Synthesis and in vivo characterization of ¹⁸F-labeled difluoroboron-curcumin derivative for β-amyloid plaque imaging.

ABSTRACT: Positron emission tomography imaging of β-amyloid (Aβ) plaques has proven useful in the diagnosis of Alzheimer's disease. A previous study from our group showed that 4'-O-[¹⁸F]fluoropropylcurcumin has poor brain permeability, which is thought to be due to its rapid metabolism. In this study, we synthesized difluoroboron complexes of fluorine-substituted curcumin derivatives (1-4) and selected one of them based on the in vitro binding assays. The selected ligand 2 was found to distinctively stain Aβ plaques in APP/PS1 transgenic mouse brain sections. Radioligand [¹⁸F]2 was synthesized via a two-step reaction consisting of [¹⁸F]fluorination and subsequent aldol condensation. Biodistribution and metabolism studies indicated that radioligand [¹⁸F]2 w

SUBMITTER: Kim H 

PROVIDER: S-EPMC6494845 | biostudies-literature | 2019 May

REPOSITORIES: biostudies-literature