Synergic Therapeutic Potential of PEA-Um Treatment and NAAA Enzyme Silencing In the Management of Neuroinflammation

Int J Mol Sci. 2020 Oct 11;21(20):7486. doi: 10.3390/ijms21207486.

Abstract

Inflammation is a key element in the pathobiology of neurodegenerative diseases and sees the involvement of different neuronal and non-neuronal cells as players able to respond to inflammatory signals of immune origin. Palmitoylethanolamide (PEA) is an endogenous potent anti-inflammatory agent, in which activity is regulated by N-acylethanolamine acid amidase (NAAA), that hydrolyzes saturated or monounsaturated fatty acid ethanolamides, such as PEA. In this research, an in vitro study was performed on different neuronal (SH-SY5Y) and non-neuronal cell lines (C6, BV-2, and Mo3.13) subjected to NAAA enzyme silencing and treated with PEA ultra-micronized (PEA-um) (1, 3, and 10 μM) to increase the amount of endogenous PEA available for counteract neuroinflammation provoked by stimulation with lipopolysaccharide (LPS) (1 μg/mL) and interferon gamma (INF-γ )(100 U/mL). Cell viability was performed by MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide) staining, suggesting a protective effect of PEA-um (3 and 10 μM) on all cell lines studied. Western Blot analysis for inflammatory markers (Inducible nitric oxide synthase (iNOS) and cyclooxygenase 2 (COX-2)) was carried out in control and NAAA-silenced cells, highlighting how the concomitant treatment of the neuronal and non-neuronal cells with PEA-um after NAAA genic downregulation is satisfactory to counteract neuroinflammation. These in vitro findings support the protective role of endogenous PEA availability in the neuronal field, bringing interesting information for a translational point of view.

Keywords: glioma; microglia; neuroblastoma; neuroinflammation; oligodendrocytes; palmitoylethanolamide.

MeSH terms

  • Amides / pharmacology*
  • Amidohydrolases / antagonists & inhibitors*
  • Amidohydrolases / metabolism*
  • Animals
  • Biomarkers
  • Cell Line
  • Cell Survival / drug effects
  • Disease Management
  • Disease Susceptibility
  • Drug Synergism
  • Enzyme Activation / drug effects
  • Ethanolamines / pharmacology*
  • Humans
  • Inflammation / drug therapy
  • Inflammation / etiology
  • Inflammation / metabolism
  • Mice
  • Neurons / drug effects
  • Neurons / metabolism
  • Neuroprotective Agents / pharmacology*
  • Palmitic Acids / pharmacology*
  • Rats

Substances

  • Amides
  • Biomarkers
  • Ethanolamines
  • Neuroprotective Agents
  • Palmitic Acids
  • palmidrol
  • Amidohydrolases
  • NAAA protein, human