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用于急性哮喘成像的脂质滴靶向近红外极性探针

Lipid Droplet-Targeted NIR Polarity Probe for the Imaging of Acute Asthma .

作者信息

Li Mingyue, Zhu Yanmei, Hu Linlin, Li Jun, Yoo Jiyoung, Zhang Huamei, Qian Zhaosheng, Zhou Xucong, Kim Jong Seung, Zhou Jin

机构信息

School of Pharmacy, School of Basic Medical Sciences, Shandong Second Medical University, Weifang 261053, China.

Weifang People's Hospital, Shandong Second Medical University, Weifang 261000, China.

出版信息

J Med Chem. 2025 Jul 24;68(14):15165-15175. doi: 10.1021/acs.jmedchem.5c01403. Epub 2025 Jul 11.

Abstract

Polarity changes are significant indicators during inflammation. Acute lung injury (ALI) and asthma, both inflammatory lung diseases, necessitate the detection of these polarity changes for early diagnosis and treatment monitoring. We designed and synthesized a lipid droplet-targeting, polarity-dependent near-infrared fluorescent probe, , on the basis of an intramolecular charge-transfer mechanism to noninvasively detect these inflammatory conditions. The probe exhibits a consistent decrease in fluorescence intensity with an increase in solvent polarity, demonstrating excellent photostability and biocompatibility. Utilizing , we can differentiate between normal cells and cancer cells and successfully detect polarity changes targeting lipid droplets within the lungs of mice suffering from ALI and asthma. Furthermore, we can monitor the therapeutic effects of dexamethasone on asthmatic mice, confirming the clinical application potential of . In summary, we believe that offers a novel and effective approach to the diagnosis of acute ALI and asthma.

摘要

极性变化是炎症过程中的重要指标。急性肺损伤(ALI)和哮喘均为炎症性肺部疾病,需要检测这些极性变化以进行早期诊断和治疗监测。我们基于分子内电荷转移机制设计并合成了一种靶向脂滴、依赖极性的近红外荧光探针,用于无创检测这些炎症状态。该探针随着溶剂极性的增加荧光强度持续降低,表现出优异的光稳定性和生物相容性。利用该探针,我们能够区分正常细胞和癌细胞,并成功检测患有ALI和哮喘的小鼠肺内靶向脂滴的极性变化。此外,我们可以监测地塞米松对哮喘小鼠的治疗效果,证实了该探针的临床应用潜力。总之,我们认为该探针为急性ALI和哮喘的诊断提供了一种新颖有效的方法。

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