麻黄挥发油对麻黄碱和伪麻黄碱经Caco-2细胞转运特征的影响

Effects of Essential Oils in Ephedra on Intestinal Transport Characteristics of Ephedrine and Pseudoephedrine by Caco-2 Cell Model

目的:基于“性味药理”研究思路,选取麻黄挥发油和生物碱作为其辛温解表主要功效成分,从药物吸收转运角度研究麻黄解表发散的作用原理。方法:采用Caco-2细胞转运模型,HPLC同步对比分析麻黄挥发油加入对麻黄碱和伪麻黄碱从板顶端(AP)→底端(BL)及BL→AP的双向转运过程的影响,计算表观渗透系数,并分析挥发油对其转运特征的影响。结果:麻黄碱和伪麻黄碱的Caco-2细胞表观渗透系数(Papp)与浓度无显著关系。麻黄碱的Papp(AP→BL)约为19×10^-6 cm·s^-1,伪麻黄碱的Papp(AP→BL)约为16×10^-6 cm·s^-1,吸收作用均较好,外排率均值为0.72,推测其转运过程主要为被动转运过程。麻黄挥发油促进麻黄碱和伪麻黄碱的转运吸收,其对伪麻黄碱促进吸收作用更为显著。结论:挥发油和生物碱在麻黄解表发散功效可能存在协同作用。

Objective:To select essential oil and alkaloids as the bioactive components from the perspective of nature and flavor pharmacology and to measure the effect of release the exterior with pungent-warm by drug transport.Methods:The transport characteristics of ephedrine and pseudoephedrine were compared when combined with essential oil using Caco-2 cell model.And then the values of apparent permeability coefficient(Papp)of both Basolateral-to-Apical side(BL-to-AP)and Apical-to-Basolateral side(AP-to-BL)were calculated by HPLC.Results:No significant correlation was found between Pappand drug concentrations.Papp(AP→BL)of ephedrine and pseudoephedrine was about 19×10^-6 cm·s^-1 and 16×10^-6 cm·s^-1,respectively.The data indicated that ephedrine and pseudoephedrine had good intestinal permeability with the efflux ratio of 0.72 and their transport across the gut wall probably mediated by passive diffusion.Essential oil could significantly improve the intestinal absorption of alkaloid,especially pseudoephedrine.Conclusion:The effect of promoting sweating to release the exterior may occur by the synergistic action of both essential oil and alkaloids.