Roles of inhibitors of poly(ADP-ribose) polymerase in protecting rat RINm5F cell line against free fatty acid-induced apoptosis

Exp Clin Endocrinol Diabetes. 2009 Jun;117(6):274-82. doi: 10.1055/s-0029-1202794. Epub 2009 Jun 9.

Abstract

Background: Chronic exposure to high levels of free fatty acid (FFA) has adverse effects on the function of pancreatic beta-cell, with a consequent increase in the production of reactive oxygen species. Poly (ADP-Ribose) polymerase (PARP-1) overactivation leads to massive NAD(+) consumption and ATP depletion with induction of cellular necrosis under high reactive oxygen species. In the present study, we investigated whether inhibitors of poly(ADP-ribose) polymerase were capable of protecting beta-cells from death induced by extended exposure to FFA.

Materials and methods: RINm5F cell line was cultured in the presence of FFA (palmitate) in order to induce apoptosis, and then cells were treated with low-potency poly(ADP-ribose) polymerase inhibitor (3-aminobenzamide) or potent poly(ADP-ribose) polymerase inhibitor (PJ34). In order to explore whether poly(ADP-ribose) polymerase inhibitors could inhibit the apoptosis induced by FFA, expression of PARP-1 was measured by RT-qPCR and Western blot, while the apoptosis of RINm5F cells were analyzed by flow cytometry and Tdt-mediated dUTP Nick-End Labeling(TUNEL).

Results: Low-potency poly(ADP-ribose) polymerase inhibitor (3-aminobenzamide) significantly suppressed the impaired insulin secretion and FFA-induced apoptosis (P<0.01). However, potent poly(ADP-ribose) polymerase inhibitor (PJ34) had no significant effects on FFA-induced apoptosis (P>0.05). Moreover, low-potency inhibitors of PARP-1 increased PDX-1 expression down-regulated by FFA-treatment.

Conclusions: These findings suggested that low-potency inhibitors of poly(ADP-ribose) polymerases could protect rat RINm5F cell line against free fatty acid-induced apoptosis, and it was through regulatory pathway of regulating PDX-1 expression.

MeSH terms

  • Animals
  • Apoptosis / drug effects*
  • Benzamides / pharmacology*
  • Cell Line
  • Down-Regulation / drug effects
  • Enzyme Inhibitors / pharmacology*
  • Fatty Acids, Nonesterified / pharmacology*
  • Homeodomain Proteins / biosynthesis
  • Insulin / metabolism
  • Insulin Secretion
  • Insulin-Secreting Cells / enzymology*
  • Phenanthrenes / pharmacology*
  • Poly (ADP-Ribose) Polymerase-1
  • Poly(ADP-ribose) Polymerase Inhibitors
  • Poly(ADP-ribose) Polymerases / biosynthesis*
  • Rats
  • Trans-Activators / biosynthesis

Substances

  • Benzamides
  • Enzyme Inhibitors
  • Fatty Acids, Nonesterified
  • Homeodomain Proteins
  • Insulin
  • N-(oxo-5,6-dihydrophenanthridin-2-yl)-N,N-dimethylacetamide hydrochloride
  • Phenanthrenes
  • Poly(ADP-ribose) Polymerase Inhibitors
  • Trans-Activators
  • pancreatic and duodenal homeobox 1 protein
  • 3-aminobenzamide
  • Parp1 protein, rat
  • Poly (ADP-Ribose) Polymerase-1
  • Poly(ADP-ribose) Polymerases