[关键词]
[摘要]
目的 研究杜仲Eucommia ulmoides不同部位提取物中的主要成分,并对其降血糖活性进行研究,阐明其降血糖的药效物质基础。方法 基于HPLC-Q-TOF-MS技术研究杜仲中主要类型化合物的质谱裂解规律,基于质谱裂解规律结合质谱挖掘技术对杜仲不同部位提取物中的活性成分进行系统鉴定,并基于糖尿病小鼠模型对杜仲不同部位提取物及主要成分降血糖活性进行评价。结果 阐明了杜仲中环烯醚萜、呋喃型木脂素、黄酮及多酚类化合物的质谱裂解规律,构建了杜仲植株中化合物的挖掘方法,从杜仲的皮、叶、枝、根中共鉴定了60个化合物,包括环烯醚萜类化合物17个、呋喃型木脂素类化合物13个、黄酮类化合物18个、多酚类化合物10个、其他类型化合物2个。其中25个化合物首次在杜仲中报道。杜仲枝提取物及其主要成分(化合物27 ,京尼平苷)表现出显著的降血糖活性,使小鼠血糖水平从最初的(26.33±0.57)、(25.34±0.24)mmol/L分别下降到(20.56±1.23)、(21.56±1.56)mmol/L。杜仲枝提取物及化合物27 还能改善糖尿病引起的多饮、多食及体质量减轻的症状。结论 环烯醚萜、呋喃型木脂素、黄酮及多酚类化合物为杜仲中主要成分,且杜仲枝提取物及其主要成分-京尼平苷具有显著的降血糖活性,具有开发成为降血糖药物的潜力。
[Key word]
[Abstract]
Objective To identify the chemical constituents in extracts from different parts of Eucommia ulmoides and investigate its hypoglycemic activities. Methods High performance liquid chromatography-tandem quadrupole time-of-flight mass spectrometry (HPLC-Q-TOF-MS) was applied to profile the mass fragmentation pattern of chemical constituents in E. ulmoides, and the active ingredients in extracts from different parts of E. ucommia were identified based on the well-established mass fragmentation pattern combined with mass spectrometry mining technology. The main identified components in extracts from different parts of E. ulmoides were evaluated for the hypoglycemic effect in a hyperglycemia mouse model. Results The mass fragmentation pathways of iridoids, furanoid lignans, flavonoids and polyphenols in E. ulmoides were clarified to establish the mining technology of compounds in E. ulmoides. Sixty compounds, including 17 iridoids, 13 furanoid lignans, 18 flavonoids, ten polyphenols, and two others, were identified or tentatively characterized from the roots, stems, leaves and bark of E. ulmoides. A total of 25 compounds were reported for the first time. The dominant component from the twig extract, geniposide, exhibited significant hypoglycemic activity by lowering blood glucose levels from (26.33±0.57) and (25.34±0.24) mmol/L to (20.56±1.23) and (21.56±1.56) mmol/L, respectively. Diabetes-related symptoms, such as polydipsia, polyphagia, and weight loss, were alleviated after administering geniposide and the total twig extract. Conclusion Iridoids, furanoid lignans, flavonoids and polyphenols are the main components of E. ulmoides. The extract of E. ulmoides twig and its main component, geniposide, have significant hypoglycemic activity, providing further insights into their potential as bioactive hypoglycemic components.
[中图分类号]
R284.1;R285
[基金项目]
杜仲综合利用技术国家地方联合工程实验室开放项目(NLE201608)