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

Sergi, B; Bulut, I; Xia, Y; Waller, ZAE; Yildizhan, Y; Acilan, C; Lord, RM; (2021) Understanding the Potential In Vitro Modes of Action of Bis(beta-diketonato) Oxovanadium(IV) Complexes. ChemMedChem 10.1002/cmdc.202100152. (In press). Green open access

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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).

Type: Article
Title: Understanding the Potential In Vitro Modes of Action of Bis(beta-diketonato) Oxovanadium(IV) Complexes
Open access status: An open access version is available from UCL Discovery
DOI: 10.1002/cmdc.202100152
Publisher version: https://doi.org/10.1002/cmdc.202100152
Language: English
Additional information: © 2021 The Authors. ChemMedChem published by Wiley-VCH GmbH. This is an open access article under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/).
Keywords: Apoptosis, &#946, -diketonate complexes, Bioinorganic Chemistry, DNA interactions, Vanadium complexes
UCL classification: UCL
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy > Pharma and Bio Chemistry
URI: https://discovery.ucl.ac.uk/id/eprint/10129240
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