Organic anion transporter
1 (OAT1,
SLC22A6
) and
3 (OAT3,
SLC22A8
) are multispecific drug transporters
highly expressed on the basolateral membranes of the renal proximal
tubules. OAT1 and OAT3 mediate the tubular secretion of clinically
significant drugs; thus, they influence the pharmacokinetics of drugs
and further determine their efficacy and toxicity. OAT1 and OAT3 are
also the target of drug–drug interactions. In this study, we
examined the effects of the tea catechin (−)-epigallocatechin-3-gallate
(EGCG) on human (h) and rat (r) OAT1 and OAT3 using the fluorescent
organic anion 6-carboxyfluorescein (6-CF) and hOAT1-, hOAT3-, rOat1-,
or rOat3-expressing HEK293 cells and on renal elimination of 6-CF
in rats. 6-CF is transported by hOAT1, hOAT3, rOat1, and rOat3. 6-CF
is urinary excreted by Oats in rats. EGCG, a dominant catechin in
green tea leaf, inhibits human and rat OAT1 and OAT3 and reduces the
renal elimination of 6-CF in rats. Our findings are useful for the
assessment of food–drug interactions mediated by renal OATs.