The phospholipase A(2) inhibitor methyl indoxam suppresses diet-induced obesity and glucose intolerance in mice

Br J Pharmacol. 2009 Aug;157(7):1263-9. doi: 10.1111/j.1476-5381.2009.00308.x. Epub 2009 Jun 25.

Abstract

Background and purpose: Previous results have shown that mice lacking in the group 1B phospholipase A(2) (Pla2g1b) are resistant to obesity and diabetes induced by feeding a diabetogenic high-fat/high-carbohydrate diet. This study examined the potential of using the Pla2g1b inhibitor methyl indoxam as therapy to suppress diet-induced obesity and diabetes.

Experimental approach: Male C57BL/6 mice were fed the diabetogenic diet with or without methyl indoxam supplementation. Body weight gain, fasting plasma glucose levels, glucose tolerance and postprandial lysophospholipid absorption were compared.

Key results: Wild-type C57BL/6 mice fed the diabetogenic diet without Pla2g1b inhibitor showed 31 and 69% body weight gain after 4 and 10 weeks respectively. These animals also showed elevated plasma glucose levels and were glucose intolerant. In contrast, C57BL/6 mice fed the diabetogenic diet with 90 mg.kg(-1) of methyl indoxam gained only 5% body weight after 10 weeks. These animals were also euglycaemic and displayed normal glucose excursion rates in glucose tolerance test. Methyl indoxam suppression of diet-induced body weight gain and glucose intolerance was correlated with the inhibition of Pla2g1b-mediated postprandial lysophospholipid absorption.

Conclusions and implications: These results show that oral supplementation of a diabetogenic diet with the Pla2g1b inhibitor methyl indoxam effectively suppresses diet-induced obesity and diabetes in mice. This suggests that Pla2g1b inhibition may be a potentially effective oral therapeutic option for treatment of obesity and diabetes.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Obesity Agents / pharmacokinetics
  • Anti-Obesity Agents / therapeutic use*
  • Bile / drug effects
  • Bile / enzymology
  • Biphenyl Compounds / pharmacology*
  • Caco-2 Cells
  • Dietary Carbohydrates / administration & dosage
  • Dietary Fats / administration & dosage
  • Eating / drug effects
  • Glucose Intolerance / blood
  • Glucose Intolerance / drug therapy*
  • Glucose Intolerance / etiology
  • Group IB Phospholipases A2 / antagonists & inhibitors*
  • Group IB Phospholipases A2 / genetics
  • Group IB Phospholipases A2 / metabolism
  • Humans
  • Hydrolysis
  • Hypoglycemic Agents / pharmacokinetics
  • Hypoglycemic Agents / therapeutic use*
  • Indoles / pharmacology*
  • Lysophospholipids / blood
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Mice, Knockout
  • Obesity / blood
  • Obesity / drug therapy*
  • Obesity / etiology
  • Postprandial Period
  • Recombinant Proteins / antagonists & inhibitors
  • Recombinant Proteins / metabolism
  • Weight Gain / drug effects

Substances

  • Anti-Obesity Agents
  • Biphenyl Compounds
  • Dietary Carbohydrates
  • Dietary Fats
  • Hypoglycemic Agents
  • Indoles
  • Lysophospholipids
  • Recombinant Proteins
  • methyl indoxam
  • Group IB Phospholipases A2