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

Glutathione Peroxidase like Activities of Amino Acid Derivatives of Benzisoselenazolone

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．

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.