Ratiometric Fluorescence Assay for Nitroreductase Activity: Locked-Flavylium Fluorophore as a NTR-Sensitive Molecular Probe

Su Jung Kim; Jung Won Yoon; Shin A Yoon; Min Hee Lee

doi:10.3390/molecules26041088

Molecules (Feb 2021)

Ratiometric Fluorescence Assay for Nitroreductase Activity: Locked-Flavylium Fluorophore as a NTR-Sensitive Molecular Probe

Su Jung Kim,
Jung Won Yoon,
Shin A Yoon,
Min Hee Lee

Affiliations

Su Jung Kim: Department of Chemistry, Sookmyung Women’s University, Seoul 04310, Korea
Jung Won Yoon: Department of Chemistry, Sookmyung Women’s University, Seoul 04310, Korea
Shin A Yoon: Department of Chemistry, Sookmyung Women’s University, Seoul 04310, Korea
Min Hee Lee: Department of Chemistry, Sookmyung Women’s University, Seoul 04310, Korea

DOI: https://doi.org/10.3390/molecules26041088
Journal volume & issue: Vol. 26, no. 4
p. 1088

Abstract

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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.

Published in Molecules

ISSN: 1420-3049 (Online)
Publisher: MDPI AG
Country of publisher: Switzerland
LCC subjects: Science: Chemistry: Organic chemistry
Website: http://www.mdpi.com/journal/molecules

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