Issue 6, 2023

An AIEgen-based “turn-on” probe for sensing cancer cells and tiny tumors with high furin expression

Abstract

Peptide-aggregation-induced emission (AIE) luminogen (AIEgen) conjugates are widely used in the bioimaging field for their good resistance to photobleaching, red and near-infrared light emission, good biocompatibility, etc. However, their peptides are mainly negatively charged and the positively charged peptide-AIEgen conjugates are rarely used in in vivo imaging due to their high non-specific interaction with protein to cause “false-positive” results and their potential risk of triggering hemolysis. Herein, we introduce a black hole quencher 3 (BHQ3) to RVRRGFF-AIE (FA) to build a “turn-on” probe, named BHQ3-RVRRGFF-AIE (BFA). Compared with FA, BFA has advantages in the anti-interference ability for different proteins and many solution environments. But, both BFA and FA have high risks of inducing hemolysis, which restricts their further application. Through co-assembly with poly-γ-glutamic acid (γ-PGA), molecular probes BFA and FA are formed into PGA-BFA and PGA-FA nanoparticles with high biocompatibility and suppressed phototoxicity. Cell studies show that PGA-BFA can discriminate cancer cells with high furin expression from low furin-expressed cancer cells and normal cells. In vivo studies show that PGA-BFA can light up tiny tumors in the abdominal cavity with a better tumor-to-intestine ratio (3.14) than that of PGA-FA (1.47), which is helpful for the accurate excision of tiny tumors. This study will advance the development of constructing good biosafety probes with a high signal-to-noise ratio for fluorescence image-guided cancer surgery.

Graphical abstract: An AIEgen-based “turn-on” probe for sensing cancer cells and tiny tumors with high furin expression

Supplementary files

Article information

Article type
Paper
Submitted
02 Dec 2022
Accepted
29 Jan 2023
First published
31 Jan 2023

Biomater. Sci., 2023,11, 2221-2229

An AIEgen-based “turn-on” probe for sensing cancer cells and tiny tumors with high furin expression

S. Ji, S. Li, H. Gao, J. Wang, K. Wang, W. Nan, H. Chen and Y. Hao, Biomater. Sci., 2023, 11, 2221 DOI: 10.1039/D2BM01979E

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