Evaluation of the anticancer activity of a novel naringin-V(IV)O coordination complex in human lung cancer A549 cells.

LUCIANA G. NASO; PATRICIA A.M. WILLIAMS; GONZALEZ, PABLO J.; RESTREPO-GUERRERO, ANDRÉS GONZALO; EVELINA G. FERRER

Mar del Plata

Encuentro; Reunión anual de sociedades de biociencias.; 2023

Coordination complexes ofbioactive compounds often display an enhanced pharmacological profile comparedto the original compound. Their pharmacological effects are influenced byfactors such as the identity and quantity of ligands, the metal atom, itsoxidation state, coordination mode, and geometry. Variations in these factorscan impact properties such as interaction with specific biomolecules, complexstability, solubility, and bioavailability. In a previous study, we prepared twocoordination complexes derived from the glycosylated flavonoid naringin and theoxidovanadium(IV) cation, [VO(Narg)2]·8H2O (VONarg) and[VO(Narg)(Phen)Cl]·3H2O (VONargPh). These complexes exhibitedenhanced biological activity when compared to naringin. The aim of this study wasto modify the coordination site of the oxidovanadium(IV) cation with theflavonoid and assess its anticancer potential against the A549 lung cancer cellline. Physicochemical analysis revealed that the new complex, synthesized at pH= 12, K2[VO(Narg)(H2O)2]·3H2O,coordinates with naringin through the glycosidic region, in contrast to the initialtwo complexes, which coordinate through the 5-C-O- and 4-C=O groups.It demonstrated higher solubility in aqueous media and exhibited a notablereduction in cell viability (42 %) at 100 μM after 24 h. These resultssurpassed the effectiveness of VONarg (20%). Additionally, the treatment led toa 112% increase in the production of reactive oxygen species after 4 h ofincubation. Furthermore, the levels of the endogenous antioxidant glutathionedecreased by 46%, and the mitochondrial membrane potential reduced 12 % incomparison to the control. Moreover, alterations in cellular morphologyindicated a loss of cytoplasm and the formation of apoptotic bodies. Thesefindings collectively point to the potential of this complex as an effectiveagent against cancer cells by inducing oxidative stress (to which cancer cellsare more susceptible) and triggering apoptosis.