Artículo
Phenanthroline Complexation Enhances the Cytotoxic Activity of the VO-Chrysin System
Actis Dato, Agustín Bruno
; Naso, Luciana Gissella
; Rey, Marilin de Los Angeles; González, Pablo Javier
; Ferrer, Evelina Gloria
; Williams, Patricia Ana María
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Fecha de publicación:
12/2021
Editorial:
MDPI
Revista:
Inorganics
ISSN:
2304-6740
Idioma:
Inglés
Tipo de recurso:
Artículo publicado
Clasificación temática:
Resumen
Metal complexation in general improves the biological properties of ligands. We have previously 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 by the replacement of one chrysin ligand by phenanthroline (phen), VO(chrys)phenCl, to confer high planarity 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 cytotoxic effect of this complex proved higher in the human lung cancer A549 cell line, being involved in its mechanisms of action, the production of cellular reactive oxygen species (ROS), the decrease of the natural antioxidant compound glutathione (GSH) and the ratio GSH/GSSG (GSSG, oxidized GSH), and mitochondrial membrane damage. Cytotoxic activity studies using the non-tumorigenic HEK293 cell line showed that [VO(chrys)phenCl] exhibits selectivity action towards A549 cells after 24 h incubation. The interaction with bovine serum albumin (BSA) by fluorometric determinations showed that the complex could be carried by the protein and that the binding of the complex to BSA occurs through H-bond and van der Waals interactions.
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Articulos(CCT - SANTA FE)
Articulos de CTRO.CIENTIFICO TECNOL.CONICET - SANTA FE
Articulos de CTRO.CIENTIFICO TECNOL.CONICET - SANTA FE
Articulos(CEQUINOR)
Articulos de CENTRO DE QUIMICA INORGANICA "DR. PEDRO J. AYMONINO"
Articulos de CENTRO DE QUIMICA INORGANICA "DR. PEDRO J. AYMONINO"
Citación
Actis Dato, Agustín Bruno; Naso, Luciana Gissella; Rey, Marilin de Los Angeles; González, Pablo Javier; Ferrer, Evelina Gloria; et al.; Phenanthroline Complexation Enhances the Cytotoxic Activity of the VO-Chrysin System; MDPI; Inorganics; 10; 1; 12-2021; 1-16
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