JTT-130, a novel intestine-specific inhibitor of microsomal triglyceride transfer protein, suppresses high fat diet-induced obesity and glucose intolerance in Sprague-Dawley rats

Diabetes Obes Metab. 2011 May;13(5):446-54. doi: 10.1111/j.1463-1326.2011.01368.x. Epub 2011 Jan 21.

Abstract

Aim: Microsomal triglyceride transfer protein (MTP) takes part in the mobilization and secretion of triglyceride-rich lipoproteins from enterocytes and hepatocytes. We investigated the effects of JTT-130, a novel intestine-specific MTP inhibitor, on high fat diet-induced obesity and glucose intolerance.

Methods: Male Sprague-Dawley rats were fed a 3.1% fat diet or a 35% fat diet with or without JTT-130 as a food admixture (0.029%). Food intake, body weight, abdominal fat, hepatic triglyceride, faecal free fatty acids and plasma levels of glucagon-like peptide-1 (GLP-1) and peptide YY (PYY) were assessed. Plasma levels of glucose and insulin were measured during intraperitoneal glucose tolerance tests. In addition, indirect calorimetry was performed on rats fed with a 35% fat diet.

Results: JTT-130 treatment decreased body weights, abdominal fat and hepatic triglyceride with suppression of food intake and elevation of faecal free fatty acids and plasma GLP-1 and PYY levels in rats fed with the 35% fat diet, whereas no significant effects on these parameters except for increased faecal free fatty acids were observed in rats fed with the 3.1% fat diet. JTT-130 treatment decreased plasma levels of glucose and insulin during intraperitoneal glucose tolerance tests on rats fed with the 35% fat diet, but not on rats fed with the 3.1% fat diet. JTT-130-treated rats showed increased O(2) consumption and CO(2) production on a 35% fat diet.

Conclusions: JTT-130 suppresses high fat diet-induced obesity and glucose intolerance with suppression of food intake and fat absorption and could be useful for prevention and treatment of obesity and obesity-related insulin resistance.

MeSH terms

  • Animals
  • Benzamides / pharmacology*
  • Biomarkers / blood
  • Blood Glucose / metabolism
  • Carrier Proteins / drug effects*
  • Diet, High-Fat / adverse effects*
  • Dietary Fats / adverse effects
  • Eating / drug effects
  • Fatty Acids / metabolism
  • Feces / chemistry
  • Glucagon-Like Peptide 1 / blood
  • Glucose Intolerance / drug therapy*
  • Glucose Intolerance / prevention & control
  • Glucose Tolerance Test
  • Hypoglycemic Agents / pharmacology*
  • Insulin / blood
  • Insulin Resistance
  • Liver / metabolism
  • Male
  • Malonates / pharmacology*
  • Obesity / chemically induced
  • Obesity / drug therapy*
  • Obesity / prevention & control
  • Peptide YY / blood
  • Rats
  • Rats, Sprague-Dawley
  • Triglycerides / metabolism

Substances

  • Benzamides
  • Biomarkers
  • Blood Glucose
  • Carrier Proteins
  • Dietary Fats
  • Fatty Acids
  • Hypoglycemic Agents
  • Insulin
  • Malonates
  • Triglycerides
  • diethyl 2-((3-dimethylcarbamoyl-4-((4'-trifluoromethylbiphenyl-2-carbonyl)amino)phenyl)acetyloxymethyl)-2-phenylmalonate
  • microsomal triglyceride transfer protein
  • Peptide YY
  • Glucagon-Like Peptide 1