In vivo monitoring neuropathological changes in Alzheimer’s disease (AD) animal model is critical for drug development. Here, by integrating blood-brain barrier penetrable peptide, we have developed a peptide probe which based on angiopep-2. Angiopep-based probe exhibited high binding affinity to Aβ aggregates and labeled senile plaques in vivo. Remarkably, the in vivo near-infrared imaging data revealed that fluorescence signals of this probe were nearly 3-fold higher in the brains of 16-month-old APP/PS1 transgenic mice compared to C57 mice and exhibited linear correlation with the senile plaques load process in 4-, 8-, 16-month-old APP/PS1 transgenic mice. Moreover, senile plaques load was detected in vivo as early as 4 months of age that even at the very beginning of plaques developed in APP/PS1 transgenic mice. Taken together, this novel peptide-based probe achieved dynamic monitoring senile plaques in APP/PS1 transgenic mice and have been ready to use in drug development in AD mouse model.

体内监测阿尔茨海默病 (AD) 动物模型的神经病理学变化对于药物开发至关重要。在这里，通过整合血脑屏障穿透肽，我们开发了一种基于angiopep-2的肽探针。基于 Angiopep 的探针在体内对 Aβ 聚集体和标记的老年斑表现出高结合亲和力。值得注意的是，体内近红外成像数据显示，与 C57 小鼠相比，该探针的荧光信号在 16 个月大的 APP/PS1 转基因小鼠的大脑中高出近 3 倍，并且与老年斑负荷呈线性相关4、8、16 个月大的 APP/PS1 转基因小鼠的过程。此外，早在 4 个月大时就在体内检测到老年斑负荷，甚至在 APP/PS1 转基因小鼠中斑块形成的最开始。综合起来，