摘要
目的:探讨海藻铁钉菜提取物对α-葡萄糖苷酶活性的影响及其反应动力学。方法:萃取法获得铁钉菜甲醇提取物的石油醚部位、二氯甲烷部位、乙酸乙酯部位、正丁醇部位、水部位等5个部位,采用PNPG筛选其中具有α-糖苷酶酶抑制的活性部位,通过酶促动力学方法与Lineweaver-Burk曲线,推断酶抑制类型。结果:包括甲醇提取物在内的6种铁钉菜提取物均具有一定的α-葡萄糖苷酶抑制活性,其中乙酸乙酯部位、石油醚部位、正丁醇部位、二氯甲烷部位的抑制活性均较强,IC50分别为3.4,4.4,5.1,7.8μg·mL^(-1),均远强于阳性对照阿卡波糖Acarbose(IC501 075.8μg·mL^(-1))。抑制动力学分析显示,乙酸乙酯部位、石油醚部位、正丁醇部位、二氯甲烷部位等对α-葡萄糖苷酶抑制作用均属于混合Ⅰ型抑制类型。结论:铁钉菜提取物具有作为新型α-葡萄糖苷酶抑制剂的药用开发价值,特别是乙酸乙酯部位。
OBJECTIVE To study the influence of seaweed Ishige okamurai onα-glucosidase activity and its reaction kinetics.METHODS Five solvent fractions,including petroleum ether fraction,dichloromethane fraction,ethylacetate fraction,n-butanol fraction and water fraction,were extracted from methanol extract of Ishige okamurai.Among them,α-glucosidase inhibiting extracts were screened by PNPG method,their inhibitory types were inferred by enzymatic dynamics and Lineweaver-Burk curve methods.RESULTS Six kinds of extracts,including methanol extract fromIshige okamurai,had certainα-glucosidase inhibiting activity,in which ethyl acetate fraction,petroleum ether fraction,dichloromethane fraction and n-butanol fraction had strong inhibitory activity with IC50 values of 3.4,4.4,5.1,7.8μg·mL^（-1）,respectively,more potent than acarbose（IC501075.8μg·mL^（-1））,the positive control of this study.Inhibition dynamics analysis showed that the enzyme inhibitions of ethyl acetate fraction,petroleum ether fraction,dichloromethane fraction and n-butanol fraction were all close to mixed type Ⅰ inhibition.CONCLUSION The extracts of Ishige okamurai have medicinal development values as newα-glucosidase inhibitors,especially ethyl acetate fraction.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2016年第1期16-20,共5页
Chinese Journal of Hospital Pharmacy
基金
福建省自然科学基金海洋经济发展专项重点项目(编号:2014N0017)
泉州市科技计划项目(编号:2014Z129)资助
泉州市第二批科技项目(编号:2013Z126)
福建省大学生创新创业计划项目(编号:201410399027)
