Contribution of Hydrophobicity of Nonionic Detergents to Membrane Lipid Fluidity and Disopyramide Uptake by Rat Intestinal Brush-Border Membrane Vesicles
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概要
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The contribution of hydrophobicity of different types of detergents to disopyramide uptake by rat small intestinal brush-border membrane vesicles was studied in relation to their membrane lipid fluidity and the physicochemical parameters of the detergents, i.e., hydrophile-lipophile balance (HLB). Span-, Tween-type detergents or glycerol esters at non-solubilizing concentrations (0.01-0.05% (w/v)) decreased the extent of maximum uptake of the drug in the presence of outward H^+ -gradient, but not in the absence of the gradient. The fluorescence anisotropy of the vesicles using diphenylhexatriene (DPH), as reflected by its incorporation into the membrane inner lipid layer, decreased with the addition of all detergents used. In contrast, that of the vesicles using trimethylammoniumphenyl phenylhexatriene (TMA-DPH), which reflected its incorporation into the membrane outer lipid layer, increased depending on the concentration of Tween-type detergents except for Tween 81 and Tween 85,glycerol esters (MO-500,MO-750,ML-500 and ML-750); it decreased with the addition of Span-type detergents, Tween 81 and glycerol ester (MO-310). Therefore, the membrane lipid fluidity change of the outer leaflet, rather than the inner lipophilic domain, of the membrane vesicles caused by the detergents was found to be dependent on the hydrophobicity, but not on the type of detergent. This seems to correlate with the inhibitory effects on the facilitated uptake of the drug by the membrane vesicles.
- 公益社団法人日本薬学会の論文
- 1997-06-15
著者
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村上 正裕
京都薬科大学 薬剤
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MURAKAMI Masahiro
Department of Synthetic Chemistry and Biological Chemistry, Graduate School of Engineering, Kyoto Un
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村上 正裕
天藤製薬
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Koga Kenjiro
Department Of Pharmaceutics Faculty Of Pharmaceutical Sciences Hokuriku University
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Koga Kenjiro
Division Of Pharmaceutical Information Research Laboratory For Development Of Medicine Faculty Of Ph
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Murakami Masahiro
Kyoto Research Laboratory Amato Pharmaceutical Products
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KAWASHIMA Susumu
Division of Pharmaceutical Information, Faculty of Pharmaceutical Sciences, Hokuriku University
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Murakami Masahiro
Department Of Biopharmaceutics Kyoto Pharmaceutical University
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古賀 憲司
Department Of Pharmaceutics Faculty Of Pharmaceutical Sciences Hokuriku University
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Murakami M
Showa Univ. Tokyo Jpn
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Kawashima S
Faculty Of Pharmaceutical Science Hokuriku University
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村上 正裕
京都薬大 薬剤学
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村上 正裕
京都薬科大学
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Murakami Masahiro
Department Of Aquatic Bioscience Graduate School Of Agricultural And Life Sciences The University Of
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MURAKAMI Masahiro
Department of Anatomy, Kurume University School of Medicine
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