Neuroprotective effects of diarylpropionitrile against β-amyloid peptide-induced neurotoxicity in rat cultured cortical neurons

Neurosci Lett. 2014 Aug 22:578:44-9. doi: 10.1016/j.neulet.2014.06.029. Epub 2014 Jun 21.

Abstract

Alzheimer's disease is a major cause of dementia in the elderly that involves a β-amyloid peptide (Aβ)-induced cascade of an increase in oxidative damage and inflammation. The present study demonstrated the neuroprotective effects of diarylpropionitrile (DPN), a non-steroidal estrogen receptor β selective ligand, against 10 μM Aβ1-42-induced oxidative stress and inflammation in primary rat cortical cell culture. Pre-treatment with 1-100 nM DPN significantly decreased neuronal cell death by increasing cell viability through a significant attenuation in the reactive oxygen species level, downregulation of pro-apoptotic activated caspase-3 and Bax, and upregulation of anti-apoptotic Bcl-2, thereby mitigating apoptotic morphological alterations. DPN pre-treatment decreased the expression levels of pro-inflammatory cytokines IL-1β and IL-6 through attenuation of Aβ1-42-induced phosphorylation of mitogen-activated protein kinases JNK and p38. In addition, DPN enhanced ERK1/2 and Akt phosphorylation depressed by Aβ1-42. These findings suggest that DPN protects neurons from Aβ1-42-induced neurotoxicity through a variety of mechanisms, ranging from anti-oxidation, anti-apoptosis, through to anti-inflammation.

Keywords: Alzheimer's disease; Anti-inflammation; Antioxidant; Apoptosis; Diarylpropionitrile; β-Amyloid peptide.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amyloid beta-Peptides / toxicity*
  • Animals
  • Apoptosis / drug effects*
  • Cell Survival
  • Cerebral Cortex / drug effects*
  • Estrogen Receptor beta / agonists
  • Inflammation
  • Neurons / drug effects*
  • Neuroprotective Agents / pharmacology*
  • Nitriles / pharmacology*
  • Oxidative Stress / drug effects
  • Peptide Fragments / toxicity*
  • Primary Cell Culture
  • Propionates / pharmacology*
  • Rats
  • Rats, Wistar

Substances

  • 2,3-bis(4-hydroxyphenyl)-propionitrile
  • Amyloid beta-Peptides
  • Estrogen Receptor beta
  • Neuroprotective Agents
  • Nitriles
  • Peptide Fragments
  • Propionates
  • amyloid beta-protein (1-42)