Department of Chemistry; Department of Biology
Alzheimer’s disease (AD) is the most prevalent but still incurable neurodegenerative form of dementia. Early diagnosis and intervention are crucial for delaying the onset and progression of the disease. We herein report a novel fluoro-substituted cyanine, F-SLOH, which exhibits good Aβ oligomer selectivity with a high binding affinity, attributed to the synergistic effect of strong π–π stacking and intermolecular CH⋯O and CH⋯F interactions. The selectivity towards the Aβ oligomers in the brain was ascertained by in vitrolabelling on tissue sections and in vivo labelling through the systemic administration of F-SLOH in 7 month APP/PS1 double transgenic (Tg) and APP/PS1/Tau triple Tg mouse models. F-SLOH also shows remarkably effective inhibition on Aβ aggregation and highly desirable neuroprotective effects against Aβ-induced toxicities, including the inhibition of ROS production and Ca2+ influx. Its excellent blood–brain barrier (BBB) penetrability and low bio-toxicity further support its tremendous potential as a novel theranostic agent for both early diagnosis and therapy of AD.
Source Publication Title
Royal Society of Chemistry
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The authors acknowledge the nancial support through the Cooperative Research Fund of Hong Kong Research Grant Council (C2012-15G), the Faculty Research Grant of Hong Kong Baptist University (FRG2/15-16/054), the General Research Fund (12301317), the 2014 Hong Kong Scholars Program, the China Postdoctoral Science Foundation funded project (2015M580685), the National Natural Science Foundation of China (21305036, 21675135, 30470594 and 30772282) and the Hunan Provincial Natural Science Foundation of China (2015JJ3035).
Link to Publisher's Edition
Li, Yinhui, Di Xu, Anyang Sun, See-Lok Ho, Chung-Yan Poon, Hei-Nga Chan, Olivia T. W. Ng, Ken K. L. Yung, Hui Yan, Hung-Wing LI, and Man Shing Wong. "Fluoro-substituted cyanine for reliable in vivo labelling of amyloid-β oligomers and neuroprotection against amyloid-β induced toxicity." Chemical Science 8.12 (2017): 8279-8284.
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