Abstract
Impaired L-carnitine uptake correlates with higher blood pressure in adult men, and L-carnitine restores endothelial function in aortic rings from spontaneously hypertensive rat (SHR). Thus, endothelial dysfunction in hypertension could result from lower L-carnitine transport in this cell type. L-Carnitine transport is mainly mediated by novel organic cation transporters 1 (Octn1, Na(+)-independent) and 2 (Octn2, Na(+)-dependent); however, their kinetic properties and potential consequences in hypertension are unknown. We hypothesize that L-carnitine transport kinetic properties will be altered in aortic endothelium from spontaneously hypertensive rats (SHR). L-Carnitine transport was measured at different extracellular pH (pHo 5.5-8.5) in the absence or presence of sodium in rat aortic endothelial cells (RAECs) from non-hypertensive Wistar-Kyoto (WKY) rats and SHR. Octn1 and Octn2 mRNA relative expression was also determined. Dilation of endothelium-intact or denuded aortic rings in response to calcitonine gene related peptide (CGRP, 0.1-100 nmol/L) was measured (myography) in the absence or presence of L-carnitine. Total L-carnitine transport was lower in cells from SHR compared with WKY rats, an effect due to reduced Na(+)-dependent (Na(+) dep ) compared with Na(+)-independent (Na(+) indep ) transport components. Saturable L-carnitine transport kinetics show maximal velocity (V max), without changes in apparent K m for Na(+) indep transport in SHR compared with WKY rats. Total and Na(+) dep component of transport were increased, but Na(+) indep transport was reduced by extracellular alkalization in WKY rats. However, alkalization reduced total and Na(+) indep transport in cells from SHR. Octn2 mRNA was higher than Octn-1 mRNA expression in cells from both conditions. Dilation of artery rings in response to CGRP was reduced in vessels from SHR compared with WKY rats. CGRP effect was endothelium-dependent and restored by L-carnitine. All together these results suggest that reduced L-carnitine transport (likely via Na(+)-dependent Octn2) could limit this compound's potential beneficial effects in RAECs from SHR.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Aorta / drug effects
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Aorta / metabolism*
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Aorta / pathology
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Biological Transport
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Blood Pressure
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Calcitonin Gene-Related Peptide / pharmacology
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Carnitine / metabolism*
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Carrier Proteins / genetics
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Carrier Proteins / metabolism
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Cells, Cultured
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Endothelial Cells / drug effects
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Endothelial Cells / metabolism*
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Endothelial Cells / pathology
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Endothelium, Vascular / drug effects
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Endothelium, Vascular / metabolism*
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Endothelium, Vascular / pathology
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Gene Expression
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Humans
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Hydrogen-Ion Concentration
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Hypertension / metabolism*
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Hypertension / pathology
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Hypertension / physiopathology
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Kinetics
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Male
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Membrane Proteins / genetics
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Membrane Proteins / metabolism
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Organic Cation Transport Proteins / genetics
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Organic Cation Transport Proteins / metabolism
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Rats
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Rats, Inbred SHR
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Rats, Inbred WKY
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Sodium / metabolism
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Solute Carrier Family 22 Member 5
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Solute Carrier Proteins
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Symporters
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Tissue Culture Techniques
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Vasodilation / drug effects
Substances
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Carrier Proteins
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Membrane Proteins
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Organic Cation Transport Proteins
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Slc22a4 protein, rat
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Slc22a5 protein, rat
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Solute Carrier Family 22 Member 5
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Solute Carrier Proteins
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Symporters
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Sodium
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Calcitonin Gene-Related Peptide
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Carnitine
Grants and funding
This work was supported by Fondo Nacional de Desarrollo Científico y Tecnológico (FONDECYT 1110977, 11100192, 3130583), Chile; Programa de Investigación Interdisciplinario (PIA) from Comisión Nacional de Investigación en Ciencia y Tecnología (CONICYT) (Anillos ACT-73); and Fellowship Apoyo de Tesis CONICYT (AT-24120944, AT-24120940), Chile. E. Guzmán-Gutiérrez and P. Arroyo hold CONICYT-PhD (Chile) fellowships. P. Arroyo was a recipient of Faculty of Medicine, Pontificia Universidad Católica de Chile-Ph.D. fellowship. C. Salomón holds a postdoctoral fellowship at The University of Queensland Centre for Clinical Research (Australia). S. Zambrano, M.V. Ruiz-Armenta and A.J. Blanca were supported by grants from Consejería de Salud, Junta de Andalucía (PI 0034/2008, 0060/2012) and Instituto de Salud Carlos III-Subdirección General de Evaluación y Fomento de la Investigación, PN de I+D+I 2008-2011, Agencia Española de Cooperación Internacional para el Desarrollo (AECID) (C/024225/09, D/031187/10, A1/036123/11), Spain. The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.