麻黄生物碱在人源肠Caco-2细胞单层模型的吸收转运研究  

Absorption and transportation characteristic of alkaloids from Herba Ephedrae in model of Caco-2 cells monolayer

作　　者：廖音[1] 杨秀伟[1] 

机构地区：[1]天然药物及仿生药物国家重点实验室北京大学药学院天然药物学系,北京100191

出　　处：《中国中药杂志》2010年第22期3010-3015,共6页China Journal of Chinese Materia Medica

基　　金：国家"十一五"科技支撑计划项目(2006BAI06A01-02);天然药物及仿生药物国家重点实验室开放课题项目

摘　　要：目的：研究传统中药麻黄中左旋麻黄碱（l-ephedrine,LEP）、右旋伪麻黄碱（d-pseudoephedrine,DPEP）和右旋去甲伪麻黄碱（d-norpseudoephedrine,DNPE）3个生物碱在人源肠Caco-2细胞单层模型中的吸收特性。方法：利用人源结肠腺癌细胞系Caco-2细胞单层模型测试LEP,DPEP和DNPE从绒毛面（AP端）到基底面（BL端）、BL端到AP端2个方向的转运过程。应用偶联紫外检测器的反相高效液相色谱法对上述3个生物碱进行定量分析,计算转运参数和表观渗透系数（Papp）,并与阳性对照药普萘洛尔和阿替洛尔的进行比较。结果：LEP,DPEP和DNPE双向转运的Papp在1.0×10-5cm.s-1数量级,与在Caco-2细胞单层模型上呈良好吸收的普萘洛尔的Papp在一个数量级。3个生物碱在10200μmol.L-1的转运效率与浓度呈正相关。结论：LEP,DPEP和DNPE可以通过小肠上皮细胞被动吸收进入体内,为吸收良好的化合物。Objective： To study the absorption and transportation characteristic of l-ephedrine（LEP）,d-pseudoephedrine（DPEP）,d-norpseudoephedrine（DNPE） isolated from Herba Ephedrae,which were classified the alkaloids,in human intestinal epithelium.Method： Caco-2（the human colon adeno carcinoma cell lines） cells monolayer was used as an intestinal epithelial cell model.The permeability of the three alkaloids from apical side（AP side） to basolateral side（BL side） or from BL side to AP side was evaluated.The concentration of the three alkaloids was measured by HPLC coupled with UV detector.Transportation parameters and apparent permeability coefficients（Papp） were then calculated,and Papp values were compared with the reported values for model compounds,propranolol and atenolol.Result： The Papp values of the three alkaloids in the bi-directional transportation were quantitative degree of 1.0× 10-5 cm·s-1,which was comparable with the Papp value of propranolol,which is a transcellular transportation marker and a well-transported compound with a Papp≥1.0×10-5 cm·s-1.The absorption and transportation of the three alkaloids were positive correlation to the concentration of 10-200 mol·L-1.Conclusion： LEP,DPEP and DNPE can be absorbed across intestinal epithelial cells by passive diffusion mechanism,and are well absorbed compounds.

关 键 词：CACO-2细胞单层 麻黄 左旋麻黄碱 右旋伪麻黄碱 右旋去甲伪麻黄碱 肠吸收 表观渗透系数 

分 类 号：R285.5[医药卫生—中药学]