pH-Sensitive Ratiometric Fluorescent Probe for Evaluation of Tumor Treatments

Peisen Zhang; Junli Meng; Yingying Li; Zihua Wang; Yi Hou

doi:10.3390/ma12101632

pH-Sensitive Ratiometric Fluorescent Probe for Evaluation of Tumor Treatments

Materials (Basel). 2019 May 18;12(10):1632. doi: 10.3390/ma12101632.

Authors

Peisen Zhang^{1

2}, Junli Meng^{3

4}, Yingying Li^{5

6}, Zihua Wang⁷, Yi Hou^{8

9}

Affiliations

¹ Key Laboratory of Colloid, Interface and Chemical Thermodynamics, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190, China. zhangps@iccas.ac.cn.
² School of Chemistry and Chemical Engineering, University of Chinese Academy of Sciences, Beijing 100049, China. zhangps@iccas.ac.cn.
³ Key Laboratory of Colloid, Interface and Chemical Thermodynamics, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190, China. mengjl@iccas.ac.cn.
⁴ School of Chemistry and Chemical Engineering, University of Chinese Academy of Sciences, Beijing 100049, China. mengjl@iccas.ac.cn.
⁵ Key Laboratory of Colloid, Interface and Chemical Thermodynamics, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190, China. liyingying@iccas.ac.cn.
⁶ School of Chemistry and Chemical Engineering, University of Chinese Academy of Sciences, Beijing 100049, China. liyingying@iccas.ac.cn.
⁷ Key Laboratory of Colloid, Interface and Chemical Thermodynamics, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190, China. wangzh@iccas.ac.cn.
⁸ Key Laboratory of Colloid, Interface and Chemical Thermodynamics, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190, China. houyi@iccas.ac.cn.
⁹ College of Life Science and Technology, Beijing University of Chemical Technology, Beijing 100029, China. houyi@iccas.ac.cn.

Abstract

Determining therapeutic efficacy is critical for tumor precision theranostics. In order to monitor the efficacy of anti-cancer drugs (e.g., Paclitaxel), a pH-sensitive ratiometric fluorescent imaging probe was constructed. The pH-sensitive ratiometric fluorescent dye ANNA was covalently coupled to the N-terminal of the cell-penetrating TAT peptide through an amidation reaction (TAT-ANNA). The in vitro cellular experiments determined that the TAT-ANNA probe could penetrate the cell membrane and image the intracellular pH in real time. The in vivo experiments were then carried out, and the ratiometric pH response to the state of the tumor was recorded immediately after medication. The TAT-ANNA probe was successfully used to monitor the pharmacodynamics of anti-cancer drugs in vivo.

Keywords: intracellular pH; pharmacodynamic evaluation; ratiometric fluorescence.

Grants and funding

81671754, 81801766, 81530057, 81471726, 81771902, 81720108024/National Natural Science Foundation of China