Pharmacological characteristics of the specific transporter for the endogenous cell growth inhibitor agmatine in six tumor cell lines

International Journal of Colorectal Disease
Anja HeinenGerhard J Molderings

Abstract

This study examined agmatine transport into six human intestinal tumor cell lines and compared the pharmacological properties of this transporter with those of the agmatine carrier previously characterized in human glioblastoma cells. Carrier-mediated uptake was determined as specific accumulation of [(14)C]agmatine in the cells. The changes in intracellular agmatine concentration in the tumor cells after 24 h incubation with 1 mM agmatine was analyzed by high-performance liquid chromatography. Specific [(14)C]agmatine accumulation was found in the six human intestinal tumor cell lines Caco2, Cx1, Colo320, HT29, Colo205E, and SW480. Specific [(14)C]agmatine accumulation was inhibited by phentolamine, putrescine, spermine, clonidine, and decynium-22 but not by corticosterone, O-methylisoprenaline, or l-carnitine. Incubation with exogenous agmatine for 24 h increased intracellular agmatine content in all cell lines by a multiple of the basal endogenous content. Transfection of HEK293 cells with cDNA encoding either hOCT1, hOCT2, or hOCT3 did not enhance [(14)C]agmatine accumulation compared to nontransfected cells. All intestinal tumor cell lines investigated express a functional specific agmatine transporter which exhibit pharma...Continue Reading

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Citations

Oct 4, 2008·American Journal of Physiology. Gastrointestinal and Liver Physiology·Britta HaenischGerhard J Molderings
Mar 30, 2019·Frontiers in Nutrition·Bruno Ramos-MolinaRafael Peñafiel
May 16, 2021·Naunyn-Schmiedeberg's Archives of Pharmacology·H BönischE Schlicker
Dec 7, 2010·Molecular Pharmaceutics·Tate N WinterCarolyn A Fairbanks
Jan 4, 2012·Pharmacology & Therapeutics·Gerhard J Molderings, Britta Haenisch

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