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Research ArticleGASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL

Correlation of Gene Expression of Ten Drug Efflux Proteins of the ATP-Binding Cassette Transporter Family in Normal Human Jejunum and in Human Intestinal Epithelial Caco-2 Cell Monolayers

Jan Taipalensuu, Hans Törnblom, Greger Lindberg, Curt Einarsson, Folke Sjöqvist, Håkan Melhus, Per Garberg, Brita Sjöström, Bo Lundgren and Per Artursson
Journal of Pharmacology and Experimental Therapeutics October 2001, 299 (1) 164-170;
Jan Taipalensuu
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Hans Törnblom
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Greger Lindberg
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Curt Einarsson
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Folke Sjöqvist
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Håkan Melhus
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Per Garberg
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Brita Sjöström
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Bo Lundgren
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Per Artursson
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Abstract

This investigation describes the expression and interindividual variability in transcript levels of multiple drug efflux systems in the human jejunum and compares the expression profiles in these cells with that of the commonly used Caco-2 cell drug absorption model. Transcript levels of ten-drug efflux proteins of the ATP-binding cassette (ABC) transporter family [MDR1, MDR3, ABCB5, MRP1–6, and breast cancer resistance protein (BCRP)], lung resistance-related protein (LRP), and CYP3A4 were determined using quantitative polymerase chain reaction in jejunal biopsies from 13 healthy human subjects and in Caco-2 cells. All genes except ABCB5 were expressed, and transcript levels varied between individuals only by a factor of 2 to 3. Surprisingly, BCRP and MRP2transcripts were more abundant in jejunum than MDR1transcripts. Jejunal transcript levels of the different ABC transporters spanned a range of three log units with the rank order: BCRP ≈ MRP2 > MDR1 ≈ MRP3 ≈ MRP6 ≈ MRP5 ≈ MRP1 > MRP4 > MDR3. Furthermore, transcript levels of 9 of 10 ABC transporters correlated well between jejunum and Caco-2 cells (r2 = 0.90). However,BCRP exhibited a 100-fold lower transcript level in Caco-2 cells compared with jejunum. Thus, the expression of a number of efflux protein transcripts in jejunum are equal to, or even higher than, that of MDR1, suggesting that the roles of these proteins (in particular BCRP and MRP2) in intestinal drug efflux have been underestimated. Also, we tentatively conclude that the Caco-2 cell line is a useful model of jejunal drug efflux, if the low expression of BCRP is taken into account.

Footnotes

  • This work was supported by grants from The Swedish Medical Research Council (Grant 9478), The Swedish National Board for Laboratory Animals (Grant 01-56), and Pharmacia, Sweden.

  • Abbreviations:
    ABC
    ATP-binding cassette
    BCRP
    breast cancer resistance protein
    LRP
    lung resistance-related protein
    PCR
    polymerase chain reaction
    RT-PCR
    reverse transcription-PCR
    • Received May 14, 2001.
    • Accepted June 29, 2001.
  • The American Society for Pharmacology and Experimental Therapeutics
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Journal of Pharmacology and Experimental Therapeutics: 299 (1)
Journal of Pharmacology and Experimental Therapeutics
Vol. 299, Issue 1
1 Oct 2001
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Research ArticleGASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL

Correlation of Gene Expression of Ten Drug Efflux Proteins of the ATP-Binding Cassette Transporter Family in Normal Human Jejunum and in Human Intestinal Epithelial Caco-2 Cell Monolayers

Jan Taipalensuu, Hans Törnblom, Greger Lindberg, Curt Einarsson, Folke Sjöqvist, Håkan Melhus, Per Garberg, Brita Sjöström, Bo Lundgren and Per Artursson
Journal of Pharmacology and Experimental Therapeutics October 1, 2001, 299 (1) 164-170;

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Research ArticleGASTROINTESTINAL, HEPATIC, PULMONARY, AND RENAL

Correlation of Gene Expression of Ten Drug Efflux Proteins of the ATP-Binding Cassette Transporter Family in Normal Human Jejunum and in Human Intestinal Epithelial Caco-2 Cell Monolayers

Jan Taipalensuu, Hans Törnblom, Greger Lindberg, Curt Einarsson, Folke Sjöqvist, Håkan Melhus, Per Garberg, Brita Sjöström, Bo Lundgren and Per Artursson
Journal of Pharmacology and Experimental Therapeutics October 1, 2001, 299 (1) 164-170;
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