Understanding the Potential In Vitro Modes of Action of Bis(β-diketonato) Oxovanadium(IV) Complexes

To understand the potential in vitro modes of action of bis(beta-diketonato) oxovanadium(IV) complexes, nine compounds of varying functionality have been screened using a range of biological techniques. The antiproliferative activity against a range of cancerous and normal cell lines has been determined, and show these complexes are particularly sensitive against the lung carcinoma cell line, A549. Annexin V (apoptosis) and Caspase-3/7 assays were studied to confirm these complexes induce programmed cell death. While gel electrophoresis was used to determine DNA cleavage activity and production of reactive oxygen species (ROS), the Comet assay was used to determine induced genomic DNA damage. Additionally, Forster resonance energy transfer (FRET)-based DNA melting and fluorescent intercalation displacement assays have been used to determine the interaction of the complexes with double strand (DS) DNA and to establish preferential DNA base-pair binding (AT versus GC).

Automated summary

By screening nine compounds with varying functionality, the in vitro modes of action of bis(beta-diketonato) oxovanadium(IV) complexes were investigated. These complexes showed sensitivity against lung carcinoma cell line A549 and induced programmed cell death and DNA damage. Various biological techniques were employed to study the antiproliferative activity, apoptosis induction, DNA cleavage activity, and DNA base-pair binding preferences of the complexes.