中药牛蒡子中的α-葡萄糖苷酶抑制剂研究  

Study on α-glucosidase Inhibitors in Arctii Fructus

作　　者：张华婷 王源[1] 阮克锋[1] 徐朝晖[1] ZHANG Huating;WANG Yuan;RUAN Kefeng;XU Zhaohui(Engineering Research Center of Modern Preparation Technology of Traditional Chinese Medicine,Ministry of Education,Innovative Chinese Medicine,Research Institute,Shanghai University of Traditional Chinese Medicine,Shanghai 201203,China)

机构地区：[1]上海中医药大学创新中药研究院中药现代制剂技术教育部工程研究中心

出　　处：《中药新药与临床药理》2020年第2期163-168,共6页Traditional Chinese Drug Research and Clinical Pharmacology

基　　金：上海市科学技术委员会中药现代化科技支撑项目（12401900300）

摘　　要：目的研究中药牛蒡子中的α-葡萄糖苷酶抑制剂。方法以对α-葡萄糖苷酶的抑制活性为考察指标,结合植物化学的分离、纯化手段,追踪牛蒡子中的α-葡萄糖苷酶抑制剂,并通过波谱解析对所得活性化合物进行结构鉴定。α-葡萄糖苷酶抑制活性实验在以4-硝基酚-α-D-吡喃葡萄糖苷(PNPG)为底物的酶抑制剂筛选模型上进行,筛选出α-葡萄糖苷酶抑制活性较强的化合物后,通过考察它们对链脲佐菌素(STZ)诱导的糖尿病模型小鼠糖耐量的影响,最终确定牛蒡子中的α-葡萄糖苷酶抑制剂。结果从牛蒡子中α-葡萄糖苷酶抑制活性较强的部位分离得到13个化合物,其中4个咖啡酰奎宁酸类化合物和牛蒡苷元的α-葡萄糖苷酶抑制活性较为明确。经糖尿病模型小鼠的口服糖耐量(OGTT)实验验证后,3-O-咖啡酰奎宁酸、3,4-O-二咖啡酰奎宁酸、5-O-咖啡酰奎宁酸和牛蒡苷元与模型组比较,均能显著提高糖耐量(P<0.05),而3-O-咖啡酰奎宁酸的作用甚至强于阳性对照药(P<0.05)。结论咖啡酰奎宁酸类化合物是牛蒡子中主要的α-葡萄糖苷酶抑制剂。Objective To study α-glucosidase inhibitors in Chinese traditional medicine Arctii fructus.Methods According to the results of previous studies,the inhibitory activity on α-glucosidase was used as an indicator to investigate the fractions of 95% ethanol extract of seeds of Arctium lappa L.combined with phytochemical separation and purification methods to trace α-glucosidase inhibitor in Arctii fructus.Spectral analysis was carried out to identify the resulting active compounds with α-glucosidase inhibitory activity.The α-glucosidase inhibitory activity assay was performed on an enzyme inhibitor-screening model using 4-nitrophenol-α-D-glucopyranoside(PNPG) as substrate.After the compounds with strong α-glucosidase inhibitory activity were selected,the α-glucosidase inhibitors in the Arctii fructus were finally determined by examining their effects on glucose tolerance in Streptozotocin(STZ)-induced diabetic model mice.Results Thirteen compounds were isolated from Arctium lappa L.seeds with strong inhibitory activities on α-glucosidase,and the α-glucosidase inhibitory activities of 4 caffeoylquinic acid compounds and arctigenin were more certain.In oral glucose tolerance(OGTT) in diabetic model mice,3-O-caffeoylquinic acid,3,4-O-dicaffeoylquinic acid,5-O-caffeoylquinic acid and arctigenin significantly increased glucose tolerance(P<0.05 compared with the model group),while 3-O-caffeoylquinic acid was the most effective(P<0.05 compared with the positive drug group).Conclusion Through this experimental study,we found that caffeoylquinic acid is the main α-glucosidase inhibitor in Arctii fructus.

关 键 词：牛蒡子 Α-葡萄糖苷酶 抑制活性 咖啡酰奎宁酸类化合物 4-硝基酚-α-D-吡喃葡萄糖苷 

分 类 号：R285.5[医药卫生—中药学]