Uridine diphosphate (UDP)-glucuronosyl-transferases (UGTs) are enzymes involved in the biotransformation of important endogenous compounds such as steroids, bile acids, and hormones as well as exogenous substances including drugs, environmental toxicants, and carcinogens. Here, a novel fluorescent probe BDMP was developed based on boron-dipyrromethene (BODIPY) with high sensitivity for the detection of UGT1A8. The glucuronidation of BDMP not only exhibited a red-emission wavelength (λ_ex/λ_em = 500/580 nm), but also displayed an excellent UGT1A8-dependent fluorescence signal with a good linear relationship with UGT1A8 concentration. Based on this perfect biocompatibility and cell permeability, BDMP was successfully used to image endogenous UGT1A8 in human cancer cell lines (LoVo and HCT15) in real time. In addition, BDMP could also be used to visualize UGT1A8 in tumor tissues. These results suggested that BDMP is a promising molecular tool for the investigation of UGT1A8-mediated physiological function in humans.

尿苷二磷酸 (UDP)-葡萄糖醛酸基转移酶 (UGT) 是参与重要的内源性化合物（如类固醇、胆汁酸和激素）以及外源性物质（包括药物、环境毒物和致癌物）的生物转化的酶。在这里，基于硼-二吡咯亚甲基（BODIPY）开发了一种新型荧光探针BDMP，该探针具有高灵敏度检测UGT1A8。BDMP 的葡萄糖醛酸化不仅表现出红色发射波长 ( λ _ex / λ _em= 500/580 nm），但也显示出优异的 UGT1A8 依赖性荧光信号，与 UGT1A8 浓度具有良好的线性关系。基于这种完美的生物相容性和细胞渗透性，BDMP 成功地用于实时成像人类癌细胞系（LoVo 和 HCT15）中的内源性 UGT1A8。此外，BDMP 还可用于可视化肿瘤组织中的 UGT1A8。这些结果表明，BDMP 是一种很有前途的分子工具，可用于研究 UGT1A8 介导的人体生理功能。