PMID: 9416764Jan 1, 1997Paper

Enhancement of the small intestinal uptake of phenylalanylglycine via a H+/oligopeptide transport system by chemical modification with fatty acids

Life Sciences
T FujitaS Muranishi

Abstract

The transport characteristics of chemically modified phenylalanylglycine (Phe-Gly) with butyric acid (C4-Phe-Gly) and caproic acid (C6-Phe-Gly) were examined using rabbit intestinal brush-border membrane vesicles (BBMVs). In the presence of an inwardly H+ gradient (pH 7.5 inside, pH 6.0 outside), the uptake of Phe-Gly via BBMVs was significantly enhanced by the covalent attachment of butyric or caproic acid to the N-terminal of Phe-Gly. Moreover, C4-Phe-Gly uptake was stimulated by the trans-stimulation effect of some dipeptides and cefadroxil, and was inhibited by other dipeptides and cefadroxil. These results indicate that N-terminal modified Phe-Gly with fatty acids are transported into BBMVs via an oligopeptide transporter. Therefore, chemical modification of dipeptides with fatty acids can enhance the intestinal absorption of dipeptide by a carrier-mediated transport via an oligopeptide transporter.

References

Jul 1, 1992·The Journal of Pharmacy and Pharmacology·M HashizumeS Muranishi
Sep 1, 1992·The Journal of Pharmacy and Pharmacology·K YamadaS Muranishi
Nov 1, 1981·Journal of Pharmacobio-dynamics·K YamaokaT Uno
Oct 1, 1995·The Journal of Pharmacy and Pharmacology·K SetohS Muranishi

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Citations

Jan 5, 2002·Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan·A Yamamoto
Oct 31, 2002·Pharmacology & Toxicology·Birger BrodinSven Frøkjaer
Dec 21, 2006·International Journal of Pharmaceutics·Nathalie OulianovaYanmin Chen
Dec 10, 1999·Current Opinion in Clinical Nutrition and Metabolic Care·D F NuttingC M Mansbach
Oct 7, 2006·Current Opinion in Gastroenterology·D F NuttingC M Mansbach
Mar 24, 2020·Pharmacology & Therapeutics·Akira YamamotoHidemasa Katsumi
Jun 9, 2006·Journal of Medicinal Chemistry·Balvinder S VigTeresa N Faria
Oct 6, 2009·Advanced Drug Delivery Reviews·Sam MaherDavid J Brayden

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