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01-07-2007 | Original Paper

Regulation of the Oligopeptide Transporter, PEPT-1, in DSS-Induced Rat Colitis

Authors: Genia Radeva, Marion Buyse, Patrick Hindlet, Benjamin Beaufils, Francine Walker, André Bado, Robert Farinotti

Published in: Digestive Diseases and Sciences | Issue 7/2007

Abstract

The effect of colitis induced with dextran sodium sulfate (DSS) in rats on the bioavailability of drugs transported by the oligopeptide transporter PepT-1 was analyzed by studying the pharmacokinetics of PepT-1 substrates: cephalexin and valacyclovir, the prodrug of antiviral acyclovir. Western blot, immunohistochemistry, and real-time PCR were used to determine the PepT-1 protein and gene expression. We observed (1) no significant modification of PepT-1 expression in the duodenum and jejunum; (2) a slight decrease in both PepT-1 mRNA (50%) and protein expression (25%) in the ileum following DSS challenge; and (3) ectopic PepT-1 immunostaining in regenerative hyperplasia segments in the distal colon from DSS-treated rats where focal inflammation is localized. However, no modification of pharmacokinetic parameters (C _max, T _max, AUC) of cephalexin or acyclovir was detected. In conclusion, DSS-induced rat colitis did not alter PepT-1 substrate bioavailability despite certain modifications in PepT-1 expression profile.

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Title: Regulation of the Oligopeptide Transporter, PEPT-1, in DSS-Induced Rat Colitis
Authors: Genia Radeva
Marion Buyse
Patrick Hindlet
Benjamin Beaufils
Francine Walker
André Bado
Robert Farinotti
Publication date: 01-07-2007
Publisher: Kluwer Academic Publishers-Plenum Publishers
Published in: Digestive Diseases and Sciences / Issue 7/2007
Print ISSN: 0163-2116
Electronic ISSN: 1573-2568
DOI: https://doi.org/10.1007/s10620-006-9667-2

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