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

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).

Enhanced selectivity towards melanoma cells with zinc(ii)-Schiff bases containing imidazole derivatives

“…The procedures outlined in a previous publication were adhered to, with slight modifications. 49 In brief, plasmid DNA (200 ng, pBOS-H2B-GFP, BD Biosciences) underwent an overnight incubation at room temperature in the presence of compounds Zn(L 1 ) 2 , Zn(L 2 ) 2 , HL 1 , HL 2 and cisplatin (100–400 μM, in 20 μL). For the evaluation of ROS scavenging activity, NaN 3 (final concentration 37.5 mM in MQ H 2 O) was introduced.…”

Dual LSD1 and HDAC6 Inhibition Induces Doxorubicin Sensitivity in Acute Myeloid Leukemia Cells

“…Activation was assessed by Muse Oxidative Stress Kit (Merck Millipore, Burlington, MA, USA, MCH100111) with a similar protocol, which was previously described in [ 18 ]. Briefly, treated cells were centrifuged (300× g , 5 min), resuspended with 1 × Assay Buffer (MCH100111-2), and mixed with Oxidative Stress Reagent (4700-1665) in 1:100 ratio.…”

Water-soluble copper pyrithione complexes with cytotoxic and antibacterial activity

“…In vitro human cell line cytotoxicity data Metal complexes have been long been explored for their potential anticancer activity. [25][26][27] For the novel copper complexes, antiproliferation studies were carried out against MIA PaCa-2 pancreatic carcinoma cells, 143B bone osteosarcoma cells and normal ARPE-19 retinal epithelial cells, using MTT assay over the course of 24 h. [Cu(PyS) 2 ] and the three novel copper(II) complexes were screened alongside the known anticancer drug cisplatin and CuCl 2 as a reference. The inhibitory concentration (IC 50 ) values of the three PEG-substituted complexes are in the sub-micromolar range and are comparable with that of the parent [Cu(PyS) 2 ] complex (Table 2).…”