Use of a benzimidazole derivative BF-188 in fluorescence multispectral imaging for selective visualization of tau protein fibrils in the alzheimer's disease brain

Ryuichi Harada, Nobuyuki Okamura, Shozo Furumoto, Takeo Yoshikawa, Hiroyuki Arai, Kazuhiko Yanai, Yukitsuka Kudo

Research output: Contribution to journalArticlepeer-review

36 Citations (Scopus)

Abstract

Purpose: Selective visualization of amyloid-β and tau protein deposits will help to understand the pathophysiology of Alzheimer's disease (AD). Here, we introduce a novel fluorescent probe that can distinguish between these two deposits by multispectral fluorescence imaging technique. Procedures: Fluorescence spectral analysis was performed using AD brain sections stained with novel fluorescence compounds. Competitive binding assay using [ 3H]-PiB was performed to evaluate the binding affinity of BF-188 for synthetic amyloid-β (Aβ) and tau fibrils. Results: In AD brain sections, BF-188 clearly stained Aβ and tau protein deposits with different fluorescence spectra. In vitro binding assays indicated that BF-188 bound to both amyloid-β and tau fibrils with high affinity (K i < 10 nM). In addition, BF-188 showed an excellent blood-brain barrier permeability in mice. Conclusion: Multispectral imaging with BF-188 could potentially be used for selective in vivo imaging of tau deposits as well as amyloid-β in the brain.

Original languageEnglish
Pages (from-to)19-27
Number of pages9
JournalMolecular Imaging and Biology
Volume16
Issue number1
DOIs
Publication statusPublished - 2014 Feb

Keywords

  • Alzheimer's disease
  • Fluorescent probes
  • Multispectral fluorescence imaging
  • Neurofibrillary tangles
  • Senile plaques

ASJC Scopus subject areas

  • Oncology
  • Radiology Nuclear Medicine and imaging
  • Cancer Research

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