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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10~200μmol.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 effects of three alkaloids, l-ephedrine (LEP), d-pseudoephedrine (DPEP) and d-norpseudoephedrine (DNPE) -2 cell monolayer model. Methods: The monolayer model of human colon adenocarcinoma cell line Caco-2 was used to test the transport process of LEP, DPEP and DNPE from villus surface (AP end) to basal surface (BL end) and BL end to AP end. The three alkaloids were quantitatively analyzed by reversed-phase high performance liquid chromatography coupled with ultraviolet detector to calculate the transport parameters and apparent permeability coefficient (Papp), and with the positive control drugs propranolol and atenolol The comparison. Results: The Papp of bidirectional transport of LEP, DPEP and DNPE was on the order of 1.0 × 10-5cm · s-1, which was an order of magnitude higher than that of propranolol on the Caco-2 cell monolayer model. The transport efficiency and concentration of 3 alkaloids at 10 ~ 200μmol.L-1 were positively correlated. Conclusion: LEP, DPEP and DNPE can passively enter the body through intestinal epithelial cells and become well-absorbed compounds.