Document Detail


Combination therapy with nateglinide and vildagliptin improves postprandial metabolic derangements in Zucker fatty rats.
MedLine Citation:
PMID:  20625970     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Postprandial metabolic derangements are one of the risk factors of cardiovascular disease in humans. Insulin resistance and/or impaired early-phase insulin secretion are major determinants of postprandial metabolic derangements. In this study, we investigated the potential utility of combination therapy with vildagliptin, a dipeptidyl peptidase IV (DPP-IV) inhibitor and nateglinide, a rapid-onset/short-duration insulinotropic agent, for the treatment of postprandial metabolic derangements in Zucker Fatty (ZF) rats, an animal model of obesity with insulin resistance. ZF rats fed twice daily with or without high fat diet (HFD) were given vehicle, 50 mg/kg of nateglinide, 10 mg/kg of vildagliptin, or both for 6 weeks. Combination therapy with nateglinide and vildagliptin for 2 weeks ameliorated postprandial hyperglycemia, hypertriglyceridemia, and elevation of free fatty acid in ZF rats fed with HFD. 6-week treatment with nateglinide and vildagliptin not only increased hepatic levels of phosphorylated forkhead box protein 1A (FOXO1A), but also reduced triglyceride contents in the liver. Combination therapy also prevented the loss of pancreatic islet mass in ZF rats fed with HFD. These observations demonstrate that combination therapy with nateglinide and vildagliptin may improve postprandial metabolic derangements probably by ameliorating early phase of insulin secretion and hepatic insulin resistance, respectively, in ZF rats fed with HFD. Since combination therapy with nateglinide and vildagliptin restored the decrease in pancreatic beta cell mass, our present findings suggest that combination therapy could be a promising therapeutic strategy for postprandial dysmetabolism associated with obese and insulin resistance.
Authors:
K Miura; Y Kitahara; S Yamagishi
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2010-07-12
Journal Detail:
Title:  Hormone and metabolic research = Hormon- und Stoffwechselforschung = Hormones et métabolisme     Volume:  42     ISSN:  1439-4286     ISO Abbreviation:  Horm. Metab. Res.     Publication Date:  2010 Sep 
Date Detail:
Created Date:  2010-09-03     Completed Date:  2010-12-15     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0177722     Medline TA:  Horm Metab Res     Country:  Germany    
Other Details:
Languages:  eng     Pagination:  731-5     Citation Subset:  IM    
Affiliation:
Pharmaceutical Research Laboratories, Ajinomoto, Kawasaki, Japan.
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MeSH Terms
Descriptor/Qualifier:
Adamantane / analogs & derivatives*,  pharmacology,  therapeutic use
Animals
Blood Glucose / drug effects,  metabolism
Cyclohexanes / pharmacology,  therapeutic use*
Drug Therapy, Combination
Fatty Acids / blood
Forkhead Transcription Factors / metabolism
Hypoglycemic Agents / pharmacology,  therapeutic use*
Insulin / blood
Insulin-Secreting Cells / drug effects,  metabolism,  pathology
Liver / drug effects,  metabolism,  pathology
Male
Metabolic Diseases / blood,  drug therapy*,  physiopathology*
Nitriles / pharmacology,  therapeutic use*
Organ Size / drug effects
Phenylalanine / analogs & derivatives*,  pharmacology,  therapeutic use
Phosphorylation / drug effects
Postprandial Period / drug effects,  physiology*
Pyrrolidines / pharmacology,  therapeutic use*
Rats
Rats, Zucker
Triglycerides / blood
Chemical
Reg. No./Substance:
0/Blood Glucose; 0/Cyclohexanes; 0/Fatty Acids; 0/Forkhead Transcription Factors; 0/Foxo1a protein, rat; 0/Hypoglycemic Agents; 0/Nitriles; 0/Pyrrolidines; 0/Triglycerides; 0/vildagliptin; 105816-04-4/nateglinide; 11061-68-0/Insulin; 281-23-2/Adamantane; 63-91-2/Phenylalanine

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


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