Methotrexate Increases Skeletal Muscle GLUT4 Expression and Improves Metabolic Control in Experimental Diabetes

Long-term administration of 5-aminoimidazole-4-carboxamide ribonucleoside (AICAR) mimics the effects of endurance exercise by activating AMP kinase and by increasing skeletal muscle expression of GLUT4 glucose transporter. AICAR is an intermediate in the purine de novo synthesis, and its tissue conc...

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Main Authors: Giuseppina T. Russo, Letteria Minutoli, Alessandra Bitto, Domenica Altavilla, Eugenio Alessi, Annalisa Giandalia, Elisabetta L. Romeo, Maria Francesca Stagno, Francesco Squadrito, Domenico Cucinotta, Jacob Selhub
Format: Article
Language:English
Published: Wiley 2012-01-01
Series:Journal of Nutrition and Metabolism
Online Access:http://dx.doi.org/10.1155/2012/132056
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author Giuseppina T. Russo
Letteria Minutoli
Alessandra Bitto
Domenica Altavilla
Eugenio Alessi
Annalisa Giandalia
Elisabetta L. Romeo
Maria Francesca Stagno
Francesco Squadrito
Domenico Cucinotta
Jacob Selhub
author_facet Giuseppina T. Russo
Letteria Minutoli
Alessandra Bitto
Domenica Altavilla
Eugenio Alessi
Annalisa Giandalia
Elisabetta L. Romeo
Maria Francesca Stagno
Francesco Squadrito
Domenico Cucinotta
Jacob Selhub
author_sort Giuseppina T. Russo
collection DOAJ
description Long-term administration of 5-aminoimidazole-4-carboxamide ribonucleoside (AICAR) mimics the effects of endurance exercise by activating AMP kinase and by increasing skeletal muscle expression of GLUT4 glucose transporter. AICAR is an intermediate in the purine de novo synthesis, and its tissue concentrations can be increased, in vivo, by low doses of methotrexate (MTX) through the inhibition of the enzyme AICAR transformylase. We report here the first evidence that, in experimental type 2 diabetes, chronic treatment with low doses of MTX increases skeletal muscle GLUT4 expression and improves metabolic control. MTX (0.5 mg/kg body weight) or vehicle was administered intraperitoneally, once a week for 4 weeks, to genetically diabetic female C57BL/KsJ-m+/+Leptdb mice (db+/db+) and their normoglycemic littermates (db+/+m). In the db+/db+ mice, MTX treatment was associated with a ∼2-fold increase in skeletal muscle GLUT4 protein concentration and a >4-fold increase in GLUT4 mRNA expression (P<0.01, all), as compared to vehicle-treated mice; no significant differences were noted in controls. MTX treatment was also associated with a significant reduction of glucose and insulin serum concentrations in diabetic mice (P<0.001), and glucose levels only (P<0.05) in controls. These data indicate a different route to increase skeletal muscle GLUT4 expression, through the potential inhibition of the enzyme AICAR transformylase.
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spelling doaj-art-9b45a9b7b29a4b538da39f59c14faef52025-08-20T03:36:57ZengWileyJournal of Nutrition and Metabolism2090-07242090-07322012-01-01201210.1155/2012/132056132056Methotrexate Increases Skeletal Muscle GLUT4 Expression and Improves Metabolic Control in Experimental DiabetesGiuseppina T. Russo0Letteria Minutoli1Alessandra Bitto2Domenica Altavilla3Eugenio Alessi4Annalisa Giandalia5Elisabetta L. Romeo6Maria Francesca Stagno7Francesco Squadrito8Domenico Cucinotta9Jacob Selhub10Department of Internal Medicine, University of Messina, 98122 Messina, ItalySection of Pharmacology, Department of Clinical and Experimental Medicine and Pharmacology, University of Messina, 98122 Messina, ItalySection of Pharmacology, Department of Clinical and Experimental Medicine and Pharmacology, University of Messina, 98122 Messina, ItalySection of Pharmacology, Department of Clinical and Experimental Medicine and Pharmacology, University of Messina, 98122 Messina, ItalyDepartment of Internal Medicine, University of Messina, 98122 Messina, ItalyDepartment of Internal Medicine, University of Messina, 98122 Messina, ItalyDepartment of Internal Medicine, University of Messina, 98122 Messina, ItalyDepartment of Internal Medicine, University of Messina, 98122 Messina, ItalySection of Pharmacology, Department of Clinical and Experimental Medicine and Pharmacology, University of Messina, 98122 Messina, ItalyDepartment of Internal Medicine, University of Messina, 98122 Messina, ItalyVitamin Bioavailability Laboratory, Jean Mayer USDA Human Nutrition Research Center on Aging, Tufts University, Boston, MA 02111, USALong-term administration of 5-aminoimidazole-4-carboxamide ribonucleoside (AICAR) mimics the effects of endurance exercise by activating AMP kinase and by increasing skeletal muscle expression of GLUT4 glucose transporter. AICAR is an intermediate in the purine de novo synthesis, and its tissue concentrations can be increased, in vivo, by low doses of methotrexate (MTX) through the inhibition of the enzyme AICAR transformylase. We report here the first evidence that, in experimental type 2 diabetes, chronic treatment with low doses of MTX increases skeletal muscle GLUT4 expression and improves metabolic control. MTX (0.5 mg/kg body weight) or vehicle was administered intraperitoneally, once a week for 4 weeks, to genetically diabetic female C57BL/KsJ-m+/+Leptdb mice (db+/db+) and their normoglycemic littermates (db+/+m). In the db+/db+ mice, MTX treatment was associated with a ∼2-fold increase in skeletal muscle GLUT4 protein concentration and a >4-fold increase in GLUT4 mRNA expression (P<0.01, all), as compared to vehicle-treated mice; no significant differences were noted in controls. MTX treatment was also associated with a significant reduction of glucose and insulin serum concentrations in diabetic mice (P<0.001), and glucose levels only (P<0.05) in controls. These data indicate a different route to increase skeletal muscle GLUT4 expression, through the potential inhibition of the enzyme AICAR transformylase.http://dx.doi.org/10.1155/2012/132056
spellingShingle Giuseppina T. Russo
Letteria Minutoli
Alessandra Bitto
Domenica Altavilla
Eugenio Alessi
Annalisa Giandalia
Elisabetta L. Romeo
Maria Francesca Stagno
Francesco Squadrito
Domenico Cucinotta
Jacob Selhub
Methotrexate Increases Skeletal Muscle GLUT4 Expression and Improves Metabolic Control in Experimental Diabetes
Journal of Nutrition and Metabolism
title Methotrexate Increases Skeletal Muscle GLUT4 Expression and Improves Metabolic Control in Experimental Diabetes
title_full Methotrexate Increases Skeletal Muscle GLUT4 Expression and Improves Metabolic Control in Experimental Diabetes
title_fullStr Methotrexate Increases Skeletal Muscle GLUT4 Expression and Improves Metabolic Control in Experimental Diabetes
title_full_unstemmed Methotrexate Increases Skeletal Muscle GLUT4 Expression and Improves Metabolic Control in Experimental Diabetes
title_short Methotrexate Increases Skeletal Muscle GLUT4 Expression and Improves Metabolic Control in Experimental Diabetes
title_sort methotrexate increases skeletal muscle glut4 expression and improves metabolic control in experimental diabetes
url http://dx.doi.org/10.1155/2012/132056
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