Effects of DHMEQ, a novel nuclear factor-kappab inhibitor, on beta cell dysfunction in INS-1 cells

Endocr J. 2008 May;55(2):433-8. doi: 10.1507/endocrj.k07e-036. Epub 2008 Apr 2.

Abstract

Aims: Recent studies suggest that nuclear factor-kappaB (NF-kappaB) activation has an important role in leading to beta cell dysfunction in both type 1 and type 2 diabetes. In this study we tested this hypothesis by investigating the effects of dehydroxymethylepoxyquinomicin (DHMEQ), a novel NF-kappaB inhibitor, on tumor necrosis factor-alpha (TNF-alpha)-induced beta cell dysfunction.

Methods: INS-1 cells were incubated with TNF- alpha and with or without DHMEQ for 24 hours. Glucose-stimulated insulin secretion, cell viability, mRNA expression and NF-kappaB activation were investigated.

Results: DHMEQ suppressed TNF-alpha-induced NF-kappaB activation and partially ameliorated glucose-stimulated insulin secretion in a dose-dependent manner. DHMEQ also partially ameliorated decreased cell viability and insulin mRNA level induced by TNF-alpha.

Conclusion: DHMEQ suppressed NF-kappaB activation and ameliorated beta cell dysfunction induced by TNF- alpha. Inhibition of activated NF-kappaB in beta cells may be important to ameliorate beta cell dysfunction in diabetes.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Benzamides / pharmacology*
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Cell Survival / physiology
  • Cyclohexanones / pharmacology*
  • Dose-Response Relationship, Drug
  • Glucose / pharmacology
  • Insulin / metabolism
  • Insulin-Secreting Cells / drug effects*
  • Insulin-Secreting Cells / pathology
  • Insulin-Secreting Cells / physiology*
  • Insulinoma / pathology
  • Insulinoma / physiopathology*
  • NF-kappa B / antagonists & inhibitors*
  • NF-kappa B / metabolism
  • Pancreatic Neoplasms / pathology
  • Pancreatic Neoplasms / physiopathology*
  • Rats
  • Tumor Necrosis Factor-alpha / pharmacology

Substances

  • Benzamides
  • Cyclohexanones
  • Insulin
  • NF-kappa B
  • Tumor Necrosis Factor-alpha
  • dehydroxymethylepoxyquinomicin
  • Glucose