Edaravone alleviates Alzheimer's disease-type pathologies and cognitive deficits

Proc Natl Acad Sci U S A. 2015 Apr 21;112(16):5225-30. doi: 10.1073/pnas.1422998112. Epub 2015 Apr 6.

Abstract

Alzheimer's disease (AD) is one of most devastating diseases affecting elderly people. Amyloid-β (Aβ) accumulation and the downstream pathological events such as oxidative stress play critical roles in pathogenesis of AD. Lessons from failures of current clinical trials suggest that targeting multiple key pathways of the AD pathogenesis is necessary to halt the disease progression. Here we show that Edaravone, a free radical scavenger that is marketed for acute ischemic stroke, has a potent capacity of inhibiting Aβ aggregation and attenuating Aβ-induced oxidation in vitro. When given before or after the onset of Aβ deposition via i.p. injection, Edaravone substantially reduces Aβ deposition, alleviates oxidative stress, attenuates the downstream pathologies including Tau hyperphosphorylation, glial activation, neuroinflammation, neuronal loss, synaptic dysfunction, and rescues the behavioral deficits of APPswe/PS1 mice. Oral administration of Edaravone also ameliorates the AD-like pathologies and memory deficits of the mice. These findings suggest that Edaravone holds a promise as a therapeutic agent for AD by targeting multiple key pathways of the disease pathogenesis.

Keywords: Alzheimer’s disease; BACE1; Edaravone; amyloid-β; oxidative stress.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Alzheimer Disease / complications
  • Alzheimer Disease / drug therapy*
  • Alzheimer Disease / pathology
  • Amyloid / metabolism
  • Amyloid beta-Peptides / toxicity
  • Animals
  • Antipyrine / administration & dosage
  • Antipyrine / analogs & derivatives*
  • Antipyrine / chemistry
  • Antipyrine / pharmacology
  • Antipyrine / therapeutic use
  • Behavior, Animal / drug effects
  • Brain / drug effects
  • Brain / pathology
  • Cell Line
  • Cognition Disorders / complications
  • Cognition Disorders / drug therapy*
  • Cognition Disorders / pathology
  • Dendrites / drug effects
  • Dendrites / pathology
  • Edaravone
  • Humans
  • Inflammation / pathology
  • Mice, Transgenic
  • Neurotoxins / toxicity
  • Oxidative Stress / drug effects
  • Phosphorylation / drug effects
  • Presenilin-1 / metabolism
  • Protein Aggregation, Pathological / complications
  • Protein Aggregation, Pathological / drug therapy
  • Protein Processing, Post-Translational / drug effects
  • tau Proteins / metabolism

Substances

  • Amyloid
  • Amyloid beta-Peptides
  • Neurotoxins
  • Presenilin-1
  • tau Proteins
  • Edaravone
  • Antipyrine