Anti-amyloid activities of three different types of water-soluble fullerene derivatives

Colloids Surf B Biointerfaces. 2019 Nov 1:183:110426. doi: 10.1016/j.colsurfb.2019.110426. Epub 2019 Aug 9.

Abstract

Anti-amyloid activity, aggregation behaviour, cytotoxicity and acute toxicity were investigated for three water-soluble fullerene derivatives with different types of solubilizing addends. All investigated compounds showed a strong anti-amyloid effect in vitrocaused by interaction of the water-soluble fullerene derivatives with the Ab(1-42)-peptide and followed by destruction of the amyloid fibrils. Notably, all of the studied fullerene derivatives showed very low cytotoxicity and low acute toxicity in mice (most promising compound 3 was more than four times less toxic than aspirin). Strong anti-amyloid effect of the fullerene derivatives together with low toxicity reveals high potential of these compounds as drug candidates for treatment of neurodegenerative diseases.

Keywords: Anti-amyloid activity; Fullerene derivatives.

MeSH terms

  • A549 Cells
  • Amyloid beta-Peptides / antagonists & inhibitors*
  • Amyloid beta-Peptides / chemistry
  • Animals
  • Animals, Newborn
  • Coculture Techniques
  • Fullerenes / chemistry
  • Fullerenes / pharmacology*
  • Hippocampus / chemistry
  • Hippocampus / cytology
  • Hippocampus / drug effects
  • Humans
  • Male
  • Mice
  • Neuroglia / chemistry
  • Neuroglia / cytology
  • Neuroglia / drug effects*
  • Neurons / chemistry
  • Neurons / cytology
  • Neurons / drug effects*
  • Neuroprotective Agents / chemical synthesis
  • Neuroprotective Agents / pharmacology*
  • Peptide Fragments / antagonists & inhibitors*
  • Peptide Fragments / chemistry
  • Protein Aggregates / drug effects*
  • Rats
  • Rats, Sprague-Dawley
  • Solubility
  • Structure-Activity Relationship
  • Toxicity Tests, Acute
  • Water / chemistry

Substances

  • Amyloid beta-Peptides
  • Fullerenes
  • Neuroprotective Agents
  • Peptide Fragments
  • Protein Aggregates
  • amyloid beta-protein (1-42)
  • Water