研究论文

三种抗坏血酸糖苷的合成及其α-糖苷酶抑制活性

  • 马济美 ,
  • 谢凌云 ,
  • 王龙文 ,
  • 陈杭炜 ,
  • 曾贞 ,
  • 陈浩 ,
  • 江洪
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  • 华中农业大学理学院化学系 武汉 430070

收稿日期: 2016-12-11

  修回日期: 2017-01-20

  网络出版日期: 2017-02-20

基金资助

国家自然科学基金(No.21402056)和中央高校基本科研业务费专项资金(No.2014QC007)资助项目.

Synthesis and α-Glycosidase Inhibitory Activity of Three Ascorbic Acid Glycosides

  • Ma Jimei ,
  • Xie Lingyun ,
  • Wang Longwen ,
  • Chen Hangwei ,
  • Zeng Zhen ,
  • Chen Hao ,
  • Jiang Hong
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  • Department of Chemistry, College of Science, Huazhong Agricultural University, Wuhan 430070

Received date: 2016-12-11

  Revised date: 2017-01-20

  Online published: 2017-02-20

Supported by

Project supported by the National Natural Science Foundation of China (No. 21402056) and the Fundamental Research Funds for the Central Universities (No. 2014QC007).

摘要

2-O-β-D-葡萄糖基-L-抗坏血酸(AA-2βG)是从枸杞中分离得到的一种天然抗坏血酸糖苷化合物,通过化学方法合成了AA-2βG及其两种类似物,并用商品化的阿卡波糖作为阳性对照,研究了三种抗坏血酸糖苷对酿酒酵母α-葡萄糖苷酶和猪胰腺α-淀粉酶的活性影响.结果显示,三种抗坏血酸糖苷对α-葡萄糖苷酶有显著的抑制作用,对α-淀粉酶抑制作用不明显,说明这三种抗坏血酸糖苷具有作为α-糖苷酶抑制剂开发的潜质.

本文引用格式

马济美 , 谢凌云 , 王龙文 , 陈杭炜 , 曾贞 , 陈浩 , 江洪 . 三种抗坏血酸糖苷的合成及其α-糖苷酶抑制活性[J]. 有机化学, 2017 , 37(6) : 1426 -1432 . DOI: 10.6023/cjoc201612037

Abstract

2-O-(β-D-Glucopyranosyl)-L-ascorbic acid, a natural β-glycoside with ascorbic acid moiety present in Lycium barbarum, and its two analogues were chemically synthesized. Their inhibitory effect on yeast α-glucosidase and α-amylase were investigated with commercially available acarbose as positive control. The biological assays demonstrated the distinct inhibitory effect of these compounds on α-glucosidase activity and weak inhibitory activity against pancreatic α-amylase. The kinetic study indicated that these compounds were competitive inhibitors. These results imply that these three β-glycosides have the potential to be developed as α-glucosidase inhibitors.

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