New insights into the mechanism of action of ebselen, a small-molecule antivirulence agent that reduces disease pathology in a mouse model of Clostridium difficile infection, suggest a different molecular target may be responsible for its efficacy.

The interaction of the novel antioxidant drug ebselen, 2-phenyl-1,2 benzisoselenazol-3 (2H)one, with human serum albumin (HSA) was investigated by spectrophotometry. 6.7 mM, pH 7.4 of phosphate buffer containing 0.4 % (v / v) dimethylformamide (DMF) was used as the solvent. Various amounts of ebselen and HSA mixtures were used. Incubations of the mixtures were performed for 15 minutes at 25°C a...

Low molecular weight seleno-organic compounds exhibit glutathione peroxidase (GPx)-like activity; the well-known compound ebselen is being used in clinical trials as a stroke medication. Here, we describe the facile one-step synthesis of novel 5-selenized salicylic acid derivatives using selenium tetrachloride. The products were analyzed by spectroscopic studies including (77)Se-NMR and some we...

The main protease (Mpro) of SARS-CoV-2 is a current target for the inhibition viral replication. Through combined Docking and Density Functional Theory (DFT) approach, we investigated in-silico molecular mechanism by which ebselen (IUPAC: 2-phenyl-1,2-benzoselenazol-3-one), most famous pharmacologically active organoselenide, inhibits Mpro. For first time, report on mechanistic investigation in...

Contracting skeletal muscle produces reactive oxygen species (ROS) that have been shown to affect muscle function and adaptation. However, real-time measurement of ROS in contracting myofibers has proven to be difficult. We used amphibian (Xenopus laevis) muscle to test the hypothesis that ROS are formed during contractile activity in isolated single skeletal muscle fibers and that this contrac...

JMJD2A, a 2-oxoglutarate dependent N(epsilon)-methyl lysine histone demethylase, is inhibited by disruption of its Zn-binding site by Zn-ejecting compounds including disulfiram and ebselen; this observation may enable the development of inhibitors selective for this subfamily of 2OG dependent oxygenases that do not rely on binding to the highly-conserved Fe(ii)-containing active site.

Cells respond to oxidative stress including nitric oxide (NO) by increasing cellular glutathione concentration, as a part of adaptive response against oxidative injury. To elucidate the mechanism by which NO induces glutathione we investigated the reactive oxygen species (ROS) generated in the cell. Treatment of RAW264.7 cells with NO donor, sodium nitroprusside (SNP), resulted in a temporary i...

Seleno-organic glutathione peroxidase (GPx) mimetics, including ebselen (Eb), have been tested in in vitro studies for their ability to scavenge reactive oxygen and nitrogen species, including hydrogen peroxide and peroxynitrite. In this study, we investigated the efficacies of two Eb analogues, m-hydroxy ebselen (ME) and ethanol-ebselen (EtE) and compared these with Eb in cell based assays. We...