A unique ternary Ce(III)-quercetin-phenanthroline assembly with antioxidant and anti-inflammatory properties.

E Halevas, S Matsia, A Hatzidimitriou, E Geromichalou, T A Papadopoulos, G Katsipis, A Pantazaki, G Litsardakis, A Salifoglou

Journal: Journal of inorganic biochemistry 2022;235():111947

PMID: 35933833

Full Text on Elsevier Science View on PubMed

Abstract

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, (Reactive Oxygen Species, 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.

Address: Laboratory of Inorganic Chemistry and Advanced Materials, School of Chemical Engineering, Aristotle University of Thessaloniki, Thessaloniki 54124, Greece; Laboratory of Materials for Electrotechnics, School of Electrical and Computer Engineering, Aristotle University of Thessaloniki, Thessaloniki 54124, Greece.; Laboratory of Inorganic Chemistry and Advanced Materials, School of Chemical Engineering, Aristotle University of Thessaloniki, Thessaloniki 54124, Greece.; Laboratory of Inorganic Chemistry, School of Chemistry, Aristotle University of Thessaloniki, Thessaloniki 54124, Greece.; Laboratory of Pharmacology, Medical School, National and Kapodistrian University of Athens, Athens 11527, Greece.; Department of Natural Sciences, University of Chester, Thornton Science Park, CH2 4NU Chester, UK.; Laboratory of Biochemistry, School of Chemistry, Aristotle University of Thessaloniki, Thessaloniki 54124, Greece.; Laboratory of Materials for Electrotechnics, School of Electrical and Computer Engineering, Aristotle University of Thessaloniki, Thessaloniki 54124, Greece.; Laboratory of Inorganic Chemistry and Advanced Materials, School of Chemical Engineering, Aristotle University of Thessaloniki, Thessaloniki 54124, Greece. Electronic address: [email protected].

DOI: 10.1016/j.jinorgbio.2022.111947

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MeSH Terms: Anti-Inflammatory Agents, Antioxidants, DNA, Phenanthrolines, Quercetin, Saccharomyces cerevisiae, Spectroscopy, Fourier Transform Infrared