【作者】 唐万侠； 朱吕会； 王金兰； 赵明； 张文治； 张树军； 福山爱保；

【Author】 TANG Wan-Xia1,3, ZHU Lv-Hui2, WANG Jin-Lan1, ZHAO Ming1, ZHANG Wen-Zhi1, ZHANG Shu-Jun1, Fukuyama Yoshiyasu3 (1. China, College of Chemistry and Chemical Engineering, Qiqihar University, Qiqihar, 161006; 2. Qiqihar Siyou Chemical Industry Co., Ltd., Qiqihar, 161000; 3. Japan, Faculty of Pharmaceutical, Tokushima Bunri University, Tokushima, 770-8514)

【机构】 齐齐哈尔大学化学与化学工程学院； 德岛文理大学药学部； 齐齐哈尔四友化工有限公司；

【摘要】 目的分离提取茯苓中神经伸展促进活性成分并讨论活性与结构之间的构效关系。方法利用PC12细胞测定生理活性,以萃取物的生理活性为导向,采用硅胶柱色谱和高效液相色谱法分离纯化茯苓的MeOH萃取物,并通过光谱数据解析对化合物进行结构鉴定。结果分离得到了7个羊毛甾烷型三萜化合物1-7。化合物1,2,and5-7在0.3-30.0μM浓度范围内,对神经生长因子诱导的PC12细胞显示出神经伸展促进活性。同时,构效关系讨论结果表明7位和9位上连接的二烯是这类化合物显示活性的关键基团。结论首次发现茯苓中的羊毛甾烷型三萜化合物具有神经伸展促进活性,证实了茯苓所具有的治疗神经疾患方面的药理作用,同时也为开发治疗老年痴呆症药物方面提供了理论依据。更多还原

【Abstract】 OBJECTIVE This research is to isolate the neurite outgrowth-promoting active components in Poria cocos and discuss the relationship between structure and activity. METHODS PC12 cells were used for the bioactivity experiment. The MeOH extract of P. cocos was separated and purified by column chromatography on silica gel and HPLC under the guidance of bioassay. The structures of isolated compounds were identified by chemical and spectroscopic analyses. RESULTS Seven lanostane type triterpenoids 1-7 were isolated from P. cocos. Compounds 1, 2, and 5-7 showed neurite outgrowth-promoting activity on NGF-mediated PC12 cells at concentrations ranging from 0.3 to 30.0 μM. The structure-bioactivity relationship discussion experiment indicated that the presence of 7,9-diene in the lanostane skeleton is presumed to be a crucial function for showing the activity of these triterpenoids. CONCLUSION It is the first time to find neurite outgrowth-promoting active triterpenoids from P. cocos. According, the presence of lanostane type triterpenoids found in this research would give a scientific proof to the nerve-related prescription of this plant.更多还原