Proflavine derivatives as fluorescent imaging agents of amyloid deposits

Bioorg Med Chem Lett. 2011 Apr 15;21(8):2203-6. doi: 10.1016/j.bmcl.2011.03.010. Epub 2011 Mar 6.

Abstract

A series of proflavine derivatives for use to further image Aβ amyloid deposits were synthesized and characterized. Aged 3xTg-AD (23 months old) mice hippocampus sections incubated with these derivatives revealed preferential labeling of amyloid plaques. Furthermore an in vitro binding study showed an inhibitory effect, although moderate, of these compounds on Aβ(40) fibril formation. This study highlights the potential of proflavine as a molecular scaffold for designing new Aβ imaging agents, its native fluorescence allowing in vitro neuropathological staining in AD damaged brain sections.

MeSH terms

  • Alzheimer Disease / pathology
  • Amyloid beta-Peptides / antagonists & inhibitors
  • Amyloid beta-Peptides / metabolism
  • Animals
  • Disease Models, Animal
  • Fluorescent Dyes / chemistry*
  • Mice
  • Mice, Transgenic
  • Microscopy, Fluorescence
  • Peptide Fragments / antagonists & inhibitors
  • Peptide Fragments / metabolism
  • Plaque, Amyloid / pathology*
  • Proflavine / chemical synthesis
  • Proflavine / chemistry*

Substances

  • Amyloid beta-Peptides
  • Fluorescent Dyes
  • Peptide Fragments
  • amyloid beta-protein (1-40)
  • Proflavine