The mechanism of the redox reaction of ebselen with superoxide was investigated using both ESR and electrochemical techniques. The reaction with superoxide in aprotic solvents was followed by means of cyclic voltammetry and ESR spin-trapping. A decrease in the oxidation current due to superoxide as a result of the addition of ebselen was clearly observed in the cyclic voltammograms. Ebselen red...

The organo-seleniumdrug ebselen exhibits a wide range of pharmacological effects that are predominantly due to its interference with redox systems catalyzed by seleno enzymes, e.g., glutathione peroxidase and thioredoxin reductase. Moreover, ebselen can covalently interact with thiol groups of several enzymes. According to its pleiotropic mode of action, ebselen has been investigated in clinica...

Ebselen [2-phenyl-1,2-benzisoselenazol-3(2H)-one], a seleno-organic compound with glutathione peroxidase-like activity is used in clinical trials against stroke. Human and bovine TrxR catalyzed the reduction of ebselen to ebselen selenol by NADPH with an apparent K(M)-value of 2.5 microM and a kcat of 588 min(-1). The addition of thioredoxin (Trx) stimulated the TrxR-catalyzed reduction of ebse...

s | 19 Methods: We studied 20 healthy volunteers who were tested on two occasions receiving either ebselen (3600mg over 24 hours) or identical placebo in a double-blind, random-order, cross-over design. Two hours after the final dose of ebselen/placebo, participants underwent proton magnetic resonance spectroscopy (1H MRS) at 7 tesla (7T) with voxels placed in anterior cingulate and occipital c...

Ebselen is a seleno-organic compound currently in clinical trials for the treatment of ischemic stroke and subarachnoid hemorrhage. Its putative mode of action as a neuroprotectant is via cyclical reduction and oxidation reactions, in a manner akin to glutathione peroxidase. For this reason, we have investigated the effects of ebselen on the redox-sensitive NMDA receptor. We have found that ebs...

The selenium-based compound ebselen is a powerful antioxidant, a potent anti-inflammatory agent and a potential neuroprotective compound. Several studies have demonstrated that part of the biological effect of ebselen is the result of the inhibition of apoptosis. We show in this report that ebselen induced the necrotic cell death of Sp2/0-Ag14 hybridoma cells. This process was rapid, with over ...

Release of arachidonic acid (AA) is a neurotoxic mechanism of oxidative nature in trauma and ischemia. We studied ebselen effects on AA and 4-hydroxynonenal toxicity in rat cortical neurons in simulated ischemia in vitro by assessing cell viability and glutathione concentration. Ebselen normalized neuronal viability diminished by AA and 4-hydroxynonenal and increased glutathione level in normox...

Five ebselen and three acyclic ebselen derivatives were synthesized. These compounds were screened for their glutathione peroxidase (GSH Px)-like activity and scavenging activity against 1,1-diphenyl-2-pycryl-hydrazyl (DPPH) and peroxynitrite radical. All tested compounds displayed similar significant GSH Px-like activity, which are slightly higher than that of ebselen. The peroxynitrite scaven...

Background and Purpose—The effect of ebselen, a seleno-organic compound with antioxidant activity through a glutathione peroxidase–like action, on the outcome of acute ischemic stroke was evaluated in a multicenter, placebo-controlled, double-blind clinical trial. Methods—Patients diagnosed as having acute ischemic stroke who could receive drug treatment within 48 hours of stroke onset were enr...

1: Ebselen (2-phenyl-1,2-benzisoselenazol-3[2H]-one) is a selenoorganic compound exhibiting both glutathione peroxidase activity and antioxidant activity. Although it has been reported that ebselen is effective for oxidative stress-induced neuronal damage both in vivo and clinically, the precise mechanisms of the efficacy have not yet been elucidated. Thus, we hypothesized that ebselen may affe...