UHPLC-QTOF-MS^E与UHPLC-MS/MS分析麻黄生物碱在血脑屏障间的移行及脑区分布特征  

Study of brain distribution of Ephedra alkaloids based on UHPLC-QTOF-MS^E and UHPLC-MS/MS method

作　　者：彭秘 苏丹[1] 李晗芸 冯冰薇 徐鹏飞 宋永贵[1] PENG Mi SU Dan LI Han-yun FENG Bing-wei XU Peng-fei SONG Yong-gui(Jiangxi University of traditional Chinese Medicine, Nanchang 330006, Chin)

机构地区：[1]江西中医药大学,江西南昌330006

出　　处：《药学学报》2017年第9期1437-1443,共7页Acta Pharmaceutica Sinica

基　　金：江西省自然科学基金资助项目(20142BAB215064;20171BAB205092)

摘　　要：利用超高效液相色谱-质谱(UHPLC-MS)联用技术,建立麻黄生物碱同分异构体的UHPLC分离方法,定性分析麻黄生物碱移行入血与入脑成分,定量测定并比较麻黄生物碱在血脑屏障间的分布情况,并获得在大鼠中枢神经系统不同部位(大脑皮层、小脑、海马、纹状体、延髓和下丘脑)的分布特征与差异。研究表明,麻黄碱、伪麻黄碱、去甲基麻黄碱、去甲基伪麻黄碱和甲基麻黄碱(甲基伪麻黄碱)经胃肠吸收后可通过血脑屏障快速入脑,定量测定结果显示,麻黄生物碱主要分布在大脑皮层、海马区域,其次为下丘脑、纹状体与小脑,最少分布在延髓部位。不同生物碱的血脑屏障分布情况:以AUC_(0-t,brain)/AUC_(0-t,blood)计,麻黄碱类>甲基麻黄碱类>去甲基麻黄碱类。麻黄生物碱能够在血脑屏障间快速分布,在中枢系统分布具有组织趋向性,不同生物碱的血脑分布情况具有差异性。本文为中药麻黄的中枢作用机制研究提供了物质效应部位与依据。Using ultra high performance liquid chromatography（UHPLC） coupled with mass spectrum（MS） technology, a method has been established for separation and analysis of alkaloid isomers. Alkaloids in Ephedra sinica transitionally crossed blood brain barrier（BBB） and the distribution were investigated. The concentrations of Ephedra alkaloids in rat central nervous system（CNS） were determined to acquire the distribution characteristics and differences in cerebral cortex, cerebellum, hippocampus, striatum, medulla oblongata and hypothalamus. It was founded that pseudoephedrine, norephedrine, norpseudoephedrine, methylephedrine（methylpseudoephedrine） were able to cross BBB fast via gastro-intestinal tract after administrated with Ephedra sinica. Cortex and hippocampus was the main distribution region, followed by hypothalamus, striatum and cerebellum, in which medulla oblongata had the least. The distribution of various alkaloids, as AUC_（0-t, brain）/AUC_（0-t, blood） was ephedrine methylephedrine demethyl ephedrine. Alkaloids in Ephedra sinica crossed BBB rapidly, showing the regional distribution tendency in central nervous system, and the distribution was diversity. This group of data provides distribution of bioactive constituents of Ephedra in CNS.

关 键 词：麻黄 生物碱 中枢系统 UHPLC-QTOF-MSE UHPLC-MS/MS 

分 类 号：R917[医药卫生—药物分析学]