A highly selective near infrared fluorescent probe for carboxylesterase 2 and its biological applications

• Published in: Journal of materials chemistry. B, Materials for biology and medicine Materials for biology and medicine, 2021-03, Vol.9 (1), p.2457-2461
• Main Authors: Zhang, Xin-Yue, Liu, Tian-Tian, Liang, Jia-Hao, Tian, Xiang-Ge, Zhang, Bao-Jing, Huang, Hui-Lian, Ma, Xiao-Chi, Feng, Lei, Sun, Cheng-Peng
• Format: Article
• Language: English
• Subjects: Carboxylesterase; Colorectal carcinoma; Fluorescent indicators; Health services; Herbal medicine; High-throughput screening; Inhibitors; Irinotecan; Medical treatment; Selectivity
• ISSN: 2050-750X; 2050-7518
• DOI: 10.1039/d0tb02673e

Carboxylesterase 2 (CES 2) is a key enzyme in the activation of the prodrug irinotecan (CPT-11) in the treatment against colorectal cancer and also has some relationship with the side effect of CPT-11 in clinical applications. Herein, a near infrared (NIR) fluorescent probe ( DSAB ) has been designed for CES 2 which possesses the advantages of prominent selectivity and high sensitivity, and DSAB has been successfully applied for the imaging of endogenous CES 2 in living cells. Moreover, a high-throughput screening method for CES 2 inhibitors has been established using DSAB and discovered four novel CES 2 inhibitors from various herbal medicines. These results fully demonstrated that DSAB is a promising molecular tool for the investigation of the biological functions of CES 2 in living systems and the discovery of novel CES 2 inhibitors for the treatment of CES 2 related physiological diseases. Carboxylesterase 2 (CES 2) is a key enzyme in the activation of the prodrug irinotecan (CPT-11) in the treatment against colorectal cancer and also has some relationship with the side effect of CPT-11 in clinical applications.