体内
化学
生物物理学
纤维
神经毒性
生物化学
毒性
生物
生物技术
有机化学
作者
Qian Zhang,Xiaoyu Chen,Congmin Yuan,Xiaobin Pang,Ping Shangguan,Yi‐Sheng Liu,Lulu Han,Jianwei Sun,Jacky W. Y. Lam,Yang Liu,Jiefei Wang,Bingyang Shi,Ben Zhong Tang
标识
DOI:10.1002/anie.202211550
摘要
Optimized theranostic strategies for Alzheimer's disease (AD) remain almost absent from bench to clinic. Current probes and drugs attempting to prevent β-amyloid (Aβ) fibrosis encounter failures due to the blood-brain barrier (BBB) penetration challenge and blind intervention time window. Herein, we design a near-infrared (NIR) aggregation-induced emission (AIE) probe, DNTPH, via balanced hydrophobicity-hydrophilicity strategy. DNTPH binds selectively to Aβ fibrils with a high signal-to-noise ratio. In vivo imaging revealed its excellent BBB permeability and long-term tracking ability with high-performance AD diagnosis. Remarkably, DNTPH exhibits a strong inhibitory effect on Aβ fibrosis and promotes fibril disassembly, thereby attenuating Aβ-induced neurotoxicity. DNTPH treatment significantly reduced Aβ plaques and rescued learning deficits in AD mice. Thus, DNTPH serves as the first AIE in vivo theranostic agent for real-time NIR imaging of Aβ plaques and AD therapy simultaneously.
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