Yang Dan, Wang Huasen, Sun Chengjie, Zhao Hui, Hu Kuan, Qin Weirong, Ma Rui, Yin Feng, Qin Xuan, Zhang Qianling, Liang Yongye, Li Zigang
School of Chemical Biology and Biotechnology , Shenzhen Graduate School of Peking University , Shenzhen , 518055 , China . Email:
Department of Materials Science and Engineering , South University of Science and Technology of China , Shenzhen 518055 , China . Email:
Chem Sci. 2017 Sep 1;8(9):6322-6326. doi: 10.1039/c7sc02698f. Epub 2017 Jul 19.
A fluorescent dye, FEB, with high fluorescence quantum yield for tumour imaging is reported. FEB dyes can be efficiently synthesized in three steps and then easily modified with either PEG or PEG-iRGD to yield FEB-2000 or FEB-2000-iRGD, respectively. Both modified dyes showed negligible toxicity and were thus able to be adopted for tumour imaging. PEG modification endowed the dye FEB-2000 with both long circulating times and good tumour targeting properties in a MDA-MB-231 xenograft model. Further conjugation with iRGD to generate FEB-2000-iRGD showed minimal targeting enhancement. These results provide a template for the efficient preparation of FEB dyes for use in tumour imaging, thus providing a foundation for future modifications.
据报道,一种用于肿瘤成像的具有高荧光量子产率的荧光染料FEB。FEB染料可通过三步高效合成,然后分别用聚乙二醇(PEG)或聚乙二醇-整合素靶向肽(PEG-iRGD)轻松修饰,分别得到FEB-2000或FEB-2000-iRGD。两种修饰后的染料均显示出可忽略不计的毒性,因此能够用于肿瘤成像。在MDA-MB-231异种移植模型中,PEG修饰赋予了染料FEB-2000较长的循环时间和良好的肿瘤靶向特性。进一步与iRGD偶联生成FEB-2000-iRGD,显示出最小的靶向增强效果。这些结果为高效制备用于肿瘤成像的FEB染料提供了模板,从而为未来的修饰奠定了基础。