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一种基于咪唑的极性敏感探针,用于脂滴靶向和体内肿瘤成像。

An imidazole-derived polarity sensitive probe for lipid droplet target and in vivo tumor imaging.

机构信息

Department of Oncology, Fuyang Hospital of Anhui Medical University, Fuyang, 236000, China; School of Pharmacy, Anhui Medical University, Hefei, 230032, China.

School of Pharmacy, Anhui Medical University, Hefei, 230032, China.

出版信息

Talanta. 2023 Jan 15;252:123903. doi: 10.1016/j.talanta.2022.123903. Epub 2022 Sep 1.

Abstract

Accurate differentiation of tumor cells from normal cells is a fundamental and critical challenge for the early diagnosis of cancer. The intrinsic low-polarity and increased numbers of lipid droplets can be utilized as potential biomarkers for tumor cells. Therefore, we synthesized and screened the polar fluorescent probe (PI-CHO), which exhibiting notable fluorescence color change and spectral shift in solvents of different polarities. PI-CHO has a high sensitivity to polarity changes in the linear range of E(30) = 37.4-63.1, with a fluorescence enhancement of more than 474-folds. Intracellular imaging experiments showed that PI-CHO has low cytotoxicity, excellent lipid droplet-targeted performance and discernibility between tumor and normal cells. Ex vivo imaging of the tumors and major organs demonstrated the great reliability and sensitive responsiveness of PI-CHO towards tumors. Moreover, the proposed probe was successfully applied to detect tumors in living mice, exhibiting the potential to become a powerful tool in early cancer diagnosis.

摘要

准确地区分肿瘤细胞和正常细胞是癌症早期诊断的一个基本和关键挑战。内在的低极性和更多数量的脂滴可以作为肿瘤细胞的潜在生物标志物。因此,我们合成并筛选了极性荧光探针(PI-CHO),它在不同极性溶剂中表现出显著的荧光颜色变化和光谱位移。PI-CHO 在 E(30) = 37.4-63.1 的线性范围内对极性变化具有高灵敏度,荧光增强超过 474 倍。细胞内成像实验表明,PI-CHO 具有低细胞毒性、优异的脂滴靶向性能以及肿瘤细胞和正常细胞之间的可分辨性。肿瘤和主要器官的离体成像表明,PI-CHO 对肿瘤具有很高的可靠性和敏感响应性。此外,该探针已成功应用于活体小鼠肿瘤的检测,有望成为癌症早期诊断的有力工具。

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