Document Detail


Comparative effects of telmisartan, sitagliptin and metformin alone or in combination on obesity, insulin resistance, and liver and pancreas remodelling in C57BL/6 mice fed on a very high-fat diet.
MedLine Citation:
PMID:  20415664     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The aim of the present study was to evaluate the effects of monotherapies and combinations of drugs on insulin sensitivity, adipose tissue morphology, and pancreatic and hepatic remodelling in C57BL/6 mice fed on a very HF (high-fat) diet. Male C57BL/6 mice were fed on an HF (60% lipids) diet or SC (standard chow; 10% lipids) diet for 10 weeks, after which time the following drug treatments began: HF-T (HF diet treated with telmisartan; 5.2 mg x kg-1 of body weight x day-1), HF-S (HF diet treated with sitagliptin; 1.08 g x kg-1 of body weight.day-1), HF-M (HF diet treated with metformin; 310.0 mg x kg-1 of body weight x day-1), HF-TM (HF diet treated with telmisartan+metformin), HF-TS (HF diet treated with telmisartan+sitagliptin) and HF-SM (HF diet treated with sitagliptin+metformin). Treated groups also had free access to the HF diet, and treatments lasted for 6 weeks. Morphometry, stereological tools, immunostaining, ELISA, Western blot analysis and electron microscopy were used. The HF diet yielded an overweight phenotype, an increase in oral glucose intolerance, hyperinsulinaemia, hypertrophied islets and adipocytes, stage 2 steatosis (>33%), and reduced liver PPAR-alpha (peroxisome-proliferator-activated receptor-alpha) and GLUT-2 (glucose transporter-2) levels, concomitant with enhanced SREBP-1 (sterol-regulatory-element-binding protein-1) expression (P<0.0001). Conversely, all drug treatments resulted in significant weight loss, a reversal of insulin resistance, islet and adipocyte hypertrophy, and alleviated hepatic steatosis. Only the HF-T and HF-TS groups had body weights similar to the SC group at the end of the experiment, and the latter treatment reversed hepatic steatosis. Increased PPAR-alpha immunostaining in parallel with higher GLUT-2 and reduced SREBP-1 expression may explain the favourable hepatic outcomes. Restoration of adipocyte size was consistent with higher adiponectin levels and lower TNF-alpha (tumour necrosis factor-alpha) levels (P<0.0001) in the drug-treated groups. In conclusion, all of the drug treatments were effective in controlling the metabolic syndrome. The best results were achieved using telmisartan and sitagliptin as monotherapies or as a dual treatment, combining partial PPAR-gamma agonism and PPAR-alpha activation in the liver with extended incretin action.
Authors:
Vanessa Souza-Mello; Bianca M Gregório; Fernando S Cardoso-de-Lemos; Laís de Carvalho; Márcia B Aguila; Carlos A Mandarim-de-Lacerda
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2010-06-08
Journal Detail:
Title:  Clinical science (London, England : 1979)     Volume:  119     ISSN:  1470-8736     ISO Abbreviation:  Clin. Sci.     Publication Date:  2010 Sep 
Date Detail:
Created Date:  2010-06-15     Completed Date:  2010-09-03     Revised Date:  2010-09-23    
Medline Journal Info:
Nlm Unique ID:  7905731     Medline TA:  Clin Sci (Lond)     Country:  England    
Other Details:
Languages:  eng     Pagination:  239-50     Citation Subset:  IM    
Affiliation:
Laboratory of Morphometry, Biomedical Center, Institute of Biology, State University of Rio de Janeiro, 20551-030 Rio de Janeiro, RJ, Brazil.
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MeSH Terms
Descriptor/Qualifier:
Adipocytes / pathology
Angiotensin II Type 1 Receptor Blockers / therapeutic use
Animals
Benzimidazoles / therapeutic use*
Benzoates / therapeutic use*
Dietary Fats / administration & dosage*
Dipeptidyl-Peptidase IV Inhibitors / therapeutic use
Drug Evaluation, Preclinical / methods
Drug Therapy, Combination
Energy Intake / drug effects
Glucose Tolerance Test
Hypoglycemic Agents / therapeutic use
Insulin Resistance
Liver / physiopathology,  ultrastructure
Male
Metabolic Syndrome X / drug therapy*,  pathology,  physiopathology
Metformin / therapeutic use*
Mice
Mice, Inbred C57BL
Obesity / drug therapy*,  pathology,  physiopathology
Pancreas / physiopathology
Pyrazines / therapeutic use*
Triazoles / therapeutic use*
Chemical
Reg. No./Substance:
0/Angiotensin II Type 1 Receptor Blockers; 0/Benzimidazoles; 0/Benzoates; 0/Dietary Fats; 0/Dipeptidyl-Peptidase IV Inhibitors; 0/Hypoglycemic Agents; 0/Pyrazines; 0/Triazoles; 0/sitagliptin; 144701-48-4/telmisartan; 657-24-9/Metformin

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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