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  • 标题:Evaluation of α-Glucosidase Inhibition by Using an Immobilized Assay System
  • 本地全文:下载
  • 作者:Tomoyuki OKI ; Toshiro MATSUI ; Kiyoshi MATSUMOTO
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:2000
  • 卷号:23
  • 期号:9
  • 页码:1084-1087
  • DOI:10.1248/bpb.23.1084
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:The inhibitory effects of natural and synthetic inhibitors on the intestinal membrane-bound hydrolase, α-glucosidase (AGH), were evaluated by using an immobilized cyanogen bromide-activated Sepharose 4B support. Immobilized AGH (iAGH) inhibition study by synthetic inhibitors (acarbose and voglibose) revealed that the magnitude of inhibition differed from that in the free AGH (fAGH) study : IC50 value of acarbose in iAGH-maltase assay system, 340-430 nM; fAGH, 11 nM. iAGH-maltase inhibition by both inhibitors was influenced by blocking reagents with different functional groups (COOH, OH, CH3, and NH2 groups). On the other hand, significant iAGH-sucrase inhibitory activity was observed only when using the negatively charged support induced by 0.1 M β-alanine. The Km values obtained in the iAGH assay system were similar to those from the fAGH method. With natural inhibitors, the iAGH-sucrase inhibitory activity of D-xylose, with in vivo glucose suppression, increased twice compared to that in fAGH. Green tea extract gave almost the same inhibition for both AGH assay systems.
  • 关键词:α-glucosidase;immobilization;inhibition;noninsulin-dependent diabetes mellitus
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