In Vitro and In Vivo Biological Activities of Dipicolinate Oxovanadium(IV) Complexes

The work is focused on anticancer properties of dipicolinate(dipic)-basedvanadium(IV) complexes [VO(dipic)((NN)-N-boolean AND)] bearingdifferent diimines (2-(1H-imidazol-2-yl)pyridine,2-(2-pyridyl)benzimidazole, 1,10-phenanthroline-5,6-dione, 1,10-phenanthroline,and 2,2 '-bipyridine), as well as differently 4,7-substituted1,10-phenanthrolines. The antiproliferative effect of V(IV) systemswas analyzed in different tumors (A2780, HCT116, and HCT116-DoxR)and normal (primary human dermal fibroblasts) cell lines, revealinga high cytotoxic effect of [VO(dipic)((NN)-N-boolean AND)] with4,7-dimethoxy-phen (5), 4,7-diphenyl-phen (6), and 1,10-phenanthroline (8) against HCT116-DoxR cells.The cytotoxicity differences between these complexes can be correlatedwith their different internalization by HCT116-DoxR cells. Worthyof note, these three complexes were found to (i) induce cell deaththrough apoptosis and autophagy pathways, namely, through ROS production;(ii) not to be cytostatic; (iii) to interact with the BSA protein;(iv) do not promote tumor cell migration or a pro-angiogenic capability;(v) show a slight in vivo anti-angiogenic capability,and (vi) do not show in vivo toxicity in a chickenembryo.

Automated summary

The study focused on the anticancer properties of dipicolinate-basedvanadium(IV) complexes with different diimines. These complexes showed high cytotoxic effect against HCT116-DoxR cells and induced cell death through apoptosis and autophagy pathways. They also interacted with BSA protein and did not promote tumor cell migration or angiogenesis.