Ebselen, a promising antioxidant drug: mechanisms of action and targets of biological pathways
Ebselen, a promising antioxidant drug: mechanisms of action and targets of biological pathways
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DOI：
10.1007/s11033-014-3417-x
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发表时间：
2014-08-01
影响因子：
2.8
通讯作者：
Tomar, Raghuvir S.
中科院分区：
文献类型：
--
作者：
Azad, Gajendra Kumar;Tomar, Raghuvir S.
Ebselen是一种有机硒化合物，模拟谷胱甘肽过氧化物酶活性。它是一种多功能化合物，催化几种基本反应，以保护细胞成分免受氧化和自由基损伤。基于大量的体外和体内研究，提出了各种机制来理解依布硒啉在健康和疾病中的生物医学作用。它调节金属蛋白、酶辅因子、基因表达、表观遗传学、抗氧化防御和免疫系统。由于这些特性，依布硒啉目前正在进行临床试验，用于预防和治疗各种疾病，如心血管疾病、关节炎、中风、动脉粥样硬化和癌症。一些基于依布硒的药剂正在进行广泛的研究。由于依布硒啉已被证明具有显著的细胞毒性，因此需要适当的研究来重新设计用于临床试验的基于依布硒啉的疗法。本文综述了依布硒啉的生物化学和分子生物学特性，以及依布硒啉的药理学应用和未来研究方向。
Ebselen, an organoselenium compound, mimics glutathione peroxidase activity. It is a multifunctional compound, which catalyzes several essential reactions for the protection of cellular components from oxidative and free radical damage. Based on a number of in vitro and in vivo studies, various mechanisms are proposed to understand the biomedical actions of ebselen in health and diseases. It modulates metallo-proteins, enzymatic cofactors, gene expression, epigenetics, antioxidant defenses and immune systems. Owing to these properties, ebselen is currently under clinical trials for the prevention and treatment of various disorders such as cardiovascular diseases, arthritis, stroke, atherosclerosis, and cancer. A few ebselen-based pharmaceutical agents are under extensive investigation. As ebselen has been shown to have significant cellular toxicity, appropriate studies are needed to redesign the ebselen-based therapy for clinical trials. This review summarizes current understanding of the biochemical and molecular properties, and pharmacological applications of ebselen and future directions in this area of research.