Contribution of organic anion transporting polypeptides to bile acid uptake in the Caco-2 cell monolayer and gastrointestinal tract.

ABSTRACT: The apical sodium-dependent bile acid transporter (ASBT, encoded by SLC10A2) is the sole transporter responsible for bile acid absorption in the human intestinal tract and is a therapeutic target for dyslipidemia. Here, we investigated the mechanisms of bile acid uptake in Caco-2 cells, a widely used in vitro model of intestinal absorption. Initial uptake assays revealed biphasic kinetics in bile acid uptake, suggesting the involvement of multiple transporters. At low substrate concentrations, uptake in Caco-2 cells showed marked sodium dependence, and the kinetic parameters were consistent with those observed in taurocholic acid (TC) uptake by ASBT-expressing cells, identifying ASBT-mediated TC uptake as one component of uptake. The second component showed pronounced pH dependence in Caco

SUBMITTER: Kurobe-Takashima Y 

PROVIDER: S-EPMC12934309 | biostudies-literature | 2026 Jan

REPOSITORIES: biostudies-literature