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用于体内肿瘤诊断的新型IR-822-甲硫氨酸近红外探针的合成。

Synthesis of a Novel IR-822-Met near-infrared probe for in vivo tumor diagnosis.

作者信息

Sun Chunlong, Zhang Hongtao, Du Wen, Wang Baoqin, Ji Min

机构信息

School of Life Sciences, Binzhou University, Binzhou, 256600, China.

Qingdao Municipal Hospital (Group), Qingdao, 266011, China.

出版信息

Biotechnol Lett. 2017 Apr;39(4):491-499. doi: 10.1007/s10529-016-2275-0. Epub 2017 Jan 3.

Abstract

OBJECTIVE

Methionine is a valid target for the treatment of cancer and to achieve in vivo imaging and early diagnosis of tumors, we have synthesized near-infrared (NIR) fluorochrome IR-822-labeled methionine (IR-822-Met).

RESULTS

NIR fluorescent dye IR-822 was conjugated with methionine through its amide bond. It had low toxicity to normal cell/tissues. In vitro and in vivo studies demonstrated its high targeting capability to tumors. The results support the potential of using ligand-modified methionine probe for tumor diagnosis and targeted therapy. The probe also exhibited good photostability, and excellent cell membrane permeability.

CONCLUSION

IR-822-Met is a promising imaging agent for tumor diagnosis, especially in their early stage.

摘要

目的

甲硫氨酸是癌症治疗的有效靶点,为实现肿瘤的体内成像和早期诊断,我们合成了近红外(NIR)荧光染料IR-822标记的甲硫氨酸(IR-822-Met)。

结果

NIR荧光染料IR-822通过其酰胺键与甲硫氨酸偶联。它对正常细胞/组织毒性低。体外和体内研究证明了其对肿瘤的高靶向能力。这些结果支持了使用配体修饰的甲硫氨酸探针进行肿瘤诊断和靶向治疗的潜力。该探针还表现出良好的光稳定性和优异的细胞膜通透性。

结论

IR-822-Met是一种有前景的肿瘤诊断成像剂,尤其是在肿瘤早期。

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