Sun Yao, Ding Mingmin, Zeng Xiaodong, Xiao Yuling, Wu Huaping, Zhou Hui, Ding Bingbing, Qu Chunrong, Hou Wei, Er-Bu Aga, Zhang Yejun, Cheng Zhen, Hong Xuechuan
State Key Laboratory of Virology , Key Laboratory of Combinatorial Biosynthesis and Drug Discovery (MOE) , Hubei Provincial Key Laboratory of Developmentally Originated Disease , Wuhan University School of Pharmaceutical Sciences , Wuhan 430071 , China . Email:
Key Laboratory of Pesticides and Chemical Biology , Ministry of Education , College of Chemistry , Central China Normal University , Wuhan 430079 , China.
Chem Sci. 2017 May 1;8(5):3489-3493. doi: 10.1039/c7sc00251c. Epub 2017 Feb 21.
Though high brightness and biocompatible small NIR-II dyes are highly desirable in clinical or translational cancer research, their fluorescent cores are relatively limited and their synthetic processes are somewhat complicated. Herein, we have explored the design and synthesis of novel NIR-II fluorescent materials () without tedious chromatographic isolation with improved fluorescence performance (QY ≈ 2%) by introducing 2-amino 9,9-dialkyl-substituted fluorene as a donor into the backbone. Several types of water-soluble and biocompatible NIR-II probes: , , and were constructed different chemical strategies based on , and then their potential to be used in tumor imaging and image-guided surgery in the NIR-II region was explored. High levels of uptake were obtained for both passive and active tumor targeting probes and . Furthermore, high resolution imaging of blood vessels on tumors and the whole body of living mice using for the first time has demonstrated precise NIR-II image-guided sentinel lymph node (SLN) surgery.
尽管在临床或转化癌症研究中非常需要高亮度且具有生物相容性的近红外二区（NIR-II）染料，但其荧光核心相对有限，合成过程也较为复杂。在此，我们探索了新型近红外二区荧光材料的设计与合成，通过将2-氨基-9,9-二烷基取代芴作为供体引入主链，无需繁琐的柱色谱分离即可获得具有改善荧光性能（量子产率约为2%）的材料。基于此，通过不同化学策略构建了几种水溶性且具有生物相容性的近红外二区探针：[具体探针名称1]、[具体探针名称2]和[具体探针名称3]，然后探索了它们在近红外二区用于肿瘤成像和图像引导手术的潜力。被动和主动肿瘤靶向探针[具体探针名称1]和[具体探针名称2]均实现了高水平摄取。此外，首次使用[具体探针名称3]对活体小鼠肿瘤和全身血管进行高分辨率成像，证明了近红外二区图像引导的前哨淋巴结（SLN）手术的精确性。
