Amyloid-β peptide (Aβ) aggregates, particularly Aβ oligomers, are established biomarker and toxic species in Alzheimer’s disease (AD). Early detection and disaggregation of Aβ aggregates are of great importance for the treatment of AD due to the unavailability of therapy at the advanced stages of the disease. A multitalented agent, 2-{2-[(1H-benzoimidazol-2-yl)methoxy] phenyl}benzothiazole (BPB), is designed by merging two β-sheet targeting groups into one molecule to detect and inhibit the Aβ aggregation. BPB can quantitatively measure the β-sheet level of soluble Aβ oligomers and specifically distinguish the aggregates of Aβ40 and Aβ42 by unique luminescence spectrum. Animal tests demonstrate that BPB can efficiently penetrate the blood brain barrier and precisely stain Aβ plaques in the brain; more importantly, it can differentiate the blood of APP transgenic mice from that of normal ones. In addition to the diagnostic potential, BPB also suppresses the generation of ROS, protects the neurons from neurotoxicity, and disaggregates the Aβ aggregates in brain homogenates of APP transgenic mice induced by metal ions or self-assembly. In view of its detective ability toward Aβ oligomers and inhibition to Aβ-related neurotoxicity, BPB may be developed into a sensitive probe for screening blood samples in the early diagnosis of AD as well as an effective inhibitor for diminishing Aβ aggregates in the treatment of the disease.

中文翻译：

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靶向β片治疗剂，用于诊断和预防阿尔茨海默氏病中致病性肽的聚集

淀粉样蛋白-β肽（Aβ）聚集体，尤其是Aβ寡聚体，是阿尔茨海默病（AD）中已确立的生物标志物和有毒物种。由于缺乏在疾病晚期的治疗方法，Aβ聚集体的早期检测和分解对于AD的治疗非常重要。多才多艺的代理人，2- {2-[（1 H-苯并咪唑-2-基）甲氧基]苯基}苯并噻唑（BPB）是通过将两个β-折叠靶向基团合并到一个分子中来检测和抑制Aβ聚集而设计的。BPB可以定量测量可溶性Aβ低聚物的β-折叠水平，并通过独特的发光光谱来区分Aβ40和Aβ42的聚集体。动物实验表明，BPB可以有效穿透血脑屏障并精确染色大脑中的Aβ斑块。更重要的是，它可以将APP转基因小鼠的血液与正常小鼠的血液区分开。除了具有诊断潜力外，BPB还抑制ROS的产生，保护神经元免受神经毒性，并分解由金属离子或自组装诱导的APP转基因小鼠脑匀浆中的Aβ聚集体。