D-葡萄糖苷酶抑制剂的研究

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．

A Study of D-Glucosidase Inhibitors

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.