枇杷叶中三萜酸类成分及其抗炎、镇咳活性研究  

Studies on constituents of triterpene acids from Eriobotrya japonica and their anti-inflammatory and antitussive effects

作　　者：鞠建华[1] 周亮[1] 林耕[1] 刘东[1] 王立为[1] 杨峻山[1] 

机构地区：[1]中国协和医科大学-中国医学科学院药用植物研究所,北京100094

出　　处：《中国药学杂志》2003年第10期752-757,共6页Chinese Pharmaceutical Journal

基　　金：国家科技部重点科技项目 (攻关 )计划 ;中药现代化研究与产业化开发项目-常用中药化学成分及其有效成分的研究 (No :99 92 9 0 1 3 4)资助项目

摘　　要：目的　对常用中药枇杷叶 [Eriobotryajaponica (Thunb .)Lindl.]的化学和药效学进行研究 ,寻找与其功能主治相吻合的有效成分。方法　利用溶剂提取、萃取、柱色谱和化学衍生化方法进行分离 ,根据化合物的光谱数据 (IR ,MS ,1H NMR ,13 C NMR)和理化性质鉴定其结构 ;根据其功能主治设计抗炎、镇咳药效学模型 ,对其萃取部位和所得单体成分进行抗炎、镇咳活性研究。结果　枇杷叶乙醇提取物的醋酸乙酯和正丁醇萃取物对二甲苯引起的小鼠耳肿胀有明显抑制作用 ,对枸橼酸喷雾引起的豚鼠咳嗽有明显的止咳作用。从正丁醇萃取物中分离得到 6个三萜酸类化合物 ,分别鉴定为齐墩果酸 (oleanolicacid ,Ⅰ ) ,2α 羟基齐墩果酸 (maslinicacid ,Ⅱ ) ,乌苏酸 (ursolicacid ,Ⅲ ) ,2α 羟基乌苏酸 (2α hydroxyursolicacid ,Ⅳ ) ,坡模酸 (pomolicacid ,Ⅴ )和蔷薇酸 (euscaphicacid ,Ⅵ ) ,其中坡模酸系首次从该植物中分离得到。乌苏酸、2α 羟基齐墩果酸和总三萜酸对二甲苯引起的小鼠耳肿胀显示很强的抗炎活性 ;乌苏酸和总三萜酸还对枸橼酸喷雾引起的豚鼠咳嗽有止咳作用。结论　枇杷叶中的三萜酸类成分是与其功能主治相吻合的活性成分 ,其中含量较高的乌苏酸可作为评价枇杷叶药材质量的指标性成分。OBJECTIVE: To investigate the effective chemical constituents of traditional Chinese medicine Eriobotrya japonica. METHODS: The plant material was extracted with ethanol, the extract was suspended in water, partitioned successively with petroleum ether, EtOAc, and n-BuOH. The compounds were isolated by various column chromatography and identified by their spectral data (IR, MS, 1H-NMR, 13C-NMR) and physicochemical properties respectively. According to the clinical efficacy of E. japonica, both anti-inflammatory and antitussive models were established for pharmacological evaluation of its fractionated extracts and constituents isolated. RESULTS: The EtOAc and n-BuOH-soluble fractions were found to show an anti-inflammatory effect on xylene-induced edema in mice as well as an antitussive effect on citric acid-induced cough on guinea pigs. Phytochemical investigation of the effective n-BuOH-soluble fraction resulted in isolation of six triterpene acids, identified as oleanolic acid (I), maslinic acid (II), ursolic acid (III), 2α-hydroxyursolic acid (IV). Pomolic acid (V), and euscaphic acid (VI) respectively. Pomolic acid was isolated from this plant for the first time. Ursolic acid, maslinic acid, and the total triterpene acids exhibited strong anti-inflammatory activity. Further more, Ursolic acid and the total triterpene acids also displayed antitussive activity. CONCLUSION: Triterpene acid components appeared to be responsible for the pharmacological activity and clinical efficacy of E. japonica. Ursolic acid, which has a large amount, could be suitable as a significant constituent for quality control of E. japonica.

关 键 词：枇杷叶 三萜酸类 抗炎活性 镇咳活性 中药 

分 类 号：R282.71[医药卫生—中药学]