Top Med Chem (2020) 34: 185–202
DOI: 10.1007/7355_2019_87
© Springer Nature Switzerland AG 2019
Published online: 14 January 2020
Fluorescent Probes for Diagnostics
of β-Galactosidase: From Micro to Macro
Anyao Bi, Xinchen Jiang, Tang Gao, Shuqi Yang, Yi Liu, Xiaohui Liu,
and Wenbin Zeng
Contents
1 Introduction . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 186
2 Fluorescent Probe for β-Galactosidase Activity Detection . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 186
2.1 Fluorescent Probe Based on Coumarins, Fluoresceins, and Rhodamines . . . . . . . . . . . 186
2.2 NIR Fluorescent Probe . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 188
2.3 ESIPT and AIE Fluorescent Probes . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 189
3 Nanomaterial for β-Galactosidase Activity Detection . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 193
3.1 Thiolated Copper Nanoclusters (CuNCs) and Silica Nanoclusters . . . . . . . . . . . . . . . . . . 194
3.2 Carbon Quantum Dots . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 196
4 Targeted Fluorescent Probes for β-Galactosidase Detection . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 197
5 Conclusion and Prospective . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 197
References . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 199
Abstract β-Galactosidase (β-gal) is an enzyme commonly served as a reporter
for the examination of transcription and transfection efficiencies. Due to its
overexpression in primary and metastatic ovarian cancers, β-gal was also usually
regarded as a molecular target for visualizing peritoneal metastases from ovarian
cancers. Moreover, β-gal has been studied as a potential therapeutic target for lactose
intolerance via gene replacement therapy in recent years. Interestingly, there were
some reports that β-gal has been abnormally accumulated in senescent cells, which
allowing this senescence-associated β-gal to be a significant biomarker for senescence. The great significance of β-gal has attracted many researchers’ attentions in
developing highly selective and sensitive approaches to monitor the activity of this
enzyme in vitro and in vivo. In this review, we reported the recent development of
the various materials for β-gal detection and their application in disease progression
monitoring, with a focus on fluorescent probe, nanomaterials, and biomolecules.
Finally, the trends for the further development of the probe for fluorescence-guided
diagnosis in clinical cases and its preclinical potential value were proposed.
A. Bi, X. Jiang, T. Gao, S. Yang, Y. Liu, X. Liu, and W. Zeng (*)
Xiangya School of Pharmaceutical Sciences, Central South University, Changsha, China
Molecular Imaging Research Center, Central South University, Changsha, China
DOI: 10.1007/7355_2019_87
© Springer Nature Switzerland AG 2019
Published online: 14 January 2020
Fluorescent Probes for Diagnostics
of β-Galactosidase: From Micro to Macro
Anyao Bi, Xinchen Jiang, Tang Gao, Shuqi Yang, Yi Liu, Xiaohui Liu,
and Wenbin Zeng
Contents
1 Introduction . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 186
2 Fluorescent Probe for β-Galactosidase Activity Detection . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 186
2.1 Fluorescent Probe Based on Coumarins, Fluoresceins, and Rhodamines . . . . . . . . . . . 186
2.2 NIR Fluorescent Probe . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 188
2.3 ESIPT and AIE Fluorescent Probes . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 189
3 Nanomaterial for β-Galactosidase Activity Detection . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 193
3.1 Thiolated Copper Nanoclusters (CuNCs) and Silica Nanoclusters . . . . . . . . . . . . . . . . . . 194
3.2 Carbon Quantum Dots . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 196
4 Targeted Fluorescent Probes for β-Galactosidase Detection . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 197
5 Conclusion and Prospective . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 197
References . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 199
Abstract β-Galactosidase (β-gal) is an enzyme commonly served as a reporter
for the examination of transcription and transfection efficiencies. Due to its
overexpression in primary and metastatic ovarian cancers, β-gal was also usually
regarded as a molecular target for visualizing peritoneal metastases from ovarian
cancers. Moreover, β-gal has been studied as a potential therapeutic target for lactose
intolerance via gene replacement therapy in recent years. Interestingly, there were
some reports that β-gal has been abnormally accumulated in senescent cells, which
allowing this senescence-associated β-gal to be a significant biomarker for senescence. The great significance of β-gal has attracted many researchers’ attentions in
developing highly selective and sensitive approaches to monitor the activity of this
enzyme in vitro and in vivo. In this review, we reported the recent development of
the various materials for β-gal detection and their application in disease progression
monitoring, with a focus on fluorescent probe, nanomaterials, and biomolecules.
Finally, the trends for the further development of the probe for fluorescence-guided
diagnosis in clinical cases and its preclinical potential value were proposed.
A. Bi, X. Jiang, T. Gao, S. Yang, Y. Liu, X. Liu, and W. Zeng (*)
Xiangya School of Pharmaceutical Sciences, Central South University, Changsha, China
Molecular Imaging Research Center, Central South University, Changsha, China
