State Key Laboratory of Luminescent Materials and Devices, College of Materials Science and Engineering , South China University of Technology , Guangzhou 510640 , China.
Anal Chem. 2018 Aug 7;90(15):8807-8815. doi: 10.1021/acs.analchem.8b00594. Epub 2018 Jul 17.
Melanoma is a type of highly malignant and metastatic skin cancer, and early detection of melanoma by analyzing the level of its biomarker may decrease the likelihood of mortality. In this study, a fluorescent probe called NBR-AP for detecting tyrosinase (a biomarker of melanoma) has been created by incorporating a hydroxyphenylurea group (as a substrate for the enzyme) onto a fluorescent dye phenoxazine derivative (as an activatable signal reporter). This probe can be activated to generate fluorescence through a tyrosinase-mediated oxidation followed by hydrolysis of the urea linkage. The probe is able to detect the endogenous tyrosinase level in live cells and in zebrafish sensitively and selectively. Moreover, by imaging the tyrosinase activity, NBR-AP has been successfully applied to diagnose the melanoma and its metastasis in xenogeneic mouse models established via subcutaneous injection of B16F10 cells.
黑色素瘤是一种高度恶性和转移性皮肤癌，通过分析其生物标志物的水平来早期检测黑色素瘤，可能降低死亡率。在这项研究中，通过将羟基苯脲基团（作为酶的底物）结合到荧光染料吩嗪衍生物（作为可激活的信号报告器）上，创建了一种称为 NBR-AP 的荧光探针，用于检测酪氨酸酶（黑色素瘤的生物标志物）。该探针可以通过酪氨酸酶介导的氧化作用随后水解脲键来被激活以产生荧光。该探针能够在活细胞和斑马鱼中敏感且选择性地检测内源性酪氨酸酶水平。此外，通过成像酪氨酸酶活性，NBR-AP 已成功应用于通过皮下注射 B16F10 细胞建立的异种小鼠模型中诊断黑色素瘤及其转移。
