Citrus juices inhibit the function of human organic anion-transporting polypeptide OATP-B.

Article Details

Citation

Satoh H, Yamashita F, Tsujimoto M, Murakami H, Koyabu N, Ohtani H, Sawada Y

Citrus juices inhibit the function of human organic anion-transporting polypeptide OATP-B.

Drug Metab Dispos. 2005 Apr;33(4):518-23. Epub 2005 Jan 7.

PubMed ID
15640378 [ View in PubMed
]
Abstract

Human organic anion-transporting polypeptide B (OATP-B; OATP2B1) is expressed in the human intestinal epithelial cells, and is suggested to be involved in the intestinal absorption of anionic drugs in vivo. Although citrus juices have been shown to inhibit the function of human OATP-A (OATP1A2), the effect of citrus juices on the OATP-B function remains unclear. In this study, we aimed to examine the effects of citrus juices on the function of OATP-B. The effects of citrus juices on the uptake of estrone-3-sulfate, a typical substrate for OATP-B, into human embryonic kidney 293 cells stably expressing OATP-B were evaluated. Juices were diluted with uptake buffer, adjusted to pH 7.4 and approximately 300 mOsm, and used for the experiments. Grapefruit juice (GFJ) and orange juice (OJ) at a concentration of 5% significantly inhibited the OATP-B-mediated uptake of estrone-3-sulfate by 82 and 53%, respectively. Major constituents of GFJ and OJ also significantly inhibited the OATP-B-mediated uptake of estrone-3-sulfate. Glibenclamide, a hypoglycemic drug, was identified for the first time as a substrate for OATP-B with a K(t) value of 6.26 microM. GFJ and OJ inhibited the OATP-B-mediated uptake of glibenclamide. These results suggest that citrus juices may inhibit the intestinal absorption of anionic drugs, such as glibenclamide, via the inhibition of OATP-B.

DrugBank Data that Cites this Article

Drug Transporters
DrugTransporterKindOrganismPharmacological ActionActions
Conjugated estrogensSolute carrier organic anion transporter family member 2B1ProteinHumans
Unknown
Substrate
Details
DexibuprofenSolute carrier organic anion transporter family member 2B1ProteinHumans
Unknown
Not AvailableDetails
GlyburideSolute carrier organic anion transporter family member 2B1ProteinHumans
Unknown
Substrate
Details
IbuprofenSolute carrier organic anion transporter family member 2B1ProteinHumans
Unknown
Substrate
Details
NaringeninSolute carrier organic anion transporter family member 2B1ProteinHumans
Unknown
Inhibitor
Details
QuercetinSolute carrier organic anion transporter family member 2B1ProteinHumans
Unknown
Inhibitor
Details
Salicylic acidSolute carrier organic anion transporter family member 2B1ProteinHumans
Unknown
Substrate
Details
Taurocholic acidSolute carrier organic anion transporter family member 2B1ProteinHumans
Unknown
Substrate
Details
TolbutamideSolute carrier organic anion transporter family member 2B1ProteinHumans
Unknown
Substrate
Details