Methionine-Decorated Near Infrared Fluorescent Probe for Prolonged Tumor Imaging,Molecular Pharmaceutics

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Methionine-Decorated Near Infrared Fluorescent Probe for Prolonged Tumor Imaging
Molecular Pharmaceutics ( IF 4.5 ) Pub Date : 2018-06-13 00:00:00 , DOI: 10.1021/acs.molpharmaceut.8b00233
Chen Wei ₁ , Zhenwei Yuan ₁ , Jinrong Zheng ₁ , Habtamu Kassaye ₁ , Lijuan Gui ₁ , Fei Wang ₁ , Hao Wan ₁ , Yue Xu ₁ , Qing He ₁ , Murat Er ₁ , Yi Ma ₁ , Haiyan Chen ₁

Affiliation

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.

中文翻译：

蛋氨酸修饰的近红外荧光探针可延长肿瘤的成像时间

蛋氨酸（Met）是必需的氨基酸之一，其转运系统L在各种肿瘤细胞中都过表达。在这项研究中，通过哌嗪-多胺接头将近红外荧光染料（IR-780）和蛋氨酸结合形成Cy-Met。通过光学表征，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。细胞毒性测定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被肝肠途径消除。值得注意的是，Cy-Met在具有明显长循环时间的U87，H22和EAC荷瘤小鼠中显示出肿瘤靶向能力。

更新日期：2018-06-13

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