Department of Biomedical Engineering, School of Engineering, State Key Laboratory of Natural Medicines , China Pharmaceutical University , 24 Tongjia Lane , Gulou District, Nanjing 210009 , China.
Mol Pharm. 2018 Aug 6;15(8):3167-3176. doi: 10.1021/acs.molpharmaceut.8b00233. Epub 2018 Jul 9.
Methionine (Met) is one of the essential amino acids of which the transport system L is overexpressed in various tumor cells. In this study, a near-infrared fluorescent dye (IR-780) and methionine were conjugated through a piperazin-polyamines linker to form Cy-Met. The successful synthesis of Cy-Met was validated by optical characterization, NMR, and MS spectra. The absorption peak of Cy-Met was at 680 nm, and the fluorescence peak was at 790 nm. The cytotoxicity assay and cell imaging studies indicated that Cy-Met had good biocompatibility and specific affinity to tumor cells. The dynamic distribution and clearance investigations showed that Cy-Met was eliminated by the liver-intestine pathway. Notably, Cy-Met displayed tumor-targeting ability in U87, H22, and EAC tumor-bearing mice with an evident long circulation time. The results implied that Cy-Met could act as a promising fluorescence probe specialized for long-term tumor monitoring.
蛋氨酸（Met）是必需氨基酸之一，其转运系统 L 在各种肿瘤细胞中过度表达。在本研究中，通过哌嗪多胺连接物将近红外荧光染料（IR-780）和蛋氨酸连接，形成 Cy-Met。通过光学特性、NMR 和 MS 光谱验证了 Cy-Met 的成功合成。Cy-Met 的吸收峰在 680nm，荧光峰在 790nm。细胞毒性试验和细胞成像研究表明，Cy-Met 具有良好的生物相容性和对肿瘤细胞的特异性亲和力。动态分布和清除研究表明，Cy-Met 经肝肠途径消除。值得注意的是，Cy-Met 在荷 U87、H22 和 EAC 肿瘤小鼠中表现出肿瘤靶向能力，具有明显的长循环时间。结果表明，Cy-Met 可以作为一种有前途的荧光探针，专门用于长期肿瘤监测。
