Synthesis, characterization and biological evaluation of aurones as potential neuroprotective agents

Future Med Chem. 2024 Aug 17;16(16):1649-1663. doi: 10.1080/17568919.2024.2363713. Epub 2024 Jun 28.

Abstract

Aim: To synthesize aurone (Ar) derivatives and to demonstrate their effects against diabetes mellitus (DM) and neurodegeneration.Materials & methods: Five Ar (A-E) derivatives were synthesized, characterized by proton NMR and screened for antioxidant, anti-diabetic and anti-cholinesterase activities. They were further evaluated for neuroprotective effects in streptozotocin (STZ)-induced neurodegenerative model.Results: Among the aurone derivatives ArE demonstrated significant reversal of cognitive impairment, oxidative stress and neuroinflammation. Biochemical analysis revealed anti-diabetic and neuroprotective effects, possibly through downregulation of inflammatory markers and upregulation of antioxidant enzymes.Conclusion: Synthesized Ar (A-E) exhibits promising therapeutic potential against STZ-induced neurodegeneration and DM by modulating inflammatory and oxidative pathways, suggesting a novel avenue for disease management.

Keywords: aurones; diabetes mellitus; neurodegeneration; neuroinflammation; oxidative stress; streptozotocin.

Plain language summary

[Box: see text].

MeSH terms

  • Animals
  • Antioxidants / chemical synthesis
  • Antioxidants / chemistry
  • Antioxidants / pharmacology
  • Benzofurans* / chemical synthesis
  • Benzofurans* / chemistry
  • Benzofurans* / pharmacology
  • Cholinesterase Inhibitors / chemical synthesis
  • Cholinesterase Inhibitors / chemistry
  • Cholinesterase Inhibitors / pharmacology
  • Diabetes Mellitus, Experimental / chemically induced
  • Diabetes Mellitus, Experimental / drug therapy
  • Hypoglycemic Agents / chemical synthesis
  • Hypoglycemic Agents / chemistry
  • Hypoglycemic Agents / pharmacology
  • Male
  • Molecular Structure
  • Neuroprotective Agents* / chemical synthesis
  • Neuroprotective Agents* / chemistry
  • Neuroprotective Agents* / pharmacology
  • Oxidative Stress / drug effects
  • Rats
  • Streptozocin
  • Structure-Activity Relationship

Substances

  • Neuroprotective Agents
  • aurone
  • Benzofurans
  • Antioxidants
  • Streptozocin
  • Hypoglycemic Agents
  • Cholinesterase Inhibitors