Inhibition of histone deacetylase 3 protects beta cells from cytokine-induced apoptosis

Chem Biol. 2012 Jun 22;19(6):669-73. doi: 10.1016/j.chembiol.2012.05.010.

Abstract

Cytokine-induced beta-cell apoptosis is important to the etiology of type-1 diabetes. Although previous reports have shown that general inhibitors of histone deacetylase (HDAC) activity, such as suberoylanilide hydroxamic acid and trichostatin A, can partially prevent beta-cell death, they do not fully restore beta-cell function. To understand HDAC isoform selectivity in beta cells, we measured the cellular effects of 11 structurally diverse HDAC inhibitors on cytokine-induced apoptosis in the rat INS-1E cell line. All 11 compounds restored ATP levels and reduced nitrite secretion. However, caspase-3 activity was reduced only by MS-275 and CI-994, both of which target HDAC1, 2, and 3. Importantly, both MS-275 and genetic knockdown of Hdac3 alone were sufficient to restore glucose-stimulated insulin secretion in the presence of cytokines. These results suggest that HDAC3-selective inhibitors may be effective in preventing cytokine-induced beta-cell apoptosis.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Apoptosis / drug effects*
  • Benzamides / pharmacology*
  • Cytokines / metabolism*
  • Dose-Response Relationship, Drug
  • Glucose / pharmacology
  • Histone Deacetylase Inhibitors / pharmacology*
  • Histone Deacetylases / metabolism*
  • Insulin / metabolism
  • Insulin Secretion
  • Insulin-Secreting Cells / cytology*
  • Insulin-Secreting Cells / drug effects*
  • Insulin-Secreting Cells / enzymology
  • Insulin-Secreting Cells / metabolism
  • Phenylenediamines / pharmacology*
  • Pyridines / pharmacology*
  • Rats
  • Structure-Activity Relationship
  • Tumor Cells, Cultured

Substances

  • Benzamides
  • Cytokines
  • Histone Deacetylase Inhibitors
  • Insulin
  • Phenylenediamines
  • Pyridines
  • entinostat
  • Histone Deacetylases
  • histone deacetylase 3
  • Glucose
  • tacedinaline