Towards Novel Photodynamic Anticancer Agents Generating Superoxide Anion Radicals: A Cyclometalated IrIII Complex Conjugated to a Far-Red Emitting Coumarin
Language English Country Germany Media print-electronic
Document type Journal Article, Research Support, Non-U.S. Gov't
Grant support
2017 FI_B 00617, 2018 FI_B1 00174 and 2019 FI_B2 00167
Departament d'Universitats, Recerca i Societat de la Informació - International
2017 DI 072
Departament d'Universitats, Recerca i Societat de la Informació - International
CTQ2015-64319-R
Ministerio de Economía, Industria y Competitividad, Gobierno de España - International
CTQ2017-84779-R
Ministerio de Economía, Industria y Competitividad, Gobierno de España - International
CTQ2014-52658-R
Ministerio de Economía, Industria y Competitividad, Gobierno de España - International
CTQ2016-78454-C2-1-R
Ministerio de Economía, Industria y Competitividad, Gobierno de España - International
18-09502S
Czech Science Foundation - International
R-1034/2016
Universidad de Murcia - International
CTQ2015-64319-R
FEDER funds - International
CTQ2017-84779-R
FEDER funds - International
CTQ2014-52658-R
FEDER funds - International
CTQ2016-78454-C2-1-R
FEDER funds - International
- Keywords
- conjugation, coumarin, cyclometalated iridium(III) complexes, photodynamic therapy, photosensitizer,
- MeSH
- Photochemotherapy MeSH
- HeLa Cells MeSH
- Cell Hypoxia MeSH
- Iridium chemistry MeSH
- Coordination Complexes chemistry pharmacology therapeutic use MeSH
- Coumarins chemistry MeSH
- Humans MeSH
- Neoplasms drug therapy pathology MeSH
- Antineoplastic Agents chemistry pharmacology therapeutic use MeSH
- Superoxides metabolism MeSH
- Light MeSH
- Cell Survival drug effects radiation effects MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- coumarin MeSH Browser
- Iridium MeSH
- Coordination Complexes MeSH
- Coumarins MeSH
- Antineoplastic Agents MeSH
- Superoxides MeSH
Although cyclometalated IrIII complexes have emerged as promising photosensitizers for photodynamic therapy, some key drawbacks still hamper clinical translation, such as operability in the phototherapeutic window and reactive oxygen species (ROS) production efficiency and selectivity. In this work, a cyclometalated IrIII complex conjugated to a far-red-emitting coumarin, IrIII -COUPY, is reported with highly favourable properties for cancer phototherapy. IrIII -COUPY was efficiently taken up by HeLa cells and showed no dark cytotoxicity and impressive photocytotoxicity indexes after irradiation with green and blue light, even under hypoxia. Importantly, a clear correlation between cell death and intracellular generation of superoxide anion radicals after visible light irradiation was demonstrated. This strategy opens the door to novel fluorescent photodynamic therapy agents with promising applications in theragnosis.
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