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Cancer-Specific hNQO1-Responsive Biocompatible Naphthalimides Providing a Rapid Fluorescent Turn-On with an Enhanced Enzyme Affinityopen access

Authors
Park, Sun YoungJung, EugeineKim, Jong SeungChi, Sung-GilLee, Min Hee
Issue Date
Jan-2020
Publisher
MDPI
Keywords
human NAD(P)H:quinone oxidoreductase 1 (hNQO1); fluorescent off-on naphthalimides; trimethyl lock quinone; triphenylphosphonium salt
Citation
SENSORS, v.20, no.1
Journal Title
SENSORS
Volume
20
Number
1
URI
https://scholarworks.sookmyung.ac.kr/handle/2020.sw.sookmyung/2556
DOI
10.3390/s20010053
ISSN
1424-8220
Abstract
Human NAD(P)H:quinone oxidoreductase 1 (hNQO1) is overexpressed in cancer cells and associated with the drug resistance factor of cancer. The objective of this work is the development of fluorescent probes for the efficient detection of hNQO1 activity in cancer cells, which can be employed for the cancer diagnosis and therapeutic agent development. Herein, we report naphthalimide-based fluorescent probes 1 and 2 that can detect hNQO1. For hNQO1 activity, the probes showed a significant fluorescence increase at 540 nm. In addition, probe 1, the naphthalimide containing a triphenylphosphonium salt, showed an enhanced enzyme efficiency and rapid detection under a physiological condition. The detection ability of probe 1 was superior to that of other previously reported probes. Moreover, probe 1 was less cytotoxic during the cancer cell imaging and readily provided a strong fluorescence in hNQO1-overexpressed cancer cells (A549). We proposed that probe 1 can be used to detect hNQO1 expression in live cells and it will be applied to develop the diagnosis and customized treatment of hNQO1-related disease.
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