P-glycoprotein (P-gp) mediated efflux in Caco-2 cell monolayers: The influence of culturing conditions and drug exposure on P-gp expression levels

Journal of Pharmaceutical Sciences

Volumn 87, Issue 6, 1998, Pages 757-762

  Anderle, Pascale ^a   Niederer, Eva ^a   Rubas, Werner ^b   Hilgendorf, Constanze ^c   Spahn Langguth, Hilde ^c   Wunderli Allenspach, Heidi ^a   Merkle, Hans P ^a   Langguth, Peter ^a,d  

^a ETH ZURICH   (Switzerland)

^b GENENTECH INC   (United States)

^c MARTIN LUTHER UNIVERSITY HALLE WITTENBERG   (Germany)

^d ASTRAZENECA R AND D   (Sweden)

Author keywords

[No Author keywords available]

Indexed keywords

2 BUTYL 4 CHLORO 1 [[2' (1H TETRAZOL 5 YL) 4 BIPHENYLYL]METHYL] 5 IMIDAZOLECARBOXYLIC ACID; CELIPROLOL; GLYCOPROTEIN P; LOSARTAN; METKEPHAMID; MONOCLONAL ANTIBODY; MONOCLONAL ANTIBODY MRK 16; PENICILLIN G; STREPTOMYCIN; TALINOLOL; TROSPIUM CHLORIDE; UNCLASSIFIED DRUG; VERAPAMIL; VINBLASTINE;

APICAL MEMBRANE; ARTICLE; BASOLATERAL MEMBRANE; CELL STRAIN CACO 2; CONFOCAL LASER MICROSCOPY; CONTROLLED STUDY; DRUG PENETRATION; DRUG TRANSPORT; FLOW CYTOMETRY; HUMAN; HUMAN CELL; PROTEIN EXPRESSION;

EID: 0031834404     PISSN: 00223549     EISSN: None     Source Type: Journal    
DOI: 10.1021/js970372e     Document Type: Article

References (22)

1. Saitoh, H.; Aungst, B. J. Possible involvement of multiple P-glycoprotein-mediated efflux systems in the transport of verapamil and other organic cations across rat intestine. Pharm. Res. 1995, 12, 1304-10.
2. Hunter, J.; Jepson, M. A.; Tsuruo, T.; Simmons, N. L.; Hirst B. H. Functional expression of P-glycoprotein in apical membranes of human intestinal Caco-2 cells. Kinetics of vinblastine secretion and interaction with modulators. J. Biol. Chem. 1993a, 268, 14991-14997.
3. Hunter, J.; Hirst B. H.; Simmons, N. L. Drug absorption limited by P-glycoprotein-mediated secretory drug transport in human intestinal epithelial Caco-2 cell layers. Pharm. Res. 1993b, 10: 743-749.
4. Horio, M.; Chin K. V.; Currier S. J.; Goldenberg S.; Williams C.; Pastan I.; Gottesman M. M.; Handler J. Transepithelial transport of drugs by the multidrug transporter in cultured Madin-Darby canine kidney cell epithelia. J. Biol. Chem. 1989, 264, 14880-4.
5. Bartels, H.; Korasiak, E.; Daniel, H. Transport of Daunomycin in Caco-2 cells: What is the contribution of the mdr-1-gene product to the transepithelial fluxes. H. Presented at the 13th European Intestinal Transport Group (EITG) Congress, Sept 22-26, 1996, Mikolayki, Poland.
6. Karlsson, J.; Kuo S. M.; Ziemniak J.; Artursson, P. Transport of celiprolol across human intestinal epithelial (Caco-2) cells: Mediation of secretion by multiple transporters including P-glycoprotein. Brit. J. Pharmacol. 1993, 110, 1009-1016.
7. Wetterich, U.; Spahn-Langguth, H. Mutschler, E.; Terhaag, B.; Rosch, W.; Langguth, P. Evidence for intestinal secretion as an additional clearance pathway of talinolol enantiomers: concentration-and dose-dependent absorption in vitro and in vivo. Pharm. Res. 1996, 13, 514-22.
8. Burton, P. S.; Conradi, R. A.; Hilgers A. R.; Ho, N. F. Evidence for a polarized efflux system for peptides in the apical membrane of Caco-2 cells. Biochem. Biophys. Res. Commun. 1993, 190: 760-6.
9. Toppmeyer, D. L.; Slapak, C. A.; Croop, J.; Kufe, D. W. Role of P-glycoprotein in dolastatin 10 resistance. Biochem. Pharmacol. 1994, 48, 609-12.
10. Sarkadi, B.; Muller, M.;. Homolya, L.; Hollo, Z.; Seprodi, J.; Germann, U. A.; Gottesman, M. M.; Price, E. M.; Boucher, R. Interaction of bioactive hydrophobic peptides with the human multidrug transporter. C. FASEB J. 1994, 8, 766-70.
11. Smit, J. J.; Schinkel, A. H.; Mol, C. A.; Majoor, D.; Mooi, W. J.; Jongsma, A. P.; Lincke, C. R.; Borst, P. Tissue distribution of the human MDR3 P-glycoprotein [see comments] [published erratum appears in Lab. Invest. 1995, Mar, 72(3), following table of contents]. Lab Invest. 1994, 71, 638-49.
12. Hosoya, K; Kim K. J.; Lee, V. H. L. Expression of P-glycoprotein, a drug efflux pump, in Caco-2 cell monolayers as a function of age. Pharm. Res. 1996, 13, 885-890.
13. Hoskins, J.; DeHerdt S. V.; Moore R. E.; Bumol T. F. The development and characterization of Vinca alkaloid-resistant Caco-2 human colorectal cell lines expressing mdr-1. Int. J Cancer 1993, 53, 680-8.
14. Wils, P.; Phung-Ba, V.; Warnery, A.; Lechardeur, D.; Raeissi, S.; Hidalgo, I. J.; Scherman, D. Polarized transport of docetaxel and vinblastine mediated by P-glycoprotein in human intestinal epithelial cell monolayers. Biochem. Pharmacol. 1994a, 48, 1528-30.
15. Wils, P.; Warnery, A.; Phung-Ba, V.; Legrain, S.; Scherman D. High lipophilicity decreases drug transport across intestinal epithelial cells. J. Pharmacol Exp. Ther. 1994b, 269, 654-658.
16. Bohner Lang, V.; Langguth, P.; Ottiger, C.; Wunderli-Allenspach, H.; Rognan, D.; Rothen-Rutishauser, B.; Perriard, J. C.; Lang, S.; Biber, J.; Merkle, H. P. Structure-permeation relations of met-enkephalin peptide analogues on absorption and secretion mechanisms in Caco-2 cell monolayers. J. Pharm. Sci. 1996, 86, 846-853.
17. Lehel, C.; Los, D.; Wada, H.; Gyorgyei, J.; Horvath, I.; Kovacs, E.; Murata, N.; Vigh, L. A second groEL-like gene, organized in a groESL operon is present in the genome of Synechocystis sp. PCC 6803. J. Biol. Chem. 1993, 268, 1799-804.
18. Thiebaut, F.; Tsuruo, T.; Hamada, H.; Gottesman, M. M.; Pastan, I.; Willingham, M. C. Immunohistochemical localization in normal tissues of different epitopes in the multidrug transport protein P170: evidence for localization in brain capillaries and crossreactivity of one antibody with a muscle protein. J. Histochem. Cytochem. 1989, 37, 159-64.
19. Georges, E.; Bradley, G.; Gariepy, J.; Ling, V. Detection of P-glycoprotein isoforms by gene-specific monoclonal antibodies. Proc. Natl. Acad. Sci. U.S.A. 1990, 87, 152-6.
20. Muller, C.; Bailly, J. D.; Goubin, F.; Laredo, J.;. Jaffrezou, J. P.; Bordier, C.; Laurent, G. Verapamil decreases P-glycoprotein expression in multidrug-resistant human leukemic cell lines. Int. J. Cancer 1994, 56, 749-54.
21. Rubas, W.; Jezyk, N.; Grass, G. M. Flux Measurements Across Caco-2 Monolayers May Predict Transport In Human Large Intestinal Tissue. Pharm. Res. 1993, 10, 113-8.
22. Endo, K.; Maehara, Y.; Ichiyoshi, Y.; Kusumoto, T.; Sakaguchi, Y.; Ohno, S.; Sugimachi, K. Multidrug resistance-associated protein expression in clinical gastric carcinoma. Cancer 1996, 77, 1681-7.