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  • 标题:2,2-Diphenyl-1-picrylhydrazyl Hydrate, a Stable Free Radical, Is an α-Glucosidase Inhibitor
  • 本地全文:下载
  • 作者:Dong-Sun LEE ; Nam-Soon KIM ; Sang-Han LEE
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:2001
  • 卷号:24
  • 期号:6
  • 页码:727-728
  • DOI:10.1248/bpb.24.727
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:Glycosidases play a pivotal role in processing of various glycoproteins and glycolipids. It is well known that glycosidases are also involved in a variety of degenerative metabolic disorders such as cancer and AIDS. In order to develop potent α-glucosidase inhibitors, we first screened 2,2-diphenyl-1-picrylhydrazyl hydrate as a candidate. 2,2-Diphenyl-1-picrylhydrazyl hydrate was found to inhibit α- and β-glucosidases as well as α- and β-mannosidases. It was also shown to be a non-competitive inhibitor of yeast α-glucosidase with a Ki value of 1.1×10-6M. Taken together, we anticipate that 2,2-diphenyl-1-picrylhydrazyl hydrate may be a potent inhibitor for some incurable metabolic disorders including AIDS.
  • 关键词:2,2-diphenyl-1-picrylhydrazyl hydrate;α-glucosidase inhibitor;enzyme kinetics;non-competitive inhibition
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