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Effect of ursodeoxycholic acid treatment on the expression and function of multidrug resistance-associated protein 2

Ryoko Yumoto1, Shota Hamada, Kaori Okada

  • 1Department of Pharmaceutics and Therapeutics, Graduate School of Biomedical Sciences, Hiroshima University, 1-2-3 Kasumi, Minami-ku, Hiroshima 734-8553, Japan.

Journal of Pharmaceutical Sciences
|December 11, 2008
PubMed

Insights

Ursodeoxycholic acid (UDCA) increases intestinal multidrug resistance-associated protein 2 (Mrp2) expression and function in rats. This enhanced Mrp2 activity may influence drug transport and detoxification in the gut.

Area of Science:

  • Pharmacology
  • Gastroenterology
  • Molecular Biology

Background:

  • Intestinal drug transport is crucial for drug efficacy and toxicity.
  • Multidrug resistance-associated protein 2 (Mrp2) plays a key role in effluxing xenobiotics from intestinal cells.
  • Ursodeoxycholic acid (UDCA) is a known therapeutic bile acid with potential effects on drug transporters.

Purpose of the Study:

  • To investigate the effect of UDCA on the expression and function of intestinal Mrp2.
  • To determine if UDCA administration alters Mrp2-mediated transport in the rat intestine.

Main Methods:

  • Oral administration of UDCA to rats for 6 days.
  • Quantitative assessment of Mrp2 mRNA and protein levels using molecular biology techniques.
  • In vitro everted sac studies to measure Mrp2-mediated substrate efflux.
  • In vivo intestinal exsorption clearance studies.
  • In situ intestinal absorption studies of Mrp2 substrates.

Main Results:

  • UDCA treatment significantly increased Mrp2 mRNA and protein levels in the rat intestine (approximately twofold).
  • UDCA enhanced Mrp2-mediated efflux of 2,4-dinitrophenyl-S-glutathione (DNP-SG) in vitro.
  • In vivo intestinal exsorption clearance of DNP-SG was increased by UDCA.
  • Intestinal absorption of methotrexate, an Mrp2 substrate, was decreased following UDCA treatment.

Conclusions:

  • Oral administration of UDCA up-regulates the expression and function of intestinal Mrp2 in rats.
  • UDCA's modulation of Mrp2 may have implications for the absorption and disposition of Mrp2 substrate drugs.
  • Further research is warranted to explore the clinical relevance of UDCA-induced Mrp2 changes.

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