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.
出处
《时珍国医国药》
CAS
CSCD
北大核心
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)
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
α-glucosidase inhibitor； Andrographolide derivatives； Noncompetitive inhibition； PSDS（Potassium Sodium Dehydroandroandrographolide Succinate）
