Understanding the potential in vitro modes of action of bis(β‐diketonato) oxovanadium(IV) complexes

Baris Sergi, Ipek Bulut, Ying Xia, Zoë A. E. Waller, Yasemin Yildizhan, Ceyda Acilan, Rianne M. Lord

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Abstract

To understand the potential in vitro modes of action of bis(β-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, Förster 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).

Original languageEnglish
Pages (from-to)2402-2410
Number of pages9
JournalChemMedChem
Volume16
Issue number15
Early online date15 Apr 2021
DOIs
Publication statusPublished - 5 Aug 2021

Keywords

  • Apoptosis
  • Bioinorganic Chemistry
  • DNA interactions
  • Vanadium complexes
  • β-diketonate complexes

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