Effect of donepezil hydrochloride on the transgenic Drosophila expressing human Aβ-42

Int J Neurosci. 2024 Nov;134(11):1293-1308. doi: 10.1080/00207454.2023.2262109. Epub 2023 Nov 21.

Abstract

Aim: In the present study, the effect of donepezil hydrochloride was studied on the transgenic Drosophila expressing human amyloid beta-42 in the neurons.

Methods: Donepezil hydrochloride at final concentration of 0.1, 1 and 10 mM was mixed in the diet and the flies expressing human amyloid beta-42 under Upstream Activation Sequence control (Alzheimer Disease [AD] flies) were allowed to feed on it for 30 days.

Results: The AD flies exposed to various doses of Donepezil hydrochloride showed a dose dependent significant delay in the loss of climbing ability, increase in activity, reduction in the oxidative stress and apoptotic markers. A significant improvement was also observed in cognitive parameters. A dose dependent significant reduction in the activity of acetylcholinesterase was also observed. The docking studies suggest the positive interaction between donepezil, amyloid beta-42 and acetylcholinesterase. The results obtained from immunohistochemistry also showed a dose dependent significant reduction in the amyloid beta-42 aggregates.

Conclusion: The results suggest that donepezil hydrochloride is potent enough to reduce the AD symptoms being mimicked in transgenic flies.

Keywords: Alzheimer disease; Donepezil hydrochloride; Drosophila; molecular docking; oxidative stress.

MeSH terms

  • Acetylcholinesterase* / metabolism
  • Alzheimer Disease / drug therapy
  • Alzheimer Disease / metabolism
  • Amyloid beta-Peptides* / metabolism
  • Animals
  • Animals, Genetically Modified*
  • Cholinesterase Inhibitors / administration & dosage
  • Cholinesterase Inhibitors / pharmacology
  • Disease Models, Animal
  • Donepezil* / pharmacology
  • Dose-Response Relationship, Drug
  • Drosophila / drug effects
  • Humans
  • Indans* / administration & dosage
  • Indans* / pharmacology
  • Oxidative Stress / drug effects
  • Peptide Fragments* / metabolism
  • Peptide Fragments* / pharmacology
  • Piperidines* / administration & dosage
  • Piperidines* / pharmacology

Substances

  • Donepezil
  • Amyloid beta-Peptides
  • Indans
  • Piperidines
  • Peptide Fragments
  • amyloid beta-protein (1-42)
  • Acetylcholinesterase
  • Cholinesterase Inhibitors