Structurally characterized copper-chrysin complexes display genotoxic and cytotoxic activity in human cells

Abstract The scientific interest in the development of novel anticancer metallodrugs with improved clinical efficiency and pharmacological properties based on a variety of metal ions and naturally derived products as biological ligands, is continuous and rising. Herein, we present the synthesis, full structural and physico-chemical characterization of two ternary complex assemblies of Cu(II) with chrysin and the anchillary aromatic chelators 1,10-phenanthroline and 2,2-bipyridine. The complexes constitute the only crystallographically characterized structures with Cu(II) as the metal core and flavonoid chrysin as the ligand. The frequency of sister chromatid exchanges (SCEs) was measured as an indicator of genotoxicity while the proliferation rate index (PRI) and mitotic index (MI) were estimated as indicators of cytostatic effect. In addition, cytotoxicity studies through resazurin assay were employed against two human lung cancer cell lines. Our results indicate significant cytotoxic and genotoxic activity of the novel ternary Cu(II)-chrysin complexes that merit further investigation of their pharmacological profile.