Mao Wuyu, Qian Xiana, Zhang Jian, Xia Lingying, Xie Hexin
State Key Laboratory of Bioreactor Engineering, Shanghai Key Laboratory of New Drug Design, School of Pharmacy East China, University of Science and Technology, Shanghai, 200237, P.R. China.
Chembiochem. 2017 Oct 18;18(20):1990-1994. doi: 10.1002/cbic.201700447. Epub 2017 Sep 12.
The dissemination of antimicrobial resistance around the world is one of the biggest threats to global public health. The acquisition and expression of extended-spectrum β-lactamases (ESBLs) in pathogenic bacterial are mainly responsible for bacterial resistance to third-generation cephalosporins. Reported herein is a ratiometric fluorescent probe for the detection of the activity of ESBLs. This imaging reagent adopts the core structure of cefotaxime as an enzymatic recognition moiety, and exhibits excellent selectivity to ESBLs over other β-lactamases. The specific activation of this sensor by ESBLs can lead to over 2500-fold changes in the fluorescent ratio, which is independent of the concentration of the probe and environmental conditions. Further experiments have demonstrated that this ratiometric fluorescent probe can distinguish bacteria with extended-spectrum antibiotic resistance from a group of clinically important pathogens within a short period of time.
抗菌药物耐药性在全球的传播是对全球公共卫生的最大威胁之一。病原菌中广谱β-内酰胺酶（ESBLs）的获得与表达是细菌对第三代头孢菌素耐药的主要原因。本文报道了一种用于检测ESBLs活性的比率荧光探针。该成像试剂采用头孢噻肟的核心结构作为酶识别部分，对ESBLs表现出优于其他β-内酰胺酶的优异选择性。ESBLs对该传感器的特异性激活可导致荧光比率发生超过2500倍的变化，这与探针浓度和环境条件无关。进一步的实验表明，这种比率荧光探针能够在短时间内从一组临床重要病原菌中区分出具有广谱抗生素耐药性的细菌。
