Reactive oxygen species (ROS) produced by gut mucosal cells during conditions such as inflammatory bowel disease (IBD) may impair mucosal repair and nutrient transport/absorptive function. Absorption of di- and tripeptides in the small intestine and colon is mediated by the H(+)-dependent transporter PepT1, but effects of oxidative stress on di- and tripeptide transport are unknown. We assessed whether exposure to hydrogen peroxide (H(2)O(2)) influences dipeptide transport in human colonic epithelial (Caco-2) cells.
View Article and Find Full Text PDFIn this report, we studied the functional characteristics of a brain peptide transporter using synaptosomes prepared from rat cerebral cortex. Crude synaptosomes (P(2) fraction) were prepared from cerebral cortices in male Wistar rats. Uptake of [14C]glycylsarcosine (Gly-Sar), a substrate for H(+)/oligopeptide transporters PEPT1 and PEPT2, and [3H]histidine, a substrate for peptide/histidine transporters PHT1 and PHT2, was measured at 37 degrees C by a rapid filtration technique.
View Article and Find Full Text PDFEur J Pharm Sci
January 2004
Peptide transporter 1, PEPT1, of the mammalian enterocyte is presently under intense investigation in many laboratories because of its nutritional importance in the absorption of protein hydrolysis products and because more recent studies have shown that many drugs and prodrugs gain entry into the systemic circulation via PEPT1. Until the exact structural features of the substrate binding site of PEPT1 become available, for example by X-ray crystallography, determination of affinities followed by proof of actual membrane translocation will have to suffice when testing for possible new substrates for PEPT1. Affinity constants reflect the strength of their interaction with the binding site of the transporter.
View Article and Find Full Text PDFBackground: Depression has been associated with a decrease in intracellular serotonin (5-HT) reuptake through its transporter, SERT. The 5-HT transporter long promoter region (5-HTTLPR) deletion in the SERT gene has also been associated with a decrease in 5-HT reuptake. Conversely, increases in extracellular 5-HT have been associated with increased temperature.
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