Functional Characterization of the Carrier-Mediated Transport System for Glycerol in Everted Sacs of the Rat Small Intestine(Biopharmacy)
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概要
- 論文の詳細を見る
The mechanism of intestinal glycerol transport was investigated by using the in vitro everted sac method involving the rat small intestine. The uptake of glycerol into everted sacs was saturable with a Michaelis constant (K_m) of 0.77 mM and a maximum transport rate (J_<max>) of 11.5 nmol/min/100 mg wet tissue weight (wtw), suggesting the involvement of carrier-mediated transport, and was accompanied by unsaturable transport (passive transport) with a membrane permeability clearance (CL_<m,d>) of 4.9μl/min/100mg wtw. The carrier-mediated uptake of glycerol was inhibited by the removal of Na^+ and also by the addition of 2,4-dinitrophenol (DNP) and sodium azide (NaN_3), which are metabolic inhibitors. These results suggest that the carrier-mediated glycerol transport is Na^+-dependent and secondary active. Since glycerol uptake was also inhibited by β-chloromercuribenzene sulfonate (pCMBS), a thiol-modifying reagent, cysteine residues, which have a thiol group, seem to play an important role in the function of the carrier. We further found that glycerol uptake was selectively inhibited by glycerol-3-phosphate, chloramphenicol and voglibose, which are alcohol-related compounds analogous to glycerol. Several other compounds that did not inhibit glycerol uptake included D-glucose and 5-fluorouracil, which are known to be transported by specific carriers, and none of the selective inhibitors of glycerol uptake inhibited the uptake of D-glucose and 5-fluorouracil. Therefore, the carriers for these two compounds do not seem to be involved in glycerol uptake. It is likely that the carrier-mediated transport system involved in glycerol uptake is specific to glycerol and, possibly, some analogous compounds with hydroxyl groups. It would be interesting to examine the possibility that the carrier-mediated glycerol transport system might be involved in drug absorption and also that it might be used for oral drug delivery.
- 社団法人日本薬学会の論文
- 2004-11-01
著者
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Hayashi Yoshie
Department Of Pharmacy Kyoto University Hospital Faculty Of Medicine Kyoto University
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Hayashi Yoshie
京都大学医学部附属病院 薬剤
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林 弥生
College Of Pharmacy Kinjo Gakuin University
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Kato T
Graduate School Of Pharmaceutical Sciences Nagoya City University
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Kato Toyonori
名古屋市立大学 薬学研究科
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INOUE Katsuhisa
Graduate School of Pharmaceutical Sciences, Nagoya City University
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YUASA Hiroaki
Graduate School of Pharmaceutical Sciences, Nagoya City University
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HAYASHI Yayoi
Graduate School of Pharmaceutical Sciences, Nagoya City University
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KATO Toyonori
Graduate School of Pharmaceutical Sciences, Nagoya City University
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Kato Toyonori
Graduate School Of Pharmaceutical Sciences Nagoya City University
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Inoue K
Gifu Pharmaceutical University
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Huang Ye
Department Of Pharmacy Kyoto University Hospital Faculty Of Medicine Kyoto University
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Itoh Kunihiko
Department Of Clinical Pharmacology And Genetics School Of Pharmaceutical Sciences University Of Shi
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Yuasa H
Department Of Pharmaceutics And Drug Delivery School Of Pharmacy Tokyo University Of Pharmacy And Li
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Hayashi Yayoi
Graduate School Of Pharmaceutical Sciences Nagoya City University
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Yuasa Hiroaki
Department Of Biopharmaceutics Graduate School Of Pharmaceutical Sciences Nagoya City University
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Yuasa Hiroaki
Graduate School Of Pharmaceutical Sciences Nagoya City University
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井上 勝央
名古屋市立大学大学院薬学研究科薬物動態制御学分野
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Hayashi Y
Life Science Laboratories Central Research Laboratories Ajinomoto Co. Inc.:pharmaceuticals Research
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Hayashi Yayoi
Department Of Biopharmaceutics Faculty Of Pharmaceutical Sciences Nagoya City University
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Inoue Katsuhisa
Graduate School Of Pharmaceutical Sciences Nagoya City University
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