Abstract
Nitroreductases belong to a member of flavin-containing enzymes that can reduce nitroaromatic compounds to amino derivatives with NADH as an electron donor. NTR activity is known to be elevated in the cancerous environment and is considered an advantageous target in therapeutic prodrugs for the treatment of cancer. Here, we developed a ratiometric fluorescent molecule for observing NTR activity in living cells. This can provide a selective and sensitive response to NTR with a distinct increase in fluorescence ratio (FI530/FI630) as well as color changes. We also found a significant increase in NTR activity in cervical cancer HeLa and lung cancer A549 cells compared to non-cancerous NIH3T3. We proposed that this new ratiometric fluorescent molecule could potentially be used as a NTR-sensitive molecular probe in the field of cancer diagnosis and treatment development related to NTR activity.
Highlights
Nitroreductases (NTR) are flavoenzymes that catalyze the reduction of nitroaromatic compounds to amines using NADH as an electron donor [1,2]
Probe 1 was devised based on a locked-flavylium fluorophore skeleton with a nitro group sensitive to NTR activity
The flavylium fluorophore was chosen because it can display a ratiometric fluorescence response based on an internal charge transfer (ICT) process
Summary
Nitroreductases (NTR) are flavoenzymes that catalyze the reduction of nitroaromatic compounds to amines using NADH as an electron donor [1,2]. NTR activity is important as a therapeutic target for biological detoxification of nitroaromatic compounds and related diseases [3]. A method capable of the accurate and spatiotemporal detection of NTR-mediated enzyme reaction in the human live cells is an important key technology for the development of theranostics. We have used several analytical tools for the detection of NTR, such as nuclear magnetic resonance (NMR), electron paramagnetic resonance (EPR), Clark electrode [7,8,9]. These are limited to a spatiotemporal detection of enzyme reactions in the human live cells
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