Alzheimer's disease is a progressive neurodegenerative disorder with an insidious onset of symptoms. At present, there are no treatments that can effectively stop or reverse the disease from progressing. The development of effective methods for early diagnosis and treatment of Alzheimer's disease is therefore still urgently needed. In this article, we designed a family of Q-series probes () that bind to Aβ aggregates by introducing different electron donors to bind to benzothiazole salts electron acceptors with different substituents to achieve imaging and photooxidation of aggregated Aβ proteins. The structure of the six probes was composed of N, N-dimethylaminophenyl and triphenylamine (donor groups), benzothiazole salts (acceptor groups), and π-conjugated double bonds. Among them, the probe with triphenylamine as the electron donor had a good singlet oxygen production efficiency, which can effectively carry out photooxidation after combining with Aβ aggregates, effectively reducing the degree of aggregation, and the cytotoxicity of Aβ aggregates was significantly reduced after bright light oxidation through cell experiments, which has great potentials in the treatment of Aβ photooxidation. On the other hand, probes and with N, N-dimethylaminophenyl as donors had excellent imaging abilities, good affinities for Aβ (Kd = 26.95 nM, Kd = 21.56 nM), can effectively image Aβ plaques in AD mouse brain slices and monitor the change of cell viscosity, and have a good application prospect in fluorescence imaging.

中文翻译：

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基于 N-甲基苯并噻唑的治疗诊断学作为淀粉样蛋白-β 的荧光成像和光氧化剂

阿尔茨海默病是一种进行性神经退行性疾病，症状起病隐匿。目前，没有任何治疗方法可以有效阻止或逆转疾病的进展。因此，仍然迫切需要开发有效的方法来早期诊断和治疗阿尔茨海默病。在本文中，我们设计了一系列与Aβ聚集体结合的Q系列探针，通过引入不同的电子供体与具有不同取代基的苯并噻唑盐电子受体结合，实现聚集的Aβ蛋白的成像和光氧化。六个探针的结构由N,N-二甲基氨基苯基和三苯胺（供体基团）、苯并噻唑盐（受体基团）和π-共轭双键组成。其中，以三苯胺为电子供体的探针具有良好的单线态氧产生效率，与Aβ聚集体结合后可有效进行光氧化，有效降低聚集程度，强光照射后Aβ聚集体的细胞毒性显着降低通过细胞实验发现氧化作用，在治疗Aβ光氧化方面具有巨大潜力。另一方面，以N,N-二甲基氨基苯基为供体的探针具有优异的成像能力，对Aβ具有良好的亲和力（Kd = 26.95 nM，Kd = 21.56 nM），可以有效对AD小鼠脑切片中的Aβ斑块进行成像并监测其变化细胞粘度的变化，在荧光成像方面具有良好的应用前景。