In this section, you can access to the latest technical information related to the FUTURE project topic.

Evaluation of N, O-Benzamide difluoroboron derivatives as near-infrared fluorescent probes to detect ?-amyloid and tau tangles

?-Amyloid (A?) plaques and Tau tangles are cognitive impairment markers vital for diagnosing and preventing Alzheimer's disease (AD). To systematically explore the relationship between the number or position of nitrogen atoms and their optical properties and biological properties, five series of new N, O-coordinated organo-difluoroboron probes were introduced as binding scaffolds for A? plaques and Tau tangles. These probes exhibited suitable optical properties for near-infrared (NIR) imaging. Probe 4PmNO-2 (4-((1E,3E)-4-(1,1-difluoro-1H-1?4,9?4-pyrimido[1,6-c][1,3,5,2]oxadiazaborinin-3-yl)buta-1,3-dien-1-yl)-N,N-dimethylaniline) displayed the excellent emission maximum (716?nm in PBS), a high quantum yield (61.4% in CH2Cl2), and a high affinity for synthetic A?1?42 (Kd?=?23.64???1.08?nM) and Tau (K18) aggregates (Kd?=?26.38???1.29?nM), as well as for native A? plaques and NFTs in the brain tissue from AD patients. 4PmNO-2, with significantly enhanced fluorescence (A?1?42, 136 fold; Tau (K18), 96 fold) and the highest initial brain uptake (11.57% ID/g at 2?min) in normal ICR mice, was evaluated further. In?vivo NIR fluorescent imaging studies in living A? and Tau transgenic mice revealed that it could differentiate healthy and diseased animals. Further ex?vivo fluorescent staining studies showed that 4PmNO-2 specifically bound to A? plaques and Tau tangles in transgenic mice. In summary, the probe 4PmNO-2 may be a useful near-infrared fluorescence (NIRF) probe for AD biomarkers.

» Author: Yimin Chen, Qingwen Ouyang, Yuying Li, Qi Zeng, Bin Dai, Yi Liang, Baian Chen, Hongwei Tan, Mengchao Cui

» Publication Date: 05/01/2022

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