藏药绿萝花化学成分及降糖生物活性的研究

With the socioeconomic development, the improvement of living standard and the changes of dietary ingredient, diabetes metllitus becomes more prevalence and the incidence of this disease rises year after year. To prevent and remedy diabetes mellitus is a remarkable topic. The flower of Edgeworthia gardneri is peculiar in Tibet and the local residents usually drink tea of flower of Edgeworthia. for treatment of diabetes. Previous studies revealed that flower of Edgeworthia. significantly decrease the blood glucose levels in our group and other groups and it is very suitable to be developed into anti-diabetic drugs. Although the flower of Edgeworthia. has been used as anti-diabetic drugs for long time and has significant hypoglycemic activity, the active chemical constituents and mechanism are unknown. In addition, the hypoglycemic activity of flower of Edgeworthia.. is only about the crude extract. Thus, it is necessary to clearly explain the hypoglycemic chemical constitutes and mechanism of flower of Edgeworthia.. The search for the constituents reducing α-glucosidase activity based on previous studies will lead to the finding of active compounds in the flower of Edgeworthia gardneri. The active fractions were separated by different methods, such as HPLC and recrystallization and the compounds will be identified by means of NMR, MS, IR, UV, and CD. Then, the compounds will be evaluated hypoglycemic activity and mechanism by in vitro and in vivo. Finally, the clear hypoglycemic chemical constituents and mechanism provide basis in developing new anti-diabetic drugs.

随着社会经济的发展、人们生活水平的提高和饮食结构的变化，糖尿病的患病呈流行趋势，发病率逐年上升，预防和治疗糖尿病成为热门话题。藏药绿萝花是西藏地区特有的民族特色习用药材，西藏当地将绿萝花通过泡水饮用的方式来治疗糖尿病。本课题组及其他课题组研究表明绿萝花能显著降低血糖浓度，非常适合开发成为降糖药物。尽管绿萝花用药历史悠久，降血糖活性显著，但是其有效成分与作用机理却并不明确，降糖活性仅仅是对绿萝花粗提物的研究。因此，有必要阐明绿萝花中降血糖活性的药效物质基础及其作用机制。本项目将在本课题组前期研究基础上，以α-葡萄糖苷酶为靶标，活性跟踪为导向，综合各种分离手段，分离纯化活性组分，得到单体化合物，借助现代波谱学技术进行化合物的结构鉴定。对分离得到的单体化合物进行体外与体内实验，进行降糖活性评价与机理研究，阐明绿萝花的药效活性物质基础，为新型降糖药物的研发提供先导化合物。

藏药绿萝花为瑞香科结香属植物滇结香（Edgeworthia gardneri）的花蕾，是西藏地区特有的民族特色习用药材，西藏当地将绿萝花通过泡水饮用的方式来治疗糖尿病、高血脂等慢性疾病。本文以西藏绿萝花为研究对象，综合运用各种色谱技术对其甲醇提取物的乙酸乙酯部分进行了系统的化学成分研究，共分离得到30个化合物，包括3个新化合物，采用现代波谱技术（NMR，MS，IR，UV）和X-ray单晶衍射等方法对其进行了结构鉴定，分别为12个香豆素类、7个黄酮类、6个苯丙素类、2个木脂素类化合物以及3个苯的衍生物。对化合物进行了α-糖苷酶、葡萄糖吸收、淀粉酶、醛糖还原酶、抗氧化以及动物实验等方面的研究。对藏药绿萝花进行系统的化学成分研究，得到30个单体化合物（包括3个新化合物），对单体化合物进行了α-糖苷酶、葡萄糖吸收、淀粉酶、醛糖还原酶、抗氧化以及动物降血糖实验等方面的研究，初步阐明绿萝花的降糖活性物质基础和作用机理，为绿萝花进一步的开发利用提供了科学依据。