Interplay between CYP3A-mediated metabolism and polarized efflux of terfenadine and its metabolites in intestinal epithelial Caco-2 (TC7) cell monolayers.

作者: Shamsi D. Raeissi , Ismael J. Hidalgo , Juan Segura‐Aguilar , Per Artursson

DOI: 10.1023/A:1018851919674

关键词: EffluxBiochemistryTerfenadineCytochrome P450BiologyMetabolismCYP3ACellIntestinal epitheliumCell Clone

摘要: Purpose. To further characterize cytochrome P450 (CYP) and P-glyco-protein (Pgp) expression in monolayers of the Caco-2 cell clone TC7, a culture model human intestinal epithelium. study interplay between CYP3A Pgp as barriers to drug absorption TC7 cells using terfenadine its metabolites substrates.

参考文章(27)
Rikard Sandström, Intestinal permeability and presystemic metabolism of R/S-verapamil and fluvastatin Acta Universitatis Upsaliensis. ,(1998)
Shamsi D. Raeissi, Zuyu Guo, Glenn L. Dobson, Per Artursson, Ismael J. Hidalgo, Comparison of CYP3A activities in a subclone of Caco-2 cells (TC7) and human intestine Pharmaceutical Research. ,vol. 14, pp. 1019- 1025 ,(1997) , 10.1023/A:1012197110917
Rikard Sandström, Anders Karlsson, Lars Knutson, Hans Lennernäs, Jejunal absorption and metabolism of R/S-verapamil in humans. Pharmaceutical Research. ,vol. 15, pp. 856- 862 ,(1998) , 10.1023/A:1011916329863
P. H. Beaune, Chung Yang, I. De Waziers, J. P. Leroux, P. H. Cugnenc, Cytochrome P 450 isoenzymes, epoxide hydrolase and glutathione transferases in rat and human hepatic and extrahepatic tissues Journal of Pharmacology and Experimental Therapeutics. ,vol. 253, pp. 387- 394 ,(1990)
C Roque, H Joyeux, I Fabre, M Bourrie, X Boulenc, G Fabre, Y Berger, Regulation of cytochrome P450IA1 gene expression in a human intestinal cell line, Caco-2. Journal of Pharmacology and Experimental Therapeutics. ,vol. 263, pp. 1471- 1478 ,(1992)
William N. Hait, Joan F. Gesmonde, John R. Murren, Yang Jin-Ming, Chen Hong-Xing, Michael Reiss, Terfenadine (seldane®): A new drug for restoring sensitivity to multidrug resistant cancer cells☆ Biochemical Pharmacology. ,vol. 45, pp. 401- 406 ,(1993) , 10.1016/0006-2952(93)90076-9
Kari T. Kivistö, Pertti J. Neuvonen, Ulrich Klotz, Inhibition of terfenadine metabolism. Pharmacokinetic and pharmacodynamic consequences. Clinical Pharmacokinectics. ,vol. 27, pp. 1- 5 ,(1994) , 10.2165/00003088-199427010-00001
M.G. Mercurio, S.J. Shiff, R.A. Galbraith, S. Sassa, Expression of Cytochrome P450 mRNAs in the Colon and the Rectum in Normal Human Subjects Biochemical and Biophysical Research Communications. ,vol. 210, pp. 350- 355 ,(1995) , 10.1006/BBRC.1995.1668
A. Sparreboom, J. van Asperen, U. Mayer, A. H. Schinkel, J. W. Smit, D. K. F. Meijer, P. Borst, W. J. Nooijen, J. H. Beijnen, O. van Tellingen, Limited oral bioavailability and active epithelial excretion of paclitaxel (Taxol) caused by P-glycoprotein in the intestine Proceedings of the National Academy of Sciences of the United States of America. ,vol. 94, pp. 2031- 2035 ,(1997) , 10.1073/PNAS.94.5.2031
Joseph C. Kolars, Kenneth S. Lown, Phyllissa Schmiedlin-Ren, Mita Ghosh, Che Fang, Steven A. Wrighton, Robert M. Merion, Paul B. Watkins, CYP3A gene expression in human gut epithelium. Pharmacogenetics. ,vol. 4, pp. 247- 259 ,(1994) , 10.1097/00008571-199410000-00003