Chemistry Department, Lomonosov Moscow State University, Leninskie gory 1,3, 119991, Moscow, Russia; Department of Materials Science of Semiconductors and Dielectrics, National University of Science and Technology (MISIS), Leninskiy prospect 4, 101000, Moscow, Russia.
Chemistry Department, Lomonosov Moscow State University, Leninskie gory 1,3, 119991, Moscow, Russia.
Eur J Med Chem. 2024 Oct 5;276:116682. doi: 10.1016/j.ejmech.2024.116682. Epub 2024 Jul 20.
Timely diagnosis and therapy of Alzheimer's disease remains one of the greatest questions in medicinal chemistry of neurodegenerative disease. The lack of low-cost sensors capable of reliable detection of structural changes in AD-related proteins is the driving factor for the development of novel molecules with affinity for AD hallmarks. The development of cheap, safe diagnostic methods is a highly sought-after area of research. Optical fluorescent probes are of great interest due to their non-radioactivity, low cost, and ability of the real-time visualization of AD hallmarks. Boron dipyrromethene (BODIPY)-based fluorophore is one promising fluorescent unit for in vivo labeling due to its high photostability, easy modification, low toxicity, and cell-permeability. In recent years, many fluorescent BODIPY-based probes capable of Aβ plaque, Aβ soluble oligomers, neurofibrillary tangles (NFT) optical detection, as well as probes with copper ion chelating units and viscosity sensors have been developed. In this review, we summarized BODIPY derivatives as fluorescent sensors capable of detecting pathological features of Alzheimer's disease, published from 2009 to 2023, as well as their design strategies, optical properties, and in vitro and in vivo activities.
及时诊断和治疗阿尔茨海默病仍然是神经退行性疾病医学化学的最大问题之一。缺乏能够可靠检测与 AD 相关蛋白质结构变化的低成本传感器，是开发具有 AD 特征亲和力的新型分子的驱动因素。开发廉价、安全的诊断方法是一个备受关注的研究领域。由于其非放射性、低成本以及实时可视化 AD 特征的能力，光学荧光探针引起了极大的兴趣。基于硼二吡咯甲川（BODIPY）的荧光团因其高光稳定性、易于修饰、低毒性和细胞通透性，是用于体内标记的有前途的荧光单元之一。近年来，已经开发了许多能够光学检测 Aβ斑块、Aβ可溶性寡聚物、神经原纤维缠结（NFT）的荧光 BODIPY 探针，以及具有铜离子螯合单元和粘度传感器的探针。在这篇综述中，我们总结了 2009 年至 2023 年期间发表的作为能够检测阿尔茨海默病病理特征的荧光传感器的 BODIPY 衍生物，以及它们的设计策略、光学性质以及体外和体内活性。
