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A unique ternary Ce(III)-quercetin-phenanthroline assembly with antioxidant and anti-inflammatory properties
Halevas, Eleftherios ; Matsia, Sevasti ; Hatzidimitriou, Antonios ; Geromichalou, Elena ; Papadopoulos, Theodoros A. ; Katsipis, Georgios ; Pantazaki, Anastasia ; Litsardakis, George ; Salifoglou, Athanasios
Halevas, Eleftherios
Matsia, Sevasti
Hatzidimitriou, Antonios
Geromichalou, Elena
Papadopoulos, Theodoros A.
Katsipis, Georgios
Pantazaki, Anastasia
Litsardakis, George
Salifoglou, Athanasios
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2022-06-30
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Quercetin is one of the most bioactive and common dietary flavonoids, with a significant repertoire of biological and pharmacological properties. The biological activity of quercetin, however, is influenced by its limited solubility and bioavailability. Driven by the need to enhance quercetin bioavailability and bioactivity through metal ion complexation, synthetic efforts led to a unique ternary Ce(III)-quercetin-(1,10-phenanthroline) ( 1 ) compound. Physicochemical characterization (elemental analysis, FT-IR, Thermogravimetric analysis (TGA), UV-Visible, NMR, Electron Spray Ionization-Mass Spectrometry (ESI-MS), Fluorescence, X-rays) revealed its solid-state and solution properties, with significant information emanating from the coordination sphere composition of Ce(III). The experimental data justified further entry of 1 in biological studies involving toxicity, ROS-suppressing potential, cell metabolism inhibition in Saccharomyces cerevisiae (S. cerevisiae) cultures, and plasmid DNA degradation. DFT calculations revealed its electronic structure profile, with in silico studies showing binding to DNA, DNA gyrase, and glutathione S-transferase, thus providing useful complementary insight into the elucidation of the mechanism of action of 1 at the molecular level and interpretation of its bio-activity. The collective work projects the importance of physicochemically supported bio-activity profile of well-defined Ce(III)-flavonoid compounds, thereby justifying focused pursuit of new hybrid metal-organic materials, effectively enhancing the role of naturally-occurring flavonoids in physiology and disease.
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Halevas, E., Matsia, S., Hatzidimitriou, A. G., Geromichalou, E., Papadopoulos, T. A., Katsipis, G., Pantazaki, A., Litsardakis, G., & Salifoglou, A, A unique ternary Ce(III)-quercetin-phenanthroline assembly with antioxidant and anti-inflammatory properties. Available at SSRN: https://ssrn.com/abstract=4143265 or http://dx.doi.org/10.2139/ssrn.4143265
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S.M. would like to acknowledge support of this research by the State Scholarships Foundation (IΚΥ) for the doctoral scholarship co-financed by Greece and the European Union (European Social Fund - ESF) through the Operational Program “Human Resources Development, Education and Lifelong Learning” (NSRF 2014-2020), Act: “Strengthening the Human Research Resources through the Implementation of Doctoral Research” - MIS 5000432.
T.P. gratefully acknowledges use of Cirrus UK National Tier-2 HPC Service at EPCC, Edinburgh, under EPSRC grant EP/P020267/1.
