The pharmacology of ebselen

Role of enteral nutrition supplemented with ebselen and EHEC in pancreatitis-associated multiple organ dysfunction in rats

“…otal role in the pathological mechanism of pancreatitis-associated MODS. Experimental studies have suggested that MIP-2 may play a key role in the pathophysiology of acute pancreatitis and in the development of pancreatitis-associated lung injury [13]. Results from our experimental studies demonstrated that circulating MIP-2 was signifi cantly higher in AP rats, while the treatment with ebselen and EHEC did not have reversible effects.…”

“…Ebselen (2-phenyl-1,2-benzisoselenazol-3(2H)-one) is a non-toxic seleno-organic drug with anti-infl ammatory, antiatherosclerotic and cytoprotective properties by downregulating the production of oxygen free radicals [13][14][15]. Ebselen is a mimic of GSH peroxidase which also reacts with peroxynitrite and can inhibit enzymes such as lipoxygenases, NO synthases, NADPH oxidase, protein kinase C and H(+)/K(+)-ATPase [16].…”

Free Radicals, Neuronal Death and Neuroprotection

“…The group of patients treated with acetyl-L-carnitine showed a significant improvement in learning abilities, and longterm memory skills, suggesting the therapeutic importance of this metabolite for the treatment of geriatric patients with mental disfunction. Besides the natural AO, there is also a growing list of synthetic AO that have been widely studied, for example, conjugated forms of the enzymes SOD and CAT (Greenwald, 1990) and supplements of selenium (Parnham et al, 1991). Similarly, there is growing evidence that give, some drugs with different therapeutic uses to neuroprotection such as probucol (hypocholesterolemic) and salicylates, a certain capacity as recycler of free radicals under experimental conditions (Cui et al, 2004;Juliano et al, 1995;Zhao et al, 1995).…”

Synthesis and <i>in Vitro</i> Antiproliferative Evaluation of Novel Hybrids from 1,3,4-Thiadiazole and Benzisoselenazolone

“…1], which possess potent antioxidant, anti-inflammatory, anticancer and cholinesterase inhibitory activities. 4,[11][12][13][14] Particularly, as a novel organoselenium compound targeting thioredoxin reductase (TrxR), ethaselen has been reported to exhibit broad spectrum of antitumor effects with slight toxicity, and has now entered Phase I clinical trials in China. [4][5][6] 1,3,4-Thiadiazole is a privileged scaffold incorporated in many compounds presenting a wide range of pharmacological activities, such as antioxidant, 15,16) antibacterial, 17,18) antidepressant, 19,20) antidiabetic, 21,22) antifungal, 23,24) anticonvulsant, 25,26) antiinflammatory, 27,28) antileishmanial 29) and acetylcholinesterase inhibitory properties.…”