School of Chinese Materia Medica, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, PR China.
School of Chinese Materia Medica, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, PR China.
Spectrochim Acta A Mol Biomol Spectrosc. 2022 Jun 5;274:121110. doi: 10.1016/j.saa.2022.121110. Epub 2022 Mar 6.
Although there is no cure for Alzheimer's disease (AD) due to its complex pathogenesis, early detection and treatment can help delay the development of the disease. So, it is necessary to develop multifunctional metal regulators that can integrate the therapeutics and diagnostics effect against AD. In this work, N-(anthracene-9-ylmethylene)benzohydrazide (probe 1), a fluorescent probe with imine and carbonyl as chelating sites was designed and synthesized. Results showed that 1 had good activities related to AD, such as regulation of metal homeostasis, inhibition of β-amyloid (Aβ) aggregation and scavenging of reactive oxygen species. The selectivity experiment showed that probe 1 had a good recognition effect on Cu. Fluorescence imaging assay also indicated that probe 1 had a good fluorescence imaging effect on Cu in living cells. Furthermore, probe 1 had showed no cytotoxicity and good BBB permeability. These results indicated that probe 1 had potential diagnostic and therapeutic capabilities, and can be used as the multifunctional theranostic agent for AD.
虽然由于阿尔茨海默病（AD）的复杂发病机制，目前还没有治愈方法，但早期发现和治疗可以帮助延缓疾病的发展。因此，有必要开发多功能金属调节剂，以整合针对 AD 的治疗和诊断效果。在这项工作中，设计并合成了具有亚胺和羰基作为螯合位点的荧光探针 N-(蒽-9-亚甲基)苯甲酰肼（探针 1）。结果表明，1 具有与 AD 相关的良好活性，如调节金属内稳态、抑制β-淀粉样蛋白（Aβ）聚集和清除活性氧。选择性实验表明，探针 1 对 Cu 具有良好的识别效果。荧光成像实验也表明，探针 1 对活细胞中的 Cu 具有良好的荧光成像效果。此外，探针 1 表现出无细胞毒性和良好的 BBB 通透性。这些结果表明，探针 1 具有潜在的诊断和治疗能力，可作为 AD 的多功能治疗药物。
