Bivalent ligand containing curcumin and cholesterol as a fluorescence probe for Aβ plaques in Alzheimer's disease

Kai Liu, Tai L. Guo, Jeremy Chojnacki, Hyoung Gon Lee, Xinglong Wang, Sandra L. Siedlak, Wei Rao, Xiongwei Zhu, Shijun Zhang

Research output: Contribution to journalArticlepeer-review

54 Scopus citations

Abstract

A recently developed bivalent ligand BMAOI 14 (7) has been evaluated for its ability to label and detect aggregated β-amyloid (Aβ) peptide as a fluorescent probe. This probe contains curcumin as the Aβ recognition moiety and cholesterol as an anchor to the neuronal cell membrane-lipid rafts. The results demonstrate that 7 binds to the monomers, oligomers, and fibrils of Aβ42 with low micromolar to submicromolar binding affinities. This chemical probe also has many of the required optical properties for use in imaging and can rapidly cross the blood-brain barrier in vivo. Furthermore, 7 specifically binds to Aβ plaques in both Alzheimer's disease human patients and Aβ precursor protein transgenic mouse brain tissues. Collectively, these results suggest that 7 is a strong candidate as an Aβ imaging agent and encourage further optimization of 7 as a new lead for the development of the next generation of Aβ imaging probes.

Original languageEnglish (US)
Pages (from-to)141-146
Number of pages6
JournalACS Chemical Neuroscience
Volume3
Issue number2
DOIs
StatePublished - Feb 15 2012
Externally publishedYes

Keywords

  • Aâ plaques
  • Alzheimer's disease
  • Bivalent ligands
  • fluorescent probes

ASJC Scopus subject areas

  • Biochemistry
  • Physiology
  • Cognitive Neuroscience
  • Cell Biology

Fingerprint Dive into the research topics of 'Bivalent ligand containing curcumin and cholesterol as a fluorescence probe for Aβ plaques in Alzheimer's disease'. Together they form a unique fingerprint.

Cite this