Rofecoxib derivatives as NIR fluorescent probes for mitochondrial viscosity and in vivo imaging of Aβ plaques

作者：Anwar, Gulziba; Chen, Daoyuan; Chen, Qingxiu; Xia, Chunli^*; Yan, Jinwu^*

来源：Spectrochimica Acta - Part A: Molecular and Biomolecular Spectroscopy , 2024, 307: 123637.

DOI：10.1016/j.saa.2023.123637

• Alzheimer's disease
• Beta-amyloid
• Rofecoxib
• Fluorescence imaging
• Viscosity

Alzheimer's disease (AD) is a multifaceted neurodegenerative disorder for which the underlying causes remain largely unknown. Therefore, the development of imaging agents capable of detecting biomarkers associated with this disease is crucial. Dual -functional probes are particularly important as they can track two biomarkers at the same time and examine their interaction. Herein, Two red -emissive dual -functional fluorescent probes, RC -1 and RA -2, have been designed and synthesized based on the Rofecoxib scaffold. When probes (RC -1 and RA -2) are in viscous media or bound to A beta aggregates, there is a dramatic enhancement in fluorescence emission due to the constraint of the twisted intramolecular charge transfer effect (TICT). RC -1 with ideal blood-brain barrier (BBB) penetrability enables visualization of A beta plaques in vivo AD mice. These results suggest that RC -1 and RA -2 have the potential to serve as powerful fluorescence imaging agents for A beta and mitochondria -related pathology in AD.