摘要
以阿卡波糖为阳性对照,半数抑制浓度(IC 50)为α-葡萄糖苷酶抑制活性评价指标,采用体外抑制模型方法评价葫芦茶醇提物不同溶剂(石油醚、乙酸乙酯、正丁醇、水)萃取物对α-葡萄糖苷酶(酵母菌来源和小鼠小肠来源)的抑制作用。经酶促动力学与Lineweaver-Burk双倒数法探讨抑制作用最强萃取物对α-葡萄糖苷酶活性的抑制机制,以期为葫芦茶有效提取物在医学、食品及化工领域的应用提供参考依据。结果表明,葫芦茶不同溶剂提取物抑制酵母、小鼠小肠来源α-葡萄糖苷酶活性强弱均为正丁醇提取物>水提取物>乙酸乙酯提取物>石油醚提取物。其中,葫芦茶正丁醇提取物对酵母菌源α-葡萄糖苷酶和小鼠小肠源α-葡萄糖苷酶的抑制作用(IC 50分别为13.08±1.23和221.21±3.75μg/mL)显著强于其他提取物和阳性对照阿卡波糖(P<0.05)。动力学研究表明,葫芦茶正丁醇提取物对α-葡萄糖苷酶的抑制类型为竞争性抑制。以上结果表明葫芦茶醇提物的正丁醇萃取物对α-葡萄糖苷酶活性的抑制作用较强,是挖掘抑制α-葡萄糖苷酶活性物质的主要部位。
Using acarbose as positive control and half-inhibitory concentration value(IC 50)as evaluation index,and inhibitory effects of different polarity fractions of the ethanol extracts from Tadehagi triquetrum on the activities ofα-glucosidase(from yeast and small intestine in mice)were evaluated with in vitro inhibition model.The enzymatic dynamics and Lineweaver-Burk methods were used to analyze the inhibitory type of the best medicinal part on the activities ofα-glucosidase,which will provide a reference evidence for the application of effective polarity fraction from T.triquetrum in medical,food,and chemical fields.The results indicated that inhibitory activity of different polarity fractions of the ethanol extracts from T.triquetrum on the activities ofα-glucosidase(from yeast and small intestine in mice)were n-butanol fraction>water fraction>ethylacetate fraction>petroleum ether fraction.n-Butanol fraction of T.triquetrum had the stronger inhibition activity againstα-glucosidase(IC 50 toα-glucosidase from yeast andα-glucosidase from small intestine in mice were 13.08±1.23 and 221.21±3.75μg/mL,respectively)than other fractions and reference substance acarbose(P<0.05).Kinetic analysis showed that the inhibitory mechanism of n-butanol fraction onα-glucosidase was competitive inhibition.The n-butanol fraction from the T.triquetrum exhibited the highestα-glucosidase inhibitory activities,indicated that it was a good source of nature could be used as the main active fractions to excavate active substances for inhibition activity onα-glucosidase.
作者
何贝桥
张园园
庄远杯
魏爱红
李榕娣
张声源
HE Bei-qiao;ZHANG Yuan-yuan;ZHUANG Yuan-bei;WEI Ai-hong;LI Rong-di;ZHANG Sheng-yuan(Department of Chinese Medicine,Beijing University of Chinese Medicine,Beijing 100049,China;Guangdong Provincial Key Laboratory of Conservation and Precision Utilization of Characteristic Agricultural Resources in Mountainous Areas;Institute of Hakka Medicinal Bio-resources,Medical College,Jiaying University,Meizhou 514031,China)
出处
《天然产物研究与开发》
CAS
CSCD
北大核心
2020年第12期2026-2030,共5页
Natural Product Research and Development
基金
国家自然科学基金青年基金(81703662)
广东省科技计划(2014A020221061,2015A090905019)
广东省高等教育“冲补强”提升计划重点建设学科(农业资源与环境)建设项目(粤教科函[2018]181号)。
关键词
葫芦茶
Α-葡萄糖苷酶
酶促反应动力学
竞争性抑制
Tadehagi triquetrum(L.)Ohashi
α-glucosidase
enzymatic reaction kinetics
competitive inhibition
