Premium
Understanding the Potential In Vitro Modes of Action of Bis(β‐diketonato) Oxovanadium(IV) Complexes
Author(s) -
Sergi Baris,
Bulut Ipek,
Xia Ying,
Waller Zoë A. E.,
Yildizhan Yasemin,
Acilan Ceyda,
Lord Rianne M.
Publication year - 2021
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.202100152
Subject(s) - förster resonance energy transfer , dna , chemistry , intercalation (chemistry) , dna damage , in vitro , comet assay , apoptosis , microbiology and biotechnology , cleavage (geology) , cell culture , base pair , biophysics , fluorescence , programmed cell death , reactive oxygen species , stereochemistry , biochemistry , biology , genetics , inorganic chemistry , paleontology , physics , quantum mechanics , fracture (geology)
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).