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Cancer-Specific Biomarker hNQO1-Activatable Fluorescent Probe for Imaging Cancer Cells In Vitro and In Vivo
摘要： Human NAD(P)H quinone oxidoreductase-1 (hNQO1) is an important cancer-related biomarker, which shows significant overexpression in malignant cells. Developing an effective method for detecting NQO1 activity with high sensitivity and selectivity in tumors holds a great potential for cancer diagnosis, treatment, and management. In the present study, we report a new dicyanoisophorone (DCP) based fluorescent probe (NQ-DCP) capable of monitoring hNQO1 activity in vitro and in vivo in both ratiometric and turn-on model. NQ-DCP was prepared by conjugating dicyanoisophorone fluoroprobe with hNQO1 activatable quinone propionic acid (QPA), which remain non-fluorescent until activation by tumor-specific hNQO1. NQ-DCP featured a large Stokes shift (145 nm), excellent biocompatibility, cell permeability, and selectivity towards hNQO1 allowed to differentiate cancer cells from healthy cells. We have successfully employed NQ-DCP to monitor non-invasive endogenous hNQO1 activity in brain tumor cells in vitro and in xenografted tumors developed in nude mice.
关键词： NAD(P)H quinone oxidoreductase 1,cancer biomarker,tumor diagnosis,fluorescent probe,cancer imaging,large Stokes shift,dicyanoisophorone
更新于2025-09-19 17:15:36
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A near-infrared fluorescent probe based on SNAr reaction for H2S/GSH detection in living cells and zebrafish
摘要： Hydrogen sulfide (H2S) and biothiols such as cysteine (Cys), homocysteine (Hcy) and glutathione (GSH), play critical roles in physiological and pathological processes. However, due to the challenge in sensing H2S and biothiols simultaneously, it is of great importance to solve this problem in biological processes. Herein, a near-infrared fluorescent probe (HZ-NBD) based on SNAr reactions was exploited to achieve the sensitive and selective detection of H2S and glutathione (GSH) simultaneously in the same conditions. The design strategy was employing dicyanoisophorone based fluorescent dye as the fluorophore, the NBD moiety as a response unit and a quencher of fluorophore. The probe exhibited a low limit of detection to H2S (13.2 nM) and GSH (112 nM) as well as a favorable large stokes shift (112 nm). The reaction mechanism was investigated via mass spectra. What’s more, owing to the advantages of low cytotoxicity, fast response and strong anti-interference ability, the probe HZ-NBD was successfully applied to bioimage H2S and GSH in HepG2 cells and zebrafish.
关键词： fluorescent probe,SNAr,dicyanoisophorone,near-infrared emission
更新于2025-09-10 09:29:36
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Dicyanoisophorone-Based Near-Infrared Emission Fluorescent Probe for Detecting NAD(P)H in Living Cells and <i>in Vivo</i>
摘要： NADH and NADPH are ubiquitous coenzymes in all living cells and play vital roles in numerous redox reactions in cellular energy metabolism. To accurately detect the distribution and dynamic changes of NAD(P)H under physiological condition is essential for understanding its biological functions and pathological roles. In this work, we developed a near-infrared (NIR) emission fluorescent small-molecule probe (DCI-MQ) composed of a dicyanoisophorone chromophore conjugated with a quinolinium moiety for in vivo NAD(P)H detection. DCI-MQ owns the advantages of high water solubility, rapid response, extraordinary selectivity, great sensitivity (detection limit of 12 nM), low cytotoxicity and a NIR emission (660 nm) in response to NAD(P)H. Moreover, the probe DCI-MQ was successfully applied for the detection and imaging of endogenous NAD(P)H in both living cells and tumor-bearing mice, which provides an effective tool for the study of NAD(P)H-related physiological and pathological processes.
关键词： NAD(P)H,near-infrared emission,fluorescent probe,bioimaging,dicyanoisophorone
更新于2025-09-04 15:30:14