A Reversible Fluorescent Probe for Real‐Time Quantitative Monitoring of Cellular Glutathione

• Published in: Angewandte Chemie International Edition Vol. 56; no. 21; pp. 5812 - 5816
• Main Authors: Liu, Zhixue, Zhou, Xin, Miao, Yu, Hu, Ying, Kwon, Nahyun, Wu, Xue, Yoon, Juyoung
• Format: Journal Article
• Language: English
• Published: WEINHEIM Wiley 15.05.2017; Wiley Subscription Services, Inc
• Edition: International ed. in English
• Subjects: antioxidants; Chemistry; Chemistry, Multidisciplinary; Cytotoxicity; Fluorescence; Fluorescent indicators; fluorescent probes; Glutathione; gluthionine; Monitoring; Physical Sciences; ratiometric probes; redox homeostasis; Response time; Science & Technology; Toxicity; CELLS; antioxidants; ASSISTED ELECTROSTATIC ATTRACTION; CYSTEINE; SENSOR; redox homeostasis; fluorescent probes; gluthionine; MICHAEL ADDITION; THIOLS; IN-VIVO; EMISSION CHANNELS; ratiometric probes; SELECTIVE DETECTION; GSH
• ISSN: 1433-7851; 1521-3773; 1521-3773
• DOI: 10.1002/anie.201702114

The ability to monitor and quantify glutathione (GSH) in live cells is essential in order to gain a detailed understanding of GSH‐related pathological events. However, owing to their irreversible response mechanisms, most existing fluorescent GSH probes are not suitable for this purpose. We have developed a ratiometric fluorescent probe (QG‐1) for quantitatively monitoring cellular GSH. The probe responds specifically and reversibility to GSH with an ideal dissociation constant (Kd) of 2.59 mm and a fast response time (t1/2=5.82 s). We also demonstrate that QG‐1 detection of GSH is feasible in a model protein system. QG‐1 was found to have extremely low cytotoxicity and was applied to determine the GSH concentration in live HeLa cells (5.40±0.87 mm). Given the green light: A ratiometric fluorescent probe (QG‐1) for monitoring and quantifying variations in cellular glutathione (GSH) was developed. The probe shows a fluorescence shift from red to green upon binding GSH and exhibits specificity and reversibility, with an appropriate dissociation constant for sensing species with high cellular abundance (Kd=2.59 mm) and a fast response time (t1/2=5.82 s).