PMID: 9530984Apr 8, 1998Paper

Intestinal absorption of stable cyclic dipeptides by the oligopeptide transporter in rat

The Journal of Pharmacy and Pharmacology
T MizumaS Awazu

Abstract

Intestinal absorption of four cyclic dipeptides was studied in the everted small intestine of the rat. Cyclic seryltyrosine (cyclo(Ser-Tyr)) was stable enough to be transported whereas linear seryltyrosine was not. The absorption clearance of cyclo(Ser-Tyr) was concentration-dependent, and for cyclo(Ser-Tyr) at 125 microM decreased in the presence of glycylsarcosine (10 mM) or cephalexin (10 mM), which were reported to be absorbed by oligopeptide transporter. The absorption clearance was also reduced at 4 degrees C and in the presence of 1 mM dinitrophenol. Kinetic analysis of cyclo(Ser-Tyr) absorption showed that Km and Vmax were 19.8 microM and 0.295 nmol min(-1) cm(-1), respectively. It was also suggested that cyclic aspartylphenylalanine and cyclic histidylphenylalanine were absorbed by oligopeptide transporters, but cyclic histidylproline was not. The absorption clearance of cyclo(Ser-Tyr) in the control was much higher than the value of the correlation line representing a plot of passive transport (which was obtained from the absorption clearance of cyclic peptides in the presence of glycylsarcosine (10 mM)) against hydrophobicity (oil-water partition coefficient). These results indicate that cyclo(Ser-Tyr) is absorbed by...Continue Reading

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Citations

Jul 29, 2000·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·E I LepistB Steffansen
Dec 21, 2005·European Journal of Pharmacology·Gökhan GöktalayWilliam R Millington
Oct 3, 2002·The Journal of Pharmacy and Pharmacology·Takashi MizumaShoji Awazu
Jan 18, 2018·Journal of Agricultural and Food Chemistry·Hiroshi AshigaiHiroaki Yajima

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