To estimate effective antiamyloidogenic property of melatonin and fisetin and their actions to destabilize amyloid fibrils

Pak J Pharm Sci. 2017 Sep;30(5):1589-1593.

Abstract

Aggregating of amylin as pancreatic deposition is connected with pancreas degeneration in type 2 diabetes mellitus. Suppression of the amylin accumulation and so instability of the pre-formed pancreatic β-amyloid, may be attractive curative goal for mediation of diabetes mellitus. Fluorimetric assay by Thioflavin-T was utilized for investigating the properties of melatonin and fisetin on the generation and instability of β-amyloid near to physiological conditions. The results showed that after 168 hours incubation by shaker incubator in 37oC, melatonin at 10μM and 40 µM repressed amylin amyloid formation by 20.1% and 27.5% respectively (p<0.05) and the similar values of fisetin inhibited the formation of β-sheet structure by 16.5% and 23.2% respectively (p<0.05).The obtained data also confirmed that amyloidal sheet opening was induced by melatonin and fisetin significantly (p<0.05). It may be concluded that islet amyloid cytotoxicity to β-cells may be reduced by melatonin and fisetin, and they should be important constituents of new drugs for diabetes mellitus treatment.

MeSH terms

  • Amyloid / drug effects*
  • Amyloid / metabolism
  • Amyloid beta-Peptides / drug effects*
  • Amyloid beta-Peptides / metabolism
  • Flavonoids / pharmacology*
  • Flavonols
  • Melatonin / pharmacology*
  • Plaque, Amyloid*
  • Protein Conformation
  • Protein Unfolding
  • Structure-Activity Relationship

Substances

  • Amyloid
  • Amyloid beta-Peptides
  • Flavonoids
  • Flavonols
  • Melatonin
  • fisetin