Study on microassay for screening ?-glucosidase inhibitors by orthogonal matrix method
- VernacularTitle:?-葡萄糖苷酶抑制剂微量筛选模型的正交法构建和筛选
- Author:
Fumei YANG
;
Qianyun SUN
- Publication Type:Journal Article
- Keywords:
?-glucosidase;
?-glucosidase inhibitor;
screening model;
drug screening;
diabetes mellitus;
orthogonal experiment
- From:
Chinese Pharmacological Bulletin
2003;0(08):-
- CountryChina
- Language:Chinese
-
Abstract:
Aim To provide practical microassay for screening ?-glucosidase inhibitors in drug discovery.Methods The optimal conditions of assaying the activity of ?-glucosidase were determined in 96-well plates under physiological pH value and temperature by orthogonal matrix method.Reaction time and the concentrations of ?-glucosidase and substrate were optimized.After the effects of sample solvent(DMSO) used in the assay and stopping reagent on enzyme activity were assessed,the assay conditions were finally selected.Then 492 kinds of extracts from Guizhou ethno-drugs were screened.Results Practical and sensitive microassay for screening ?-glucosidase inhibitors was successfully constituted.And in 492 kinds of extracts,145 kinds of samples effectively inhibited the enzyme activity.Conclusion The microassay constituted in this work possesses advantages of being rapid,sensitive,reliable,cost saving,easy and flexible.