Du Kui, Sheng Li, Luo Xiang, Fan Gang, Shen Dadong, Wu Chunlei, Shen Runpu
School of Chemistry and Chemical Engineering, Shaoxing University, Shaoxing 312000, China.
Research & Development Center, Zhejiang Medicine Co. Ltd. Shaoxing 312500, China.
Spectrochim Acta A Mol Biomol Spectrosc. 2021 Mar 15;249:119328. doi: 10.1016/j.saa.2020.119328. Epub 2020 Dec 15.
Leucine aminopeptidase (LAP) is known as an important potential biomarker for liver malignancy and it is urgent to develop an intuitive and effective method to monitor the activity of LAP in liver cancer. Although, numerous LAP fluorescent probes had been developed, it is still a challenge to detect LAP activity in liver cancer. Herein, combained with the DFT, we reported a novel galactose-appended hepatoma-specific ratiometric fluorescent probe (Gal-QL-Leu) based on quinoline group for imaging and tracing LAP in liver tumor cells. Probe Gal-QL-Leu demonstrated a obvious ratiometric characteristics, better selectivity, good biocompatibility and high sensitivity. Moreover, the selective imaging of LAP in HepG2, HCT116, A549 and HeLa cells had been achieved with probe Gal-QL-Leu, demonstrating good application prospect in the detection of LAP activity in liver tumor cells.
亮氨酸氨肽酶（LAP）被认为是肝脏恶性肿瘤的一种重要潜在生物标志物，因此迫切需要开发一种直观有效的方法来监测肝癌中LAP的活性。尽管已经开发了许多LAP荧光探针，但在肝癌中检测LAP活性仍然是一项挑战。在此，结合密度泛函理论（DFT），我们报道了一种基于喹啉基团的新型半乳糖附加的肝癌特异性比率荧光探针（Gal-QL-Leu），用于在肝肿瘤细胞中成像和追踪LAP。探针Gal-QL-Leu表现出明显的比率特征、更好的选择性、良好的生物相容性和高灵敏度。此外，使用探针Gal-QL-Leu已实现对HepG2、HCT116、A549和HeLa细胞中LAP的选择性成像，表明其在检测肝肿瘤细胞中LAP活性方面具有良好的应用前景。
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