Issue 2, 2019

An enzyme-activatable probe liberating AIEgens: on-site sensing and long-term tracking of β-galactosidase in ovarian cancer cells

Abstract

Development of fluorescent probes for on-site sensing and long-term tracking of specific biomarkers is particularly desirable for the early detection of diseases. However, available small-molecule probes tend to facilely diffuse across the cell membrane or remain at the activation site but always suffer from the aggregation-caused quenching (ACQ) effect. Here we report an enzyme-activatable aggregation-induced emission (AIE) probe QM–βgal, which is composed of a hydrophilic β-galactosidase (β-gal)-triggered galactose moiety and a hydrophobic AIE-active fluorophore QM–OH. The probe is virtually non-emissive in aqueous media, but when activated by β-gal, specific enzymatic turnover would liberate hydrophobic AIE luminogen (AIEgen) QM–OH, and then highly fluorescent nanoaggregates are in situ generated as a result of the AIE process, allowing for on-site sensing of endogenous β-gal activity in living cells. Notably, taking advantage of the improved intracellular retention of nanoaggregates, we further exemplify QM–βgal for long-term (∼12 h) visualization of β-gal-overexpressing ovarian cancer cells with high fidelity, which is essential for biomedicine and diagnostics. Thus, this enzyme-activatable AIE probe not only is a potent tool for elucidating the roles of β-gal in biological systems, but also offers an enzyme-regulated liberation strategy to exploit multifunctional probes for preclinical applications.

Graphical abstract: An enzyme-activatable probe liberating AIEgens: on-site sensing and long-term tracking of β-galactosidase in ovarian cancer cells

Supplementary files

Article information

Article type
Edge Article
Submitted
25 Sep 2018
Accepted
09 Oct 2018
First published
09 Oct 2018
This article is Open Access

All publication charges for this article have been paid for by the Royal Society of Chemistry
Creative Commons BY-NC license

Chem. Sci., 2019,10, 398-405

An enzyme-activatable probe liberating AIEgens: on-site sensing and long-term tracking of β-galactosidase in ovarian cancer cells

K. Gu, W. Qiu, Z. Guo, C. Yan, S. Zhu, D. Yao, P. Shi, H. Tian and W. Zhu, Chem. Sci., 2019, 10, 398 DOI: 10.1039/C8SC04266G

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