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Issue 6, 2019

In situ imaging of aminopeptidase N activity in hepatocellular carcinoma: a migration model for tumour using an activatable two-photon NIR fluorescent probe

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Abstract

CD13/aminopeptidase N (APN), which is a zinc-dependent metalloproteinase, plays a vital role in the growth, migration, angiogenesis, and metastasis of tumours. Thus, in situ molecular imaging of endogenous APN levels is considerably significant for investigating APN and its different functions. In this study, a novel two-photon near-infrared (NIR) fluorescence probe DCM-APN was prepared to perform in vitro and in vivo tracking of APN. The N-terminal alanyl site of probe DCM-APN was accurately hydrolysed to the amino group, thereby liberating strong fluorescence owing to the recovery of the Intramolecular Charge Transfer (ICT) effect. By considering its outstanding selectivity, ultra-sensitivity (DL 0.25 ng mL−1) and favourable biocompatibility, the probe DCM-APN was used to distinguish between normal cells (LO2 cells) and cancer cells (HepG-2 and B16/BL6 cells). Furthermore, migration of hepatocellular carcinoma cells was apparently inhibited by ensuring that the APN catalytic cavity was occupied by bestatin. The identification of three-dimensional (3D) fluorescence in cancer tissues was completed under two-photon excitation coupled with lighting up hepatocellular carcinoma tumours in situ; this revealed that probe DCM-APN is an effective tool for detecting APN, thereby assisting in the early diagnosis of tumour in clinical medicine.

Graphical abstract: In situ imaging of aminopeptidase N activity in hepatocellular carcinoma: a migration model for tumour using an activatable two-photon NIR fluorescent probe

Supplementary files

Article information


Submitted
21 Oct 2018
Accepted
25 Nov 2018
First published
27 Nov 2018

This article is Open Access
All publication charges for this article have been paid for by the Royal Society of Chemistry

Chem. Sci., 2019,10, 1619-1625
Article type
Edge Article

In situ imaging of aminopeptidase N activity in hepatocellular carcinoma: a migration model for tumour using an activatable two-photon NIR fluorescent probe

H. Li, Y. Li, Q. Yao, J. Fan, W. Sun, S. Long, K. Shao, J. Du, J. Wang and X. Peng, Chem. Sci., 2019, 10, 1619 DOI: 10.1039/C8SC04685A

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