Grapefruit juice activates P-glycoprotein-mediated drug transport.
作者： Andrea Soldner , Uwe Christians , Miki Susanto , Vincent J. Wacher , Jeffrey A. Silverman
关键词:
摘要: Purpose. Grapefruit juice (GJ) is known to increase the oral bioavailability of many CYP3A-substrates by inhibiting intestinal phase-I metabolism. However, magnitude AUC often insignificant and highly variable. Since we earlier suggested that CYP3A P-glycoprotein (P-gp) form a concerted barrier drug absorption, investigated role P-gp in GJ-drug interactions.
springer.com
sci-hub.se 参考文章(25)
Joanna Lopaczynska, James M. Phang, Grace Chao Yeh, C. Michael Poore, Flavonol-stimulated efflux of 7,12-dimethylbenz(a)anthracene in multidrug-resistant breast cancer cells Cancer Research. ,vol. 53, pp. 5977- 5981 ,(1993)
James W. Critchfield, Clement J. Welsh, James M. Phang, Grace Chao Yeh, Modulation of adriamycin accumulation and efflux by flavonoids in HCT-15 colon cells. Activation of P-glycoprotein as a putative mechanism. Biochemical Pharmacology. ,vol. 48, pp. 1437- 1445 ,(1994) , 10.1016/0006-2952(94)90568-1
Yuanchao Zhang, Leslie Z. Benet, Characterization of P-glycoprotein Mediated Transport of K02, a Novel Vinylsulfone Peptidomimetic Cysteine Protease Inhibitor, Across MDR1-MDCK and Caco-2 Cell Monolayers Pharmaceutical Research. ,vol. 15, pp. 1520- 1524 ,(1998) , 10.1023/A:1011990730230
M Horio, K V Chin, S J Currier, S Goldenberg, C Williams, I Pastan, M M Gottesman, J Handler, Transepithelial transport of drugs by the multidrug transporter in cultured Madin-Darby canine kidney cell epithelia. Journal of Biological Chemistry. ,vol. 264, pp. 14880- 14884 ,(1989) , 10.1016/S0021-9258(18)63784-6
J. Hunter, M.A. Jepson, T. Tsuruo, N.L. Simmons, B.H. Hirst, Functional expression of P-glycoprotein in apical membranes of human intestinal Caco-2 cells. Kinetics of vinblastine secretion and interaction with modulators. Journal of Biological Chemistry. ,vol. 268, pp. 14991- 14997 ,(1993) , 10.1016/S0021-9258(18)82429-2
U G Eriksson, J Lundahl, A Miniscalco, C G Regårdh, B Edgar, Inhibition of dihydropyridine metabolism in rat and human liver microsomes by flavonoids found in grapefruit juice. Journal of Pharmacology and Experimental Therapeutics. ,vol. 261, pp. 1195- 1199 ,(1992)
Hugo H. T. Kupferschmidt, Karin E. Fattinger, Huy Riem Ha, Ferenc Follath, Stephan Krähenbühl, Grapefruit juice enhances the bioavailability of the HIV protease inhibitor saquinavir in man British Journal of Clinical Pharmacology. ,vol. 45, pp. 355- 359 ,(1998) , 10.1046/J.1365-2125.1998.T01-1-00687.X
Susan E. Rau, John R. Bend, J. Malcolm O. Arnold, Lan T. Tran, J. David Spence, David G. Bailey, Grapefruit juice-terfenadine single-dose interaction: magnitude, mechanism, and relevance. Clinical Pharmacology & Therapeutics. ,vol. 61, pp. 401- 409 ,(1997) , 10.1016/S0009-9236(97)90190-9
K S Lown, D G Bailey, R J Fontana, S K Janardan, C H Adair, L A Fortlage, M B Brown, W Guo, P B Watkins, Grapefruit juice increases felodipine oral availability in humans by decreasing intestinal CYP3A protein expression. Journal of Clinical Investigation. ,vol. 99, pp. 2545- 2553 ,(1997) , 10.1172/JCI119439
I. Pastan, M. M. Gottesman, K. Ueda, E. Lovelace, A. V. Rutherford, M. C. Willingham, A retrovirus carrying an MDR1 cDNA confers multidrug resistance and polarized expression of P-glycoprotein in MDCK cells. Proceedings of the National Academy of Sciences of the United States of America. ,vol. 85, pp. 4486- 4490 ,(1988) , 10.1073/PNAS.85.12.4486