摘要
目的研究桑叶提取物抑制α-葡萄糖苷酶活性反应体系的条件优化及酶动力学。方法采用酶-抑制剂模型法,优化底物浓度、酶用量和反应时间,确定最佳反应体系,研究桑叶提取物对α-葡萄糖苷酶的抑制作用,并采用双倒数作图法研究桑叶提取物的酶抑制动力学特性。结果当蔗糖浓度为40 mg/mL,酶用量为0.2mL(约1.6 U/mL),反应时间为25 min时为最佳反应体系;酶抑制动力学实验表明,桑叶提取物的抑制类型为混合型竞争性抑制,阳性对照为非竞争性抑制。结论桑叶提取物对α-葡萄糖苷酶活性有抑制作用;桑叶提取物对α-葡萄糖苷酶抑制活性为混合性竞争性抑制,可以用于开发降糖药物。
Objective To establish an optimized inhibitory reaction system for the research of Folium Mori extracts in inhibiting alpha-glucosidase activity and to investigate the enzyme kinetics.Methods We studied the inhibitive effects of Folium Mori extracts on alpha-glucosidase by using enzyme-inhibitor model and optimized the reaction system by optimizing the substrate concentration,the amount of enzyme and the reaction time.We also investigated the inhibitory kinetic characteristics of extracts by using Lineweaver-Burk method.Results The optimized reaction system consisted of 40 mg/mL of the substrate concentration,0.2 mL of enzyme and 25 min for reaction time.Inhibitory kinetic results indicated that the extracts were mixed competitive inhibitors,but the positive drug was noncompetitive inhibitor.Conclusion Folium Mori extracts have inhibitory effect on α-glucosidase activity,and the inhibitory type is in mixed competitive inhibition,which are expected to be used to develop as anti-diabetes drugs.
出处
《中药新药与临床药理》
CAS
CSCD
北大核心
2012年第1期42-44,共3页
Traditional Chinese Drug Research and Clinical Pharmacology
基金
广东省自然科学基金(2008A030201031):天然降糖药物桑叶提取物的新药开发