Galantamine inhibits beta-amyloid aggregation and cytotoxicity

J Neurol Sci. 2009 May 15;280(1-2):49-58. doi: 10.1016/j.jns.2009.01.024. Epub 2009 Feb 26.

Abstract

The ability of galantamine (Reminyl) to inhibit the aggregation and toxicity of the beta-amyloid peptide (Abeta) was investigated. Galantamine showed concentration-dependent inhibition of aggregation of both Abeta 1-40 and Abeta 1-42, as determined by an ELISA method. Electron microscope studies of Abeta 1-40 incubated in the presence of galantamine revealed fibrils that were disordered and clumped in appearance. MTT and lactate dehydrogenase assays, employing SH-SY5Y human neuroblastoma cells, showed that galantamine reduced the cytotoxicity induced by Abeta 1-40. Galantamine also dramatically reduced Abeta 1-40-induced cellular apoptosis in these cells. There is some evidence that galantamine may not be acting purely as a symptomatic treatment. Disease-modifying effects of the drug could be due to an additional effect on Abeta aggregation and/or toxicity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amyloid beta-Peptides / drug effects*
  • Amyloid beta-Peptides / metabolism
  • Amyloid beta-Peptides / toxicity
  • Analysis of Variance
  • Apoptosis / drug effects
  • Cell Line, Tumor
  • Cholinesterase Inhibitors / chemistry
  • Cholinesterase Inhibitors / pharmacology*
  • Dose-Response Relationship, Drug
  • Enzyme-Linked Immunosorbent Assay
  • Galantamine / chemistry
  • Galantamine / pharmacology*
  • Humans
  • L-Lactate Dehydrogenase / metabolism
  • Microscopy, Electron
  • Models, Molecular
  • Neuroprotective Agents / chemistry
  • Neuroprotective Agents / pharmacology*
  • Nuclear Magnetic Resonance, Biomolecular
  • Peptide Fragments / drug effects*
  • Peptide Fragments / metabolism
  • Peptide Fragments / toxicity

Substances

  • Amyloid beta-Peptides
  • Cholinesterase Inhibitors
  • Neuroprotective Agents
  • Peptide Fragments
  • amyloid beta-protein (1-40)
  • amyloid beta-protein (1-42)
  • Galantamine
  • L-Lactate Dehydrogenase