Physiological characteristics of allo-cholic acid.

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Mendoza ME, Monte MJ, Serrano MA, Pastor-Anglada M, Stieger B, Meier PJ, Medarde M, Marin JJ

Physiological characteristics of allo-cholic acid.

J Lipid Res. 2003 Jan;44(1):84-92.

PubMed ID

12518026 [ View in PubMed

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Abstract

The physiological characterstics of allo-cholic acid (ACA), a typically fetal bile acid that reappears during liver regeneration and carcinogenesis were investigated. [(14)C] Tauro-ACA (TACA) uptake by Chinese hamster ovary cells expressing rat organic anion transporter polypeptide (Oatp)1 or sodium-taurocholate cotransporter polypeptide (Ntcp) was lower than that of [(14)C]taurocholic acid (TCA). Although TACA inhibited ATP-dependent TCA transport across plasma membrane vesicles from Sf9 cells expressing rat or mouse bile salt export pump (Bsep), no ATP-dependent TACA transport was found. In rats, TACA was secreted into bile with no major biotransformation and it had lower clearance and longer half-life than TCA. In mice, TACA bile output was lower (-50%) than that of TCA, whereas TACA induced 9-fold higher bile flow than TCA. Even though the intracellular levels were lower for TACA, translocation into the hepatocyte nucleus was higher for TACA than for TCA; however, rate of DNA synthesis, expression levels of alpha-fetoprotein, albumin, Ntcp, and Bsep, cell viability, and apoptosis in rat hepatocytes were similarly affected by both isomers. In conclusion, TACA partly shares hepatocellular uptake system(s) for TCA. Furthermore, in contrast to other "flat" bile acids, TACA is efficiently secreted into bile via transport system(s) other than Bsep and is highly choleretic, hence its appearance during certain situations may prevent accumulation of cholestatic precursors.

DrugBank Data that Cites this Article

Drug Transporters

Drug	Transporter	Kind	Organism	Pharmacological Action	Actions
Taurocholic acid	Bile salt export pump	Protein	Humans	Unknown	Substrate Inducer	Details
Taurocholic acid	Sodium/bile acid cotransporter	Protein	Humans	Unknown	Substrate	Details
Taurocholic acid	Solute carrier organic anion transporter family member 1A2	Protein	Humans	Unknown	Substrate Inhibitor Inducer	Details