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Ebselen, a selenoorganic compound as glutathione peroxidase mimic
Free Radical Biology and Medicine, 1993The selenoorganic compound ebselen, 2-phenyl-1,2-benzisoselenazol-3(2H)-one, exhibits activity as an enzyme mimic. The reaction catalyzed is that of a glutathione (GSH) peroxidase (i.e., the reduction of a hydroperoxide at the expense of thiol). The specificity for substrates ranges from hydrogen peroxide and smaller organic hydroperoxides to membrane ...
Helmut Sies
exaly +3 more sources
Target discovery of ebselen with a biotinylated probe
Chemical Communications, 2018An activity-based protein profiling (ABPP) method for ebselen-binding proteins based on biotin-ebselen allowed for the robust identification of 462 targeted proteins, implicating multifunctional regulation of ebselen.
Zhenzhen Chen +9 more
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Investigating the Metabolic Mechanisms of Butaselen, An Ebselen Analog
Current Drug Metabolism, 2022Background: Butaselen is an ebselen analog that is under clinical trials for treating hepatic and pulmonary fibrosis. Our previous studies showed that butaselen is mainly present in human plasma in the form of M2, a free Se-methylated metabolite. Objective: This study aimed to investigate the metabolic mechanisms of butaselen. Methods and Results:
Qianqian, Tian +10 more
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Ebselen, a Seleno-organic Antioxidant, as an Electrophile
Chemical Research in Toxicology, 2006Ebselen [2-phenyl-1,2-benzisoselenazol-3(2H)-one], a seleno-organic compound showing glutathione peroxidase-like activity, is one of the promising synthetic antioxidants. In the present study, we investigated the electrophilic potential of this antioxidant and established the mechanism of the cysteine-targeted oxidation of protein.
Toyo, Sakurai +6 more
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Ebselen: prospective therapy for cerebral ischaemia
Expert Opinion on Investigational Drugs, 2000Stroke occurs due to haemorrhage or occlusive injury and results in ischaemia and reperfusion injury. A variety of destructive mechanisms are involved including oxygen radical generation, calcium overload, cytotoxicity and apoptosis as well as the generation of inflammatory mediators.
M, Parnham, H, Sies
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Molecular Pharmacology, 1990
The therapeutic effect of ebselen has been linked to its peroxidase activity. In the present study, the peroxidase activity of ebselen toward H2O2 with the endogenous thiols GSH and dihydrolipoate [L(SH)2] as cofactors was determined. When GSH was used, peroxide removal was described by a ter uni ping pong mechanism with Dalziel coefficients for GSH ...
Haenen, G R +3 more
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The therapeutic effect of ebselen has been linked to its peroxidase activity. In the present study, the peroxidase activity of ebselen toward H2O2 with the endogenous thiols GSH and dihydrolipoate [L(SH)2] as cofactors was determined. When GSH was used, peroxide removal was described by a ter uni ping pong mechanism with Dalziel coefficients for GSH ...
Haenen, G R +3 more
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The use of ebselen for radioprotection in cultured cells and mice
Free Radical Biology and Medicine, 2009Ionizing radiation induces the production of reactive oxygen species (ROS), which play an important causative role in cell death. Therefore, compounds that control the level of ROS may confer radioprotective effects. Ebselen, a seleno-organic compound, has been shown to protect against cell injury caused by ROS.
Jean Kyoung, Tak, Jeen-Woo, Park
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Ebselen affects calcium homeostasis in human platelets
Biochemical Pharmacology, 1991Ebselen (PZ 51, 2-phenyl-1,2-benzoisoselenazol-3-(2H)-one) is a selenoorganic compound with anti-inflammatory properties. Its pharmacological action is thought to originate from its peroxidase activity which could lower the peroxide tonus required for cyclooxygenase and lipoxygenase activations.
B, Brüne, B, Diewald, V, Ullrich
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Mechanisms of Ebselen as a Therapeutic and Its Pharmacology Applications
Future Medicinal Chemistry, 2020Ebselen is a synthetic organoselenium radical scavenger compound that possesses glutathione peroxidase-like activity and its own unique bioactivity by reacting with thiols, hydroperoxides and peroxynitrites. Owing to its high affinity toward several essential reactions, ebselen protects cellular components from oxidative and free radical damage, and it
Jun Wang +6 more
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Determination of Ebselen by HPLC: Validation and Application of the Method
Chromatographia, 2004Ebselen is an organo-selenium, highly hydrophobic compound that exhibits glutathion peroxidase-like activity. It is now in phase III trials in Japan for investigating its effect on ischemic stroke. We have developed an HPLC method for the determination of Ebselen at ambient temperature and applied it to a patented tablet formulation.
Yilmaz, S, Yalcin, G
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