应用化学 ›› 1997, Vol. 0 ›› Issue (3): 66-69.

• 研究论文 • 上一篇    下一篇

苯并异硒唑酮氨基酸衍生物的谷胱甘肽过氧化物酶样活性

肖颖歆, 黄祖云, 刘秀芳, 徐汉生   

  1. 武汉大学化学系, 武汉 430072
  • 收稿日期:1996-09-12 修回日期:1997-01-23 出版日期:1997-06-10 发布日期:1997-06-10

Glutathione Peroxidase-like Activities of Amino Acid Derivatives of Benzisoselenazolone

Xiao Yingxin, Huang Zhuyun, Liu Xiufang, Xu Hansheng   

  1. Department of Chemistry, Wuhan University, Wuhan 430072
  • Received:1996-09-12 Revised:1997-01-23 Published:1997-06-10 Online:1997-06-10

摘要: 采用NADPH/GSSG还原酶为指示剂的偶合法测定了两类共7种新型苯并异硒唑酮氨基酸衍生物的GSH-Px活性。结果表明,所有模拟物均显示较好的GSH-Px样活性,并且具有明显的构-效关系。

关键词: 苯并异硒唑酮, 氨基酸衍生物, 苯基苯并异硒唑(2H)酮, 谷胱甘肽过氧化物酶

Abstract: Seven novel amino acid derivatives of benzisoselenazolone were found to have significant glutathione peroxidase(GSH-Px)like activity as determined by coupling test using NADPH/GSSG reductase as an indicator. They catalysed the reduction reaction of hydroperoxides in the presence of GSH with good structure activity relationships. The activities of the compounds 1, 6 and 7 were almost equal to that of Ebselen, which is known as the best mimic of GSH-Px. It was also found that the concentration of the mimics and GSH, the temperature and the pH value of the reaction system had great effects on the catalytic activity of the mimics. The apparent activation energy of compounds 4 and 7 had been determined as 101 and 87.3 kJ/mol respectively.

Key words: benzisoselenazolone, amino acid derivative, Ebselen, glutathione peroxidase