Antiproliferative and Cytotoxic Activities of Fluorescein-A Diagnostic Angiography Dye

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Authors

ŠRANKOVÁ Mária DVOŘÁK Aleš MARTÍNEK Marek ŠEBEJ Peter KLÁN Petr VÍTEK Libor MUCHOVÁ Lucie

Year of publication 2022
Type Article in Periodical
Magazine / Source International Journal of Molecular Sciences
MU Faculty or unit

Faculty of Science

Citation
Web https://www.mdpi.com/1422-0067/23/3/1504
Doi http://dx.doi.org/10.3390/ijms23031504
Keywords fluorescein; irradiation; singlet oxygen; carbon monoxide; viability; metabolism; proliferation
Attached files
Description Fluorescein is a fluorescent dye used as a diagnostic tool in various fields of medicine. Although fluorescein itself possesses low toxicity, after photoactivation, it releases potentially toxic molecules, such as singlet oxygen (O-1(2)) and, as we demonstrate in this work, also carbon monoxide (CO). As both of these molecules can affect physiological processes, the main aim of this study was to explore the potential biological impacts of fluorescein photochemistry. In our in vitro study in a human hepatoblastoma HepG2 cell line, we explored the possible effects on cell viability, cellular energy metabolism, and the cell cycle. We observed markedly lowered cell viability (approximate to 30%, 75-2400 mu M) upon irradiation of intracellular fluorescein and proved that this decrease in viability was dependent on the cellular oxygen concentration. We also detected a significantly decreased concentration of Krebs cycle metabolites (lactate and citrate < 30%; 2-hydroxyglutarate and 2-oxoglutarate < 10%) as well as cell cycle arrest (decrease in the G2 phase of 18%). These observations suggest that this photochemical reaction could have important biological consequences and may account for some adverse reactions observed in fluorescein-treated patients. Additionally, the biological activities of both O-1(2) and CO might have considerable therapeutic potential, particularly in the treatment of cancer.
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