中文摘要
随着人口老龄化程度的加速,与年龄相关的神经退行性病变(如阿兹海默症、帕金森病等),对人类的身心健康的危害日趋严重,寻找其有效的治疗药物迫在眉睫。Majucin型倍半萜内酯类化合物是八角属植物中发现的一类结构独特,神经营养活性显著的天然产物,可用于保护脑细胞免受神经退行性疾病和脑损伤的恢复治疗。前期研究我们发现八角属植物假地枫皮果实中含有丰富的Majucin型倍半萜内酯类化合物,并分离得到了1个含量较高且具有显著神经营养活性的化合物。本项目拟在此基础上,通过活性追踪对二种八角属植物(大八角和小花八角)展开深入的活性成分研究,并对前期发现的有进一步研究价值的先导化合物进行结构修饰和改造,探讨该类化合物神经营养活性的构效关系,以期发现更具有成药性的神经营养活性化合物,这将对创新药物的研究以及八角属植物资源的开发利用具有重要意义。
英文摘要
Neurodegenerative diseases (such as: AD、PD) are closely associated with the accelerating population aging, resulting in serious human's physical and mental problem. It becomes important to search the effective drug to treat these diseases. Majucin type sesquiterpene lactones are a series of natural products derived from genus illicium linn with special structures and remarkable neurotrophic activity. These products are mainly used for the reparative therapy of brain cells in neurodegenerative disease and brain damage. Previously, we found that the fruit of jiadifengpi, derived from genus illicium linn, was rich of Majucin type sesquiterpene lactones and we also isolated a compound from this plant with high yield and noteworthy neurotrophic activity. The current study is designed to conduct detail chemical composition research from two genus illicium linn plants (L. majus and L. micranthum), further perform structural modification of the lead compound and explore structure-activity relationship of these compounds. We are hoping to discover a novel series of compound with high drug-promising quality, which have the great significance to the research of innovative drugs and the development and utilization of genus illicium inn.
