Transport Characteristics of Multidrug Resistance–associatedProtein 5 in Human Erythrocyte Membranes

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  • Yumoto Ryoko
    Department of Pharmaceutics and Therapeutics, Graduate School of Biomedical Sciences, Hiroshima University
  • Yamakawa Keiko
    Department of Pharmaceutics and Therapeutics, Graduate School of Biomedical Sciences, Hiroshima University
  • Nagai Junya
    Department of Pharmaceutics and Therapeutics, Graduate School of Biomedical Sciences, Hiroshima University
  • Takano Mikihisa
    Department of Pharmaceutics and Therapeutics, Graduate School of Biomedical Sciences, Hiroshima University

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Abstract

In human erythrocyte membranes, multidrug resistance–associated protein (MRP) 1, 4 and 5 are expressed. Inthis study, transport function of MRP5 was evaluated using 5–(and–6)–carboxy–2’, 7’dichlorofluorescein (CDCF) asa substrate. The uptake of CDCF by inside–out vesicles (IOVs) prepared from human erythrocytes was anATP–dependent, active process, and was saturable with a Km value of 32.9μM. CDCF uptake was almost complete-ly inhibited by probenecid and sulfinpyrazone. On the other hand, prostaglandin E1(PGE1), an inhibitor of MRP4,did not affect CDCF uptake, though the uptake of methotrexate (MTX) by IOVs was strongly inhibited by PGE1.Similarly, cGMP and panipenem, a carbapenem antibiotic, inhibited MTX but not CDCF uptake, while valproic acidinhibited the uptake of both compounds. These results indicate that CDCF is a suitable compound to analyze MRP5function in human erythrocyte membranes, and sensitivity to several compounds such as PGE1, cGMP and panipen-em is different between MRP5 and MRP4.

Journal

  • MEMBRANE

    MEMBRANE 34 (3), 152-158, 2009

    THE MEMBRANE SOCIETY OF JAPAN

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