穿心莲内酯衍生物炎琥宁对α-葡萄糖苷酶抑制活性及机制研究  

Inhibition Effect and Mechanism of Potassium Sodium Dehydroandroandrographolide Succinate(PSDS) as An α-glucosidase Inhibitor

作　　者：徐俊[1] 鲍娇琳[1] 沈伟哉[2] 蔡绍晖[1] 

机构地区：[1]暨南大学药学院,广东广州510632 [2]暨南大学医学院,广东广州510632

出　　处：《时珍国医国药》2012年第7期1637-1640,共4页Lishizhen Medicine and Materia Medica Research

基　　金：国家自然科学基金(No.30973565)

摘　　要：目的测定穿心莲内酯衍生物炎琥宁对α-葡萄糖苷酶的抑制活性,并初步判断其对α-葡萄糖苷酶的抑制作用类型。方法利用体外酶促反应测定穿心莲内酯衍生物炎琥宁对α-葡萄糖苷酶的抑制活性;利用Lineweaver-Burk双倒数作图法初步判断穿心莲内酯衍生物炎琥宁和阿卡波糖对α-葡萄糖苷酶的抑制作用类型。结果体外酶促实验得到炎琥宁的IC50为0.14mmol/L;阿卡波糖组与空白组的Lineweaver-Burk直线交点情况类似于竞争性抑制,与文献报道一致;炎琥宁组与空白组的Lineweaver-Burk直线交点情况类似于非竞争性抑制。结论穿心莲内酯衍生物炎琥宁在体外对α-葡萄糖苷酶具有明显的抑制作用,初步判断其抑制类型属于非竞争性抑制。Objective To test the inhibition effect and type of andrographolide derivatives PSDS,an α-glucosidase inhibitor in vitro.Methods① IC50 of PSDS inhibiting α-glucosidase was measured in vitro.② The inhibition type of PSDS inhibiting α-glucosidase was investigated by the intersection of Lineweaver-Burk lines between PSDS and control.Results ① The IC50 of PSDS inhibiting α-glucosidase was 0.14mmol/L.② The intersection of Lineweaver-Burk lines between PSDS and control was well-fit to noncompetitive inhibition type.Conclusion The andrographolide derivative PSDS has obvious inhibition to α-glucosidase in vitro and the inhibition type is judged as noncompetitive inhibition.

关 键 词：Α-葡萄糖苷酶抑制剂 穿心莲内酯衍生物 非竞争性抑制 炎琥宁 

分 类 号：R285.5[医药卫生—中药学]