enterocytes, hepatocytes renal proximal tubular cells such as OATPs, cation (OCTs), multidrug toxin extrusion proteins (MATEs), P-glycoprotein (P-gp). Uptake typical substrates metformin for OCTs MATEs bromosulphophthalein (BSP) atorvastatin OATPs measured absence presence commercially available EGCG. Transcellular digoxin, substrate P-gp, over 4 hours or EGCG Caco-2 cell monolayers. OCT1-, OCT2-, MATE1- MATE2-K-mediated significantly reduced (P < 0.05). BSP net by OATP1B1 OATP1B3 inhibited [IC50 2.6% (v/v) 0.39% (v/v), respectively]. also OATP1B1- OATP1B3-mediated with IC50 values 1.9% 1.0% respectively. Basolateral to apical digoxin decreased These findings indicate multiple vitro. Further studies are necessary investigate effects prototoypical these humans, particular hepatic (e.g. statins) well substrates.