Highly sensitive light-up near-infrared fluorescent probe for detection and imaging of β-glucuronidase in human serum, living cells and tumor-bearing mice

作者：Zhou, Xin; Wang, Deping; Gao, Zhiyuan; He, Mingyue; Hou, Jiayi; Zhang, Hui^*; Zhang, Guoqiang^*; Ding, Dan; Feng, Guangxue^*

来源：Science China-Materials, 2022, 65(3): 836-844.

DOI：10.1007/s40843-021-1779-7

• NIR fluorescent probe
• beta-glucuronidase
• serum detection
• cell imaging
• in-vivo bioimaging

beta-Glucuronidase (GUS) plays a key role in tumor initiation, metastasis, and progression, and thus, has been proposed as a promising cancer biomarker. In this study, we designed an enzyme-activatable near-infrared (NIR) fluorescent probe (DCM-beta GlcA) for the rapid and accurate detection of GUS activity in vitro, in vivo and ex vivo. The DCM-beta GlcA was prepared by linking a glucuronic acid residue to dicyanomethylene-4H-pyran (DCM). This probe exhibited significant light-up NIR fluorescent signals at 680 nm after reacting with GUS and the Stokes shift could reach 150 nm. The DCM-beta GlcA showed a high sensitivity toward GUS and an excellent linear relationship at concentrations ranging between 0 and 4 U L-1 (R-2 = 0.9974) with the limit of detection as low as 0.19 U L-1. We used the DCM-beta GlcA to identify GUS serum levels in both cancer patients and healthy individuals with a similar accuracy as that of an enzyme-linked immunosorbent assay (ELISA) while being easier and faster to perform. Moreover, the DCM-beta GlcA was used for tracking endogenous GUS in living cells, thereby discriminating GUS-overexpressed liver cancer from normal cells. Additionally, the DCM-beta GlcA was able to detect and image endogenous GUS in liver cancer tissue and tumor-bearing mouse models. These findings demonstrate the potential of the DCM-beta GlcA as a promising tool for detecting and monitoring GUS activity in preclinical applications.

• 单位
  南开大学