Potent anti-amyloidogenic and fibril-destabilizing effects of polyphenols in vitro: implications for the prevention and therapeutics of Alzheimer's disease

J Neurochem. 2003 Oct;87(1):172-81. doi: 10.1046/j.1471-4159.2003.01976.x.

Abstract

Cerebral deposition of amyloid beta-peptide (Abeta) in the brain is an invariant feature of Alzheimer's disease (AD). A consistent protective effect of wine consumption on AD has been documented by epidemiological studies. In the present study, we used fluorescence spectroscopy with thioflavin T and electron microscopy to examine the effects of wine-related polyphenols (myricetin, morin, quercetin, kaempferol (+)-catechin and (-)-epicatechin) on the formation, extension, and destabilization of beta-amyloid fibrils (fAbeta) at pH 7.5 at 37 degrees C in vitro. All examined polyphenols dose-dependently inhibited formation of fAbeta from fresh Abeta(1-40) and Abeta(1-42), as well as their extension. Moreover, these polyphenols dose-dependently destabilized preformed fAbetas. The overall activity of the molecules examined was in the order of: myricetin = morin = quercetin > kaempferol > (+)-catechin = (-)-epicatechin. The effective concentrations (EC50) of myricetin, morin and quercetin for the formation, extension and destabilization of fAbetas were in the order of 0.1-1 micro m. In cell culture experiments, myricetin-treated fAbeta were suggested to be less toxic than intact fAbeta, as demonstrated by 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide assay. Although the mechanisms by which these polyphenols inhibit fAbeta formation from Abeta, and destabilize pre-formed fAbetain vitro are still unclear, polyphenols could be a key molecule for the development of preventives and therapeutics for AD.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alzheimer Disease* / drug therapy
  • Alzheimer Disease* / prevention & control
  • Amyloid beta-Peptides / chemistry*
  • Amyloid beta-Peptides / drug effects
  • Benzothiazoles
  • Cell Line
  • Cell Survival / drug effects
  • Dose-Response Relationship, Drug
  • Flavonoids / chemistry
  • Flavonoids / pharmacology
  • Humans
  • Kidney / cytology
  • Kidney / drug effects
  • Kidney / metabolism
  • Kinetics
  • Microscopy, Electron
  • Peptide Fragments / chemistry
  • Phenols / chemistry*
  • Phenols / pharmacology*
  • Polymers / chemistry*
  • Polymers / pharmacology*
  • Quercetin / chemistry
  • Quercetin / pharmacology
  • Spectrometry, Fluorescence
  • Tetrazolium Salts
  • Thiazoles / chemistry

Substances

  • Amyloid beta-Peptides
  • Benzothiazoles
  • Flavonoids
  • Peptide Fragments
  • Phenols
  • Polymers
  • Tetrazolium Salts
  • Thiazoles
  • amyloid beta-protein (1-40)
  • amyloid beta-protein (1-42)
  • thioflavin T
  • myricetin
  • morin
  • Quercetin
  • thiazolyl blue