Design and Evaluation of Novel Selenium-Containing Antioxidant

现在有越来越多的证据表明，自由基介导的氧化在体内进行，就像在塑料、橡胶和脂肪中一样，它们在各种疾病、癌症和衰老的发展中起着致病作用。因此，抑制这种氧化作用和开发新型高效抗氧化剂受到了人们的广泛关注。本研究旨在开发一种新型的含硒抗氧化剂，并对其抗氧化效能进行评价。以2-苯基-1，2-苯并异硒-3(2H)-酮为候选化合物，研究了其抗氧化作用和活性。研究证实，Ebselen不是自由基清除剂，也不会还原维生素E自由基来再生维生素E。Ebselen能迅速将过氧化氢还原为相应的醇，从而抑制金属催化的脂质和低密度脂蛋白的氧化。此外，还发现依布硒可完全抑制脂氧合酶诱导的脂质氧化。Ebselen对过氧亚硝酸根诱导的脂质过氧化也有较强的抗氧化作用。结论：依布硒对金属离子和过氧亚硝酸根诱导的氧化具有较强的抗氧化性。

There is now increasing evidence which shows that the free-radical mediated oxidations proceed in vivo as in plastics rubber and lipids and that they play a causative role in the progression of various diseases, cancer and aging. As a consequence, the inhibition of such oxidations and development of novel potent antioxidants have received much attention. The present research has been carried out aiming at developing a novel selenium-containing antioxidant and evaluating its antioxidant potency. Ebselen, 2-phenyl-1,2-benzisoselenazol-3 (2H) -one, was chosen as a candidate and its antioxidant action and activity were studied. It was confirmed that ebselen did not act as a radical scavenger nor did it reduce vitamin E radical to regenerate vitamin E.Ebselen reduced hydroperoxides rapidly to corresponding alcohol and thereby inhibited the metal-catalyzed oxidations of lipids and low density lipoproteins. Furthermore, it was found that ebselen completely inhibited the lipid oxidation induce by lipoxygenase. Ebselen also exerted potent antioxidant activity against lipid peroxidation induced by peroxynitrite. It was concluded that ebselen is a potent antioxidant against oxidations induced by metal ions and peroxynitrite.