应用α-葡萄糖苷酶抑制剂高通量筛选模型筛选降血糖中药  

High Throughput Screening of α-Glucosidase Inhibitors:Application to Hypoglycemic Traditional Chinese Medicine

作　　者：张冉[1] 刘泉[1] 申竹芳[1] 杜冠华[1] 

机构地区：[1]中国医学科学院-中国协和医科大学药物研究所国家药物筛选中心国家教育部天然产物药物重点实验室,北京100050

出　　处：《中国药学杂志》2007年第10期740-743,共4页Chinese Pharmaceutical Journal

基　　金：国家高技术计划(863)项目(20043Z3842)

摘　　要：目的建立筛选α-葡萄糖苷酶抑制剂的体外高通量筛选模型,并对30味常用清热解表中药进行筛选。方法应用大鼠小肠上段提取的α-葡萄糖苷酶,以蔗糖作为底物,通过测定反应体系中葡萄糖的生成量来检测α-葡萄糖苷酶的活性。通过优化酶促反应条件,建立检测α-葡萄糖苷酶活性的比色测定法及其抑制剂体外筛选的方法,并对30味中药共72个样品进行高通量筛选。结果阿卡波糖对α-葡萄糖苷酶的抑制活性与文献报道相近;筛选发现鸭跖草、山慈菇和桑叶等3味中药的不同极性提取物对α-葡萄糖苷酶有可重复的抑制作用。结论应用比色法建立的筛选模型可进行α-葡萄糖苷酶抑制剂的高通量筛选及中药相关活性物质的发现。OBJECTIVE To determine alpha-glucosidase activity in vitro for high throughput screening of Traditional Chinese Medicine. METHODS The alpha-glucosidase was prepared from rat small intestine. The inhibitory activities for alpha-glucosidase in the petroleum ether,ethanol and water extracts from 30 species of TCM were detected based on the concentration of glucose in the reaction system by rapid colorimetric assays. RESULTS Acarbose was shown to be an alpha-glucosidase inhibitor with the IC5o similar with the references. The inhibitory activities against alpha-glucosidase of the extracts from Commelina communis L ,Pseudobulbus cremastrae seu pleiones and Folium mori were significant, with inhibitory rate all above 90%. CONCLUSION This assay can be performed to screen alpha-glucosidase inhibitor. Some extracts of TCM have inhibitory activities of alpha-glucosidase.

关 键 词：Α-葡萄糖苷酶 抑制剂 高通量药物筛选 中药 

分 类 号：R965[医药卫生—药理学]