Department of Biomedical Engineering, School of Life Science and Technology, China Pharmaceutical University, Nanjing 210009, China.
Mol Imaging Biol. 2012 Dec;14(6):699-707. doi: 10.1007/s11307-012-0560-4.
A novel near infrared fluorescent probe, L-methyl-methionine (Met)-ICG-Der-02, was synthesized and characterized for in vivo imaging of tumors and early diagnosis of cancers.
Met was conjugated with ICG-Der-02 dye through the amide bond function by ethyl-3-(3-dimethyllaminopropyl) carbodiimide hydrochloride/N-hydroxysuccinimide catalysis chemistry. Met-ICG-Der-02 probe uptake was evaluated on PC3, MDA-MB-231, and human embryonic lung fibroblast cell lines. The dynamics of Met-ICG-Der-02 was investigated in athymic nude mice prior to evaluation of the probe targeting capability in prostate and breast cancer models.
Met-ICG-Der-02 was successfully synthesized. Cell experiments demonstrated excellent cellular uptake of Met-ICG-Der-02 on cancer cell lines without cytotoxicity. Optical imaging showed a distinguishable fluorescence signal in the tumor area at 2 h while maximal tumor-to-normal tissue contrast ratio was at 12 h Met-ICG-Der-02 post-injection. Additionally, dynamic study of the probe indicated intestinal and liver-kidney clearance pathways.
Met-ICG-Der-02 probe is a promising optical imaging agent for tumor diagnosis, especially in their early stage.
合成了一种新型近红外荧光探针 L-甲硫氨酸（Met）-ICG-Der-02，并对其进行了表征，用于肿瘤的体内成像和癌症的早期诊断。
Met 通过盐酸 1-乙基-3-（3-二甲基氨基丙基）碳二亚胺/N-羟基琥珀酰亚胺催化化学与 ICG-Der-02 染料通过酰胺键功能连接。在 PC3、MDA-MB-231 和人胚肺成纤维细胞系上评估了 Met-ICG-Der-02 探针的摄取情况。在评估前列腺癌和乳腺癌模型中探针的靶向能力之前，在无胸腺裸鼠中研究了 Met-ICG-Der-02 的动力学。
成功合成了 Met-ICG-Der-02。细胞实验表明，Met-ICG-Der-02 在癌细胞系上具有出色的细胞摄取能力，且无细胞毒性。光学成像显示，在注射后 2 小时时，肿瘤区域有明显的荧光信号，而在 12 小时时肿瘤与正常组织的对比率最大。此外，探针的动态研究表明了肠道和肝肾清除途径。
Met-ICG-Der-02 探针是一种很有前途的肿瘤诊断光学成像剂，特别是在早期阶段。
