Phenanthroline complexation enhances the cytotoxic activity of the VO-chrysin system.

A. ACTIS DATO; NASO, LUCIANA G.; REY, MARILIN; GONZÁLEZ, P.J.; E.G. FERRER; P.A.M. WILLIAMS

Inorganics

MPDI

Año: 2022

Metal complexation in general improves the biological properties of ligands. We havepreviously measured the anticancer effects of the oxidovanadium(IV) cation with chrysin complex,VO(chrys)2. In the present study, we synthesized and characterized a new complex generated bythe replacement of one chrysin ligand by phenanthroline (phen), VO(chrys)phenCl, to confer highplanarity for DNA chain intercalation and more lipophilicity, giving rise to a better cellular uptake.In effect, the uptake of vanadium has been increased in the complex with phen and the cytotoxiceffect of this complex proved higher in the human lung cancer A549 cell line, being involved inits mechanisms of action, the production of cellular reactive oxygen species (ROS), the decrease ofthe natural antioxidant compound glutathione (GSH) and the ratio GSH/GSSG (GSSG, oxidizedGSH), and mitochondrial membrane damage. Cytotoxic activity studies using the non-tumorigenicHEK293 cell line showed that [VO(chrys)phenCl] exhibits selectivity action towards A549 cells after24 h incubation. The interaction with bovine serum albumin (BSA) by fluorometric determinationsshowed that the complex could be carried by the protein and that the binding of the complex to BSAoccurs through H-bond and van der Waals interactions.