采用双靶点筛选体系从中药中寻找治疗糖尿病及代谢综合症的活性物质

项目名称： 采用双靶点筛选体系从中药中寻找治疗糖尿病及代谢综合症的活性物质

项目编号： No.81001611

项目类型： 青年科学基金项目

立项/批准年度： 2011

项目学科： 化学工业

项目作者： 李晓帆

作者单位： 清华大学

项目金额： 10万元

中文摘要： 围绕中药番石榴叶中降糖降脂的活性成分展开研究，主要研究进展如下：1）使用两种不同提取分离方法对番石榴叶进行活性成分研究，分离得到共27个化合物。通过各种现代波谱学手段并结合理化方法鉴定了全部27个化合物的结构，其中5个为新化合物，5个为首次从该属植物中分离得到。2）使用多种方法测定化合物活性，活性测试结果显示7种黄酮类化合物（16-21、25）具有中、强抗氧化活性，三萜类化合物（16-26）无抗氧化活性。使用FMCA法测定了各单体化合物的细胞毒活性。活性结果显示，7种三萜类化合物（16-21、25）具有较强细胞毒活性，黄酮，酚酸类化合物（1-15）在25μmL浓度下无细胞毒活性。对化合物进行PPARγ28608;动活性及MAPK活性测试，化合物21、24显示较强活性，提示三萜类化合物作为新型天然胰岛素增敏剂的可能性。对黄酮类化合物6、8进行了分子及细胞领域活性探讨。3）进行质量监控方法的研究，采用中药指纹图谱的方式对峰面积>5%的单峰，78%以上的总峰进行指认，并以其中的活性成分为指标进行质量控制，为开发新型的、天然的降糖活性保健品和药物提供理论依据。

中文关键词： 番石榴叶；糖尿病；活性；三萜；黄酮；

英文摘要： In this study, two different method of activity-guided isolation targeting antioxidative and PPARγxciting activity on Traditional Chinese Medicine (TCM) Psidium guajava L. was carried out. 27 compounds were yielded and their structures were elucidated, of which 5 were new compounds and 5 were the new isolation from Psidium genus. Several assays were performed on the isolated fractions and compounds, of which 8 flavonoid derivatives and 7 triterpene derivatives expressed antioxidative and cytotoxic activities, respectively. Compounds 21 and 24 showed activities against PPARγnd MAPK activities, suggesting the potent possibility of triterpene derivatives to act as a new series of insulin sensitizers from natural resources. Preliminary research on medicinal material quality standard of P. guajava was performed. The HPLC fingerprint of P. guajava was established by LC-MS experiments.Single chromatographic peak of >5% peak area, as well as total peaks which occupied >78% peak area were identified.These active components could be used as quality index for control.This study provided theoretical and experimental basis for the development and utilization of TCM, and also provided the basis for the application of this plant.

英文关键词： psidium guajava L.;diabetes; activity; triterpene; flavonoid