Palonosetron/Methyllycaconitine Deactivate Hippocampal Microglia 1, Inflammasome Assembly and Pyroptosis to Enhance Cognition in a Novel Model of Neuroinflammation

Molecules. 2021 Aug 21;26(16):5068. doi: 10.3390/molecules26165068.

Abstract

Since westernized diet-induced insulin resistance is a risk factor in Alzheimer's disease (AD) development, and lipopolysaccharide (LPS) coexists with amyloid β (Aβ)1-42 in these patients, our AD novel model was developed to resemble sporadic AD by injecting LPS into high fat/fructose diet (HFFD)-fed rats. The neuroprotective potential of palonosetron and/or methyllycaconitine, 5-HT3 receptor and α7 nAChR blockers, respectively, was evaluated after 8 days of daily administration in HFFD/LPS rats. All regimens improved histopathological findings and enhanced spatial memory (Morris Water Maze); however, palonosetron alone or with methyllycaconitine promoted animal performance during novel object recognition tests. In the hippocampus, all regimens reduced the expression of glial fibrillary acidic protein and skewed microglia M1 to M2 phenotype, indicated by the decreased M1 markers and the enhanced M2 related parameters. Additionally, palonosetron and its combination regimen downregulated the expression of ASC/TMS1, as well as levels of inflammasome downstream molecules and abated cleaved caspase-1, interleukin (IL)-1β, IL-18 and caspase-11. Furthermore, ACh and 5-HT were augmented after being hampered by the insult. Our study speculates that blocking 5-HT3 receptor using palonosetron overrides methyllycaconitine to combat AD-induced neuroinflammation and inflammasome cascade, as well as to restore microglial function in a HFFD/LPS novel model for sporadic AD.

Keywords: 5-HT3 receptor blocker; caspase-1/IL-1β/IL-18; inflammasome; microglia; pyroptosis; α7AChR.

MeSH terms

  • Aconitine / analogs & derivatives*
  • Aconitine / pharmacology
  • Alzheimer Disease / drug therapy*
  • Alzheimer Disease / etiology
  • Alzheimer Disease / genetics
  • Alzheimer Disease / pathology
  • Amyloid beta-Peptides / genetics
  • Animals
  • CARD Signaling Adaptor Proteins / genetics
  • Cognition / drug effects
  • Diet, Western / adverse effects
  • Disease Models, Animal
  • Hippocampus / drug effects
  • Hippocampus / pathology
  • Humans
  • Inflammasomes / drug effects
  • Inflammasomes / metabolism
  • Inflammation / drug therapy*
  • Inflammation / genetics
  • Inflammation / pathology
  • Insulin Resistance / genetics
  • Interleukin-18 / genetics
  • Lipopolysaccharides / pharmacology
  • Microglia / drug effects
  • Microglia / pathology
  • Palonosetron / pharmacology*
  • Peptide Fragments / genetics
  • Pyroptosis / drug effects
  • Rats
  • Receptors, Serotonin, 5-HT3 / genetics
  • Risk Factors
  • Spatial Memory / drug effects

Substances

  • Amyloid beta-Peptides
  • CARD Signaling Adaptor Proteins
  • Inflammasomes
  • Interleukin-18
  • Lipopolysaccharides
  • PYCARD protein, human
  • Peptide Fragments
  • Pycard protein, rat
  • Receptors, Serotonin, 5-HT3
  • amyloid beta-protein (1-40)
  • methyllycaconitine
  • Palonosetron
  • Aconitine