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D-葡萄糖苷酶抑制剂的研究

A Study of D-Glucosidase Inhibitors

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【作者】 岳保珍王孝伟贺师鹏王志文孟晓菲张佩瑛马灵台

【Author】 Yue Bao-Zhen; Wang Xiao-Wei; He Shi-Peng; Wang Zhi-Wen Meng Xiao-Fei Zhang Pei-Ying Ma Ling-Tai (School of Pharmaceutical Science,Department of Biophysics Beijing Medical University,Beijing 100083)

【机构】 北京医科大学药学院!北京100083北京医科大学药学院生物物理系!北京

【摘要】 用高灵敏度的荧光法研究了13种糖类化合物对α或β-D-葡萄糖苷酶的抑制作用.实验结果表明:5-氨基-5-脱氧-D-吡喃葡萄糖-1-磺酸铵盐(1)、5-氨基-5-脱氧-D-吡喃葡萄糖-1-磺酸(2)、5-氨基-5-脱氧-D-葡萄糖-1.亚硫酸加成物(3)等三种氮杂糖对α或β-D-葡萄糖苷酶均呈现竞争性抑制作用.化合物(1)的Kiα=372μmol/L;Kiβ=6.38μmol/L.化合物(2)的Kiα=34.4μmol/L;Kiβ=6.84μmol/L.化合物(3)的Kiα=47.2μmol/L;Kiβ=11.9μmol/L.上述三个化合物对β-D-葡萄糖苷酶的抑制作用都强子α-D-葡萄糖苷酶.尤其对化合物(1),其Kiα/Kiβ=58.3,表明其抑制糖苷酶活性有较好的选择性.

【Abstract】 Thirteen Carbohydrated derivatives as glucosidase dase inhibitor were determined using method of fluorescence analysis. The experimental adults demonstrated that the competitive inhibition by ammonium-5 -amino- 5deoxy- D -glucopyranose- 1 - sulfonate (1), 5 -amino- 5 - deoxy- D -glu-copyrannose 1 - sulfoacid (2), 5 -amino-5 - deoxy- D - glucose- 1 - sulfoacid (3) on αor β- D -glucosidases.The Kiα and Kiβ values were determines for compounds (1), (2),(3). The Parameters indicated that effects of theSe three compounds on β-D-glucosidase were. stronger than those on α-D-glucosi-dase. Especially, from the ratio (Kiα/Kiβ = 58. 3) for compound (1) shows that there is a good in- hibitory action of selectivity.

【基金】 国家自然科学基金!29170045
  • 【分类号】Q55
  • 【被引频次】10
  • 【下载频次】214
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