辛夷中肉桂酸单萜酯类成分及其肥大细胞脱颗粒抑制活性研究  

Study on cinnamic acid monoterpene esters in Magnolia biondii Pamp. and its mast cell degranulation inhibitoion activity

作　　者：张行[1] 钱菲 毛高慧 郭夫江[1] 陈凯先[1] 李医明[1] ZHANG Xing;QIAN Fei;MAO Gao-hui;GUO Fu-jiang;CHEN Kai-xian;LI Yi-ming(Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China)

机构地区：[1]上海中医药大学,上海201203

出　　处：《中华中医药杂志》2018年第5期1763-1768,共6页China Journal of Traditional Chinese Medicine and Pharmacy

基　　金：上海市优秀学术带头人项目(No.16XD1403500);国家自然科学基金项目(No.81673570;No.81261120567)~~

摘　　要：目的:研究辛夷Magnolia biondii Pamp.中的肉桂酸单萜酯类成分及其肥大细胞脱颗粒抑制活性。方法:利用硅胶、反相硅胶柱色谱以及半制备HPLC等手段进行分离纯化,利用化学合成的方法获得衍生物,并通过MS和NMR等波谱技术进行化合物结构鉴定,采用β-hex释放抑制实验测试分离得到的化合物及合成衍生物的肥大细胞脱颗粒抑制活性。结果:从辛夷中分离得到肉桂酸单萜酯类成分6个(化合物1-6),其中化合物2、3、6对肥大细胞脱颗粒具有一定的抑制作用;合成的衍生物中,7个(化合物7、8、9、10、11、12、13)对肥大细胞脱颗粒具有较好的抑制活性且比天然产物效果要好。结论:首次从辛夷中分离得到肉桂酸单萜酯类成分化合物1-6,首次报道了肉桂酸单萜酯类成分的肥大细胞脱颗粒抑制活性并总结了构效关系。Objective： To study the cinnamic acid monoterpene esters in Magnolia biondii Pamp. and its mast cell degranulation inhibition activity. Methods： The compounds of Magnolia biondii Pamp. were isolated and purified by using the methods of silica gel column chromatography, anti-phase silica gel column chromatography and semi-preparative HPLC, and the derivatives were obtained by chemical synthesis. And their structures were identified by means of spectral analyses including MS and NMR. Then, their mast cell degranulation inhibition activity of the compounds and synthetic derivatives were detected by the β-hex release inhibition experiment. Results： Six compounds（1-6） like cinnamic acid monoterpene esters were obtained from Magnolia biondii Pamp., the three compounds（2, 3, 6） had certain inhibition effects on mast cell degranulation. Seven synthetic derivatives（7, 8, 9, 10, 11, 12, 13） had better inhibition activity effects on mast cell degranulation than that of natural products. Conclusion： The compounds 1-6 including cinnamic acid monoterpene esters were initially separated and obtained from Magnolia biondii Pamp., and the mast cell degranulation inhibition activity of cinnamic acid monoterpene esters and the structure-activity relationship were first reported and concluded in this paper.

关 键 词：辛夷 肉桂酸单萜酯 肥大细胞脱颗粒抑制活性 抗过敏 

分 类 号：R284[医药卫生—中药学] R285[医药卫生—中医学]