Carrier-Mediated Transport of Bile Acids and Amino Acids in Caco-2 Cells

  • Ismael J. Hidalgo
  • Ronald T. Borchardt
Part of the NATO ASI Series book series (NSSA, volume 218)


The small intestinal epithelium comprises a cell population exhibiting continuous growth and differentiation in vivo, where the continuous loss of differentiated cells at the villus tip is compensated by cell replication at the villus crypt.1 The presence of tight junctions, which limits the paracellular diffusion of solutes, together with the numerous enzymes present in the brush border region make the intestinal epithelium the most significant barrier to mucosal absorption of drugs and nutrients.


Bile Acid Cationic Amino Acid Taurocholic Acid Large Neutral Amino Acid Transcellular Transport 
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  1. 1.
    A.B. Cairnie, L.F. Lamerton and G.G. Steel, Cell proliferation studies in the intestinal epithelium of the rat. I. Determination of the kinetic parameters, Exp. Cell Res. 39: 528–538 (1965).PubMedCrossRefGoogle Scholar
  2. 2.
    A. Quaroni, J. Wands, R.L. Trelstad and K.J. Isselbacher, Epithelioid cell cultures from rat small intestine, J. Cell Biol. 80: 248–265 (1979).PubMedCrossRefGoogle Scholar
  3. 3.
    F. Raul, M. Kedinger, P. Simon, J. Grenier and K. Haffen, Behaviour of isolated rat intestinal cells maintained in suspension or monolayer cultures, Biol. Cell 33: 163–168 (1978).Google Scholar
  4. 4.
    M. Pinto, M.-D. Appay, P. Simon-Assmann, G. Chevalier, N. Dracopoli, J. Fogh and A. Zweibaum, Enterocytic differentiation of cultured human colon cancer cells by replacement of glucose by galactose in the medium, Biol. Cell 44: 193–196 (1982).Google Scholar
  5. 5.
    M. Pinto, S. Robine-Leon, M.-D. Appay, M. Kedinger, N. Triadou, E. Dussaulx, B. Lacroix, P. Simon-Assmann, K. Haffen, J. Fogh and A. Zweibaum, Enterocytic-like differentiation and polarization of the human colon carcinoma cell line Caco-2 in culture, Biol. Cell 47: 323–330 (1983).Google Scholar
  6. 6.
    A. Leibovitz, J.C. Stinson, W.B. McCombs III, C.E. McCoy, K.C. Masur and N.D. Mabry, Classification of human colorectal adenocarcinoma cells lines. Cancer Res. 36: 4562–4569 (1976).PubMedGoogle Scholar
  7. 7.
    B.H. Tom, L.P. Rutzky, M.M. Jakstys, R. Oyasu, C.I. Kaye and B.D. Kahan, Human colon adenocarcinomas I. Establishment and description of a new line, In Vitro 12: 180–191 (1976).PubMedCrossRefGoogle Scholar
  8. 8.
    I.J. Hidalgo, T.J. Raub and R.T. Borchardt, Characterization of the human colon carcinoma cell line (Caco-2) as a. model system for intestinal epithelial permeability, Gastroenteroloay 96: 736–749 (1989).Google Scholar
  9. 9.
    T.J. Raub, I.J. Hidalgo, S.L. Kuentzel and R.T. Borchardt, Characterization of the human colon carcinoma cell line (Caco-2) as a model transport system of the intestinal epithelium, FASEB J. 2: 2538 (1988) (Abstr.).Google Scholar
  10. 10.
    M. Cereijido, E.S. Robbins, W.J. Dolan, C.A. Rotunno and D.D. Sabatini, Polarized monolayers formed by epithelial cells on a permeable and translucent support, J. Cell Biol. 77: 853–880 (1978).PubMedCrossRefGoogle Scholar
  11. 11.
    T.E. Phillips, T.L. Phillips and M. Neutra, Macromolecules can pass through occluding junctions of rat ileal epithelium during cholinergic stimulation, Cell Tissue Res. 247: 547–554 (1987).PubMedCrossRefGoogle Scholar
  12. 12.
    S. Erlinger, in: Physiology of the Gastrointestinal Tract”, L.R. Johnson, ed., Raven, New York, 1987, p. 1557–1580.Google Scholar
  13. 13.
    I.J. Hidalgo and R.T. Borchardt, Transport of taurocholic acid in an intestinal epithelial model system (Caco-2 cell), Pharm. Res. 5(Suppl): 949 (1988) (Abstr.).Google Scholar
  14. 14.
    F.A. Wilson and J.M. Dietschy, Characterization of bile acid absorption across the unstirred water layer and brush border of the rat jejunum, J. Clin. Invest. 51: 3015–3025 (1972).PubMedCrossRefGoogle Scholar
  15. 15.
    M. Hofer and J.G. Hoggett, “Transport across biological membranes,” Pitman, Boston, 1981, p. 96–102.Google Scholar
  16. 16.
    E. Krag and S.F. Phillips, Active and passive bile acid absorption in man: perfusion studies of the ileum and jejunum, J. Clin. Invest. 53: 1686–1694 (1974).PubMedCrossRefGoogle Scholar
  17. 17.
    L. Lack and I.M. Weiner, Intestinal absorption of bile acids and some biological implications, Gastroenterology 22: 1334–1338 (1963).Google Scholar
  18. 18.
    S.L. Weinberg, G. Burckhardt and F.A. Wilson, Taurocholate transport by rat intestinal basolateral membrane vesicles. Evidence for the presence of an anion exchange transport system, J. Clin. Invest. 78: 44–50 (1986).PubMedCrossRefGoogle Scholar
  19. 19.
    M.C. Lin, S.L. Weinberg, W. Kramer, G. Burckhardt and F.A. Wilson, Identification and comparison of bile acid-binding polypeptides in ileal basolateral membrane, J. Membr. Biol. 106: 1–11 (1988).PubMedCrossRefGoogle Scholar
  20. 20.
    I.J. Hidalgo and R.T. Borchardt, Amino acid transport in a novel model system of the intestinal epithelium (Caco-2 cell), Pharm. Res. 5(Suppl): 949 (1988) (Abstr.).Google Scholar
  21. 21.
    J.R. Bronk and H.J. Leese, Changes in the adenine nucleotide content of preparations of the rat small intestine in vitro, J. Physiol. (Lond.) 235: 183–196 (1973).Google Scholar
  22. 22.
    B.G. Munck, Intestinal absorption of amino acids, in: “Physiology of the Gastrointestinal Tract,” L.R. Johnson, ed., Raven, New York, 1981, p. 1097–1122.Google Scholar
  23. 23.
    R.P. Sencer and A.H. Samiy, Intestinal absorption of L-phenylalanine in vitro, Am. J. Physiol. 200: 501–504 (1961).Google Scholar
  24. 24.
    I. Osiecka, M. Cortese, P.A. Porter, R.T. Borchardt, J.A. Fix and C.R. Gardner, Intestinal absorption of α-methyldopa: In vitro mechanistic studies in rat small intestinal segments, J. Pharmacol. Exp. Ther. 242: 443–448 (1987).PubMedGoogle Scholar

Copyright information

© Plenum Press, New York 1991

Authors and Affiliations

  • Ismael J. Hidalgo
    • 1
  • Ronald T. Borchardt
    • 1
  1. 1.Department of Pharmaceutical ChemistryThe University of KansasLawrenceUSA

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