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Development of novel theranostic agents for in vivo amyloid imaging and protective effects on human neuroblastoma cells.

Abstract：

:Brain amyloid deposits have been identified as the main neuropathological hallmarks of Alzheimer's diseases (AD) and intensive efforts have been devoted to develop aggregation inhibitors preventing the formation of toxic oligomeric Aβ for therapeutic. In addition, evidence indicates that the formation and accumulation of β-amyloid plaques probably precede clinical symptoms by around 20 years and imaging of such plaques would be beneficial for early-stage AD detection. In this study, we investigated phenothiazine-based compounds as novel promising theranostic agents for AD. These multifunctional agents exhibited BBB permeability, low neurotoxicity, good bio-stability as well as strong turn-on fluorescence with a Stokes shift upon binding to Aβ aggregates. They had metal-chelating property which could delay Aβ aggregation and displayed high binding affinity for β-amyloid aggregates. Moreover, they have been simultaneously applied to perform in vivo near-infrared fluorescence imaging of β-amyloid plaques in double transgenic AD mouse model, to prevent self-aggregation of Aβ monomer from forming toxic oligomers and to protect human neuroblastoma SH-SY5Y cells against Aβ-induced toxicity and oxidative stress.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Li Y,Yan L,Cai J,Zhang W,Li L,Du Z,Dong C,Meunier B,Chen H

doi

10.1016/j.ejmech.2019.111585

subject

Has Abstract

pub_date

2019-11-01 00:00:00

pages

111585

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(19)30719-6

journal_volume

181

pub_type

杂志文章

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