Efflux properties of basolateral peptide transporter in human intestinal cell line Caco-2

Pflügers Archiv : European journal of physiology
Megumi IrieKen-Ichi Inui

Abstract

Small peptides and some pharmacologically active compounds are absorbed from the small intestine by the apical H(+)-coupled peptide transporter 1 (PEPT1) and the basolateral peptide transporter. Here we investigated the efflux properties of the basolateral peptide transporter in Caco-2 cells using two strategies, efflux measurements and a kinetic analysis of transepithelial transport of glycylsarcosine (Gly-Sar). [(14)C]Gly-Sar efflux through the basolateral membrane was not affected significantly by the external pH. Both approaches revealed that the basolateral peptide transporter was saturable in the efflux direction, and that the affinity was lower than that in the influx direction. For two peptide-like drugs, there was no difference in substrate recognition by the basolateral peptide transporter between the two sides of the membrane. Using the kinetic parameters of PEPT1 and the basolateral peptide transporter, a computational model of Gly-Sar transport in Caco-2 cells was constructed. The simulation fitted the experimental data well. Our findings suggested that substrate affinity of the basolateral peptide transporter is apparently asymmetric, but pH-dependence and substrate specificity are symmetric for the two directions...Continue Reading

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Citations

Nov 12, 2005·Pflügers Archiv : European journal of physiology·Megumi IrieKen-Ichi Inui
Feb 19, 2004·American Journal of Respiratory Cell and Molecular Biology·David A GronebergHannelore Daniel
Mar 3, 2007·Biological & Pharmaceutical Bulletin·Yukiko KomoriYuji Kurosaki
Apr 25, 2008·Expert Opinion on Drug Metabolism & Toxicology·Huadong SunK Sandy Pang
Nov 17, 2006·Journal of Infection and Chemotherapy : Official Journal of the Japan Society of Chemotherapy·Akira Tsuji
Apr 18, 2008·The Journal of Pharmacy and Pharmacology·Matthias BrandschEva Bosse-Doenecke
Jun 7, 2013·The Journal of Pharmacy and Pharmacology·Ragna BerthelsenBirger Brodin
May 23, 2006·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Rikke AndersenBente Steffansen
Apr 19, 2016·Nutrition Research Reviews·Warren M Miner-Williams, Paul J Moughan
Jan 28, 2015·Nutrition Research Reviews·Warren M Miner-WilliamsPaul J Moughan
Nov 3, 2016·Journal of Comparative Physiology. B, Biochemical, Systemic, and Environmental Physiology·Tiziano VerriAlessandro Romano
Mar 10, 2018·Nutrients·Paulus G M JochemsPrescilla V Jeurink
May 8, 2015·World Journal of Gastrointestinal Pharmacology and Therapeutics·Hugh James Freeman
May 26, 2018·Journal of the Science of Food and Agriculture·Qingbiao XuJianxin Liu
May 3, 2006·Laboratory Investigation; a Journal of Technical Methods and Pathology·Laetitia Charrier, Didier Merlin
Mar 29, 2006·Laboratory Investigation; a Journal of Technical Methods and Pathology·Laetitia CharrierDidier Merlin
Sep 21, 2013·Journal of Animal Science·A CehakG Breves
Oct 13, 2007·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Huadong Sun, K Sandy Pang
Aug 9, 2019·Molecular Nutrition & Food Research·Florian RohmBritta Spanier
Feb 22, 2007·The Journal of Nutrition·Caroline BauchartDidier Rémond
Oct 3, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Lourdes Amigo, Blanca Hernández-Ledesma

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