Effects of α7 nicotinic acetylcholine receptor agonist against α-synuclein-induced neurotoxicity

Neurosci Lett. 2024 Feb 16:823:137654. doi: 10.1016/j.neulet.2024.137654. Epub 2024 Jan 26.

Abstract

The α7 neuronal nicotinic acetylcholine receptor (α7 nAChR) is a potential target for the development of Parkinson's disease (PD) therapeutics. α-Synuclein (α-Syn), a principal component of Lewy bodies (cytoplasmic inclusions), is a major contributor to PD pathophysiology. Previous studies have demonstrated that activating α7 nAChR protects against nigrostriatal dopamine degeneration in acute and chronic PD animal models induced by 6-hydroxydopamine and rotenone, respectively. In the present study, we investigated the effects of PNU282987, a selective α7 nAChR agonist, against α-Syn-induced neurotoxicity in α-SynWT-, α-SynA30P-, and α-SynE46K-N2a cells. PNU282987 exhibited substantial neuroprotection against both wild-type and mutant-type α-Syn-induced toxicity. Furthermore, PNU282987 promoted transcription factor EB activity and reduced intracellular α-Syn protein levels through autophagy induction. These results highlight the therapeutic potential of α7 nAChR activation in diseases characterized by α-Syn aggregation, such as PD.

Keywords: Autophagy; Neuroprotection; α7 nicotinic acetylcholine receptor.

MeSH terms

  • Animals
  • Benzamides / pharmacology
  • Bridged Bicyclo Compounds*
  • Neurotoxicity Syndromes*
  • Nicotinic Agonists / toxicity
  • Parkinson Disease* / drug therapy
  • Parkinson Disease* / metabolism
  • Receptors, Nicotinic* / metabolism
  • alpha-Synuclein / metabolism
  • alpha7 Nicotinic Acetylcholine Receptor

Substances

  • alpha-Synuclein
  • PNU-282987
  • alpha7 Nicotinic Acetylcholine Receptor
  • Benzamides
  • Nicotinic Agonists
  • Receptors, Nicotinic
  • Bridged Bicyclo Compounds