Harmine prevents 3-nitropropionic acid-induced neurotoxicity in rats via enhancing NRF2-mediated signaling: Involvement of p21 and AMPK

Eur J Pharmacol. 2022 Jul 15:927:175046. doi: 10.1016/j.ejphar.2022.175046. Epub 2022 May 25.

Abstract

Oxidative stress induced neurotoxicity is increasingly perceived as an important neuropathologic mechanism underlying the motor and behavioral phenotypes associated with Huntington's disease (HD). Repeated exposure to 3-nitropropionic acid (3-NP) induces neurotoxic changes which closely simulate the neuropathological and behavioral characteristics of HD. This study aimed at evaluating the prophylactic effects of the dual-specificity tyrosine phosphorylation regulated kinase 1A (DYRK1A) inhibitor "harmine" against 3-NP-indued neurotoxicity and HD-like symptoms. The potential prophylactic effect of harmine (10 mg/kg/day; intraperitoneal) was investigated on 3-NP-induced motor and cognitive HD-like deficits, nuclear factor erythroid 2 like 2 (NRF2), AMP kinase (AMPK) and p21 protein levels and the gene expression of haem oxygenase-1 (Ho-1), NAD(P)H: quinone oxidoreductase-1 (Nqo-1) and p62 in addition to redox imbalance and histological neurotoxic changes in the striatum, prefrontal cortex, and hippocampus of male Wistar rats. Harmine successfully increased the protein levels of NRF2, AMPK and p21 and the gene expression of Ho-1, Nqo-1 and p62, restored redox homeostasis, and reduced CASPASE-3 level. This was reflected in attenuation of 3-NP-induced neurodegenerative changes and improvement of rats' motor and cognitive performance. This study draws attention to the protective role of harmine against 3-NP-induced motor and cognitive dysfunction that could be mediated via enhancing NRF2-mediated signaling with subsequent amelioration of oxidative stress injury via NRF2 activators, p21 and AMPK, in the striatum, prefrontal cortex, and hippocampus which could offer a promising therapeutic tool to slow the progression of HD.

Keywords: 3-Nitropropionic acid; AMPK; Harmine; Huntington's disease; NRF2; Neurotoxicity.

MeSH terms

  • AMP-Activated Protein Kinases* / metabolism
  • Adenylate Kinase / metabolism
  • Animals
  • Cyclin-Dependent Kinase Inhibitor p21* / metabolism
  • Harmine* / pharmacology
  • Huntington Disease* / chemically induced
  • Huntington Disease* / metabolism
  • Huntington Disease* / prevention & control
  • Male
  • NF-E2-Related Factor 2 / metabolism
  • Neuroprotective Agents* / adverse effects
  • Neurotoxicity Syndromes* / drug therapy
  • Neurotoxicity Syndromes* / etiology
  • Neurotoxicity Syndromes* / prevention & control
  • Nitro Compounds / antagonists & inhibitors
  • Nitro Compounds / pharmacology
  • Oxidative Stress
  • Propionates / antagonists & inhibitors
  • Propionates / pharmacology
  • Rats
  • Rats, Wistar
  • Signal Transduction / drug effects

Substances

  • Cyclin-Dependent Kinase Inhibitor p21
  • NF-E2-Related Factor 2
  • Neuroprotective Agents
  • Nfe2l2 protein, rat
  • Nitro Compounds
  • Propionates
  • Harmine
  • AMP-Activated Protein Kinases
  • Adenylate Kinase
  • 3-nitropropionic acid