Effects of phenylpropanoids on human organic anion transporters hOAT1 and hOAT3

摘要: Human organic anion transporters hOAT1/SLC22A6 and hOAT3/SLC22A8 are highly expressed on the basolateral membrane of renal proximal tubules mediate tubular uptake anionic drugs from blood. They play an important role for drug disposition, therefore close studies their ligand recognition therapy development. In this study, we performed experiments using HEK293 fluorescent 6-carboxyfluorescein to asses effects phenylpropanoids hOAT1 hOAT3. We found that phenylpropanoids, 3-(4'-isopentenyloxyphenyl)-benzoic acid (IBA), 3-(4'-isopentenyloxy-3'-methoxyphenyl)-benzoic (IMBA), 3-(4'-geranyloxy-3'-methoxy phenyl)-benzoic (GMBA) inhibited The Ki values were comparable probenecid, a strong inhibitor While IBA demonstrated competitive inhibition, IMBA GMBA showed mixed-type inhibition. After preincubation washout, inhibitory remained with but not IBA, suggesting functional group at 3'-position is responsible these differences. conclusion, IMBA, inhibitors