Inhibition of Vinblastine Efflux Mediated by P-Glycoprotein by Grapefruit Juice Components in Caco-2 Cells
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概要
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We investigated the effect of components in grapefuit juice (GFJ) on the transport of vinblastine, a substrate of P-glycoprotein (P-gp), across Caco-2 cells. The apical to basolateral flux of [^3H]vinblastine was increased in the presence of GFJ extracts. The steady-state uptake of [^3H]vinblastine from the apical side was significantly increased in the prsence of GFJ in a dose-dependent manner within the range of 2.5 to 50% (v/v) of GFJ. Although naringin and naringenin reduced apial efflux of [^3H]vinblastine at the concentration prenset in GFJ and increased steady-state uptake from the apical side to 124 to 240%, respectively, the observed effect of naringin was not enough to account for the effect of GFJ and naringenin is not naturally present in GFJ. To investigate the effective components in GFJ, we examined the inhibitory effect of several organic solvent extracts of GFJ on the transport of [^3H]vinblastine in Caco-2 cells. Organic solvent extracts of GFJ enhanced the apical to basolateral transcellular transport and inhibited the apical efflux. The permeability coefficient of apical to basolateral transport of [^3H]vinblastine increased in the order of the ethyl acetate>diethyl ether>methylene chloride extracts of GFJ. Since the extracted amount of naringenin by ethyl acetate was less than that with the other organic solvents, the primary inhibitor in GFJ is suggested to be different from this flavonoid. The present study demonstated the existence of inhibitory components in GFJ for the P-gp function in Caco-2 cells, which are distinct from known components such as naringin or naringenin.
- 公益社団法人日本薬学会の論文
- 1998-10-15
著者
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SAWADA Yasufumi
Laboratory of Drug Informatics, Graduate School of Pharmaceutical Sciences, The University of Tokyo
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Sawada Y
Department Of Pharmaceutics Graduate School Of Pharmacertical Sciences Kyushu University
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Sawada Yasufumi
Department Of Pharmacy The University Of Tokyo Hospital Faculty Of Medicine University Of Tokyo
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Ohnishi Ayako
Department Of Pharmaceutics Faculty Of Pharmaceutical Sciences Kyushu University
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Ohnishi Ayako
Department Of Ophthalmology Diabetes Center Tokyo Women's Medical University School Of Medicine
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Takanaga Hitomi
Department Of Molecular Biopharmacy And Genetics Graduate School Of Pharmaceutical Sciences Tohoku U
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Matsuo H
Department Of Pharmaceutics Graduate School Of Pharmacertical Sciences Kyushu University
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MATSUO Hirotami
Department of Pharmaceutics, Graduate School of Pharmacertical Sciences, Kyushu University
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Matsuo Hirotami
Department of Biopharmaceutics, Graduate School of Pharmaceutical Sciences, Kyushu University
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Takanaga Hitomi
Department of Biopharmaceutics, Graduate School of Pharmaceutical Sciences, Kyushu University
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