2-Pentadecyl-2-Oxazoline Reduces Neuroinflammatory Environment in the MPTP Model of Parkinson Disease

Mol Neurobiol. 2018 Dec;55(12):9251-9266. doi: 10.1007/s12035-018-1064-2. Epub 2018 Apr 14.

Abstract

Current pharmacological management of Parkinson disease (PD) does not provide for disease modification, but addresses only symptomatic features. Here, we explore a new approach to neuroprotection based on the use of 2-pentadecyl-2-oxazoline (PEA-OXA), the oxazoline derivative of the fatty acid amide signaling molecule palmitoylethanolamide (PEA), in an experimental model of PD. Daily oral treatment with PEA-OXA (10 mg/kg) significantly reduced behavioral impairments and neuronal cell degeneration of the dopaminergic tract induced by four intraperitoneal injections of the dopaminergic neurotoxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) on 8-week-old male C57 mice. Moreover, PEA-OXA treatment prevented dopamine depletion, increased tyrosine hydroxylase and dopamine transporter activities, and decreased α-synuclein aggregation in neurons. PEA-OXA treatment also diminished nuclear factor-κB traslocation, cyclooxygenase-2, and inducible nitric oxide synthase expression and through upregulation of the nuclear factor E2-related factor 2 pathway, induced activation of Mn-superoxide dismutase and heme oxygenase-1. Further, PEA-OXA modulated microglia and astrocyte activation and preserved microtubule-associated protein-2 alterations. In conclusion, pharmacological activation of nuclear factor E2-related factor 2 pathways with PEA-OXA may be effective in the future therapy of PD.

Keywords: 2-Pentadecyl-2-oxazoline; Inflammation; Nrf-2; Parkinson disease.

MeSH terms

  • 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine
  • Animals
  • Astrocytes / drug effects
  • Astrocytes / metabolism
  • Behavior, Animal
  • Cyclooxygenase 2 / metabolism
  • Cytokines / metabolism
  • DNA Damage
  • Disease Models, Animal
  • Dopamine Plasma Membrane Transport Proteins / metabolism
  • Inflammation / drug therapy*
  • Inflammation / pathology*
  • Mice, Inbred C57BL
  • Microglia / drug effects
  • Microglia / metabolism
  • NF-E2-Related Factor 2 / metabolism
  • Nitric Oxide Synthase Type II / metabolism
  • Nitrosative Stress / drug effects
  • Oxazoles / pharmacology
  • Oxazoles / therapeutic use*
  • Oxidative Stress / drug effects
  • Parkinson Disease / drug therapy*
  • Parkinson Disease / pathology*
  • Poly Adenosine Diphosphate Ribose / metabolism
  • Transcription Factor RelA / metabolism
  • Tyrosine / analogs & derivatives
  • Tyrosine / metabolism
  • Tyrosine 3-Monooxygenase / metabolism
  • alpha-Synuclein / metabolism

Substances

  • 2-pentadecyl-2-oxazoline
  • Cytokines
  • Dopamine Plasma Membrane Transport Proteins
  • NF-E2-Related Factor 2
  • Oxazoles
  • Transcription Factor RelA
  • alpha-Synuclein
  • Poly Adenosine Diphosphate Ribose
  • 3-nitrotyrosine
  • Tyrosine
  • 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine
  • Nitric Oxide Synthase Type II
  • Tyrosine 3-Monooxygenase
  • Cyclooxygenase 2