大黄有效成分与附子有效成分配伍在Caco-2细胞模型上的转运分析

目的:研究大黄中大黄酸、大黄素,附子中去甲乌药碱,以及大黄酸、大黄素与去甲乌药碱分别配伍后在Caco-2细胞模型上的转运过程。方法:以大黄酸、大黄素、去甲乌药碱的累积转运量及表观渗透系数(Papp)为指标,采用HPLC对大黄酸、大黄素、去甲乌药碱的含量进行检测,考察大黄酸、大黄素、去甲乌药碱在Caco-2细胞上的转运行为,以及大黄素、大黄酸分别配伍去甲乌药碱后转运行为的变化情况。结果:不同浓度去甲乌药碱的Papp均1×10-7cm·s-1,外排与吸收比值接近1.5,配伍大黄酸、大黄素后去甲乌药碱的Papp显著上升(P0.05)。大黄酸、大黄素配伍去甲乌药碱后前二者的Papp显著下降(P0.05)。结论:去甲乌药碱是1个中等吸收的药物,其吸收方式主要为被动转运。大黄中大黄酸、大黄素可促进附子中去甲乌药碱的在肠吸收,而去甲乌药碱却会抑制大黄酸、大黄素的在肠吸收。

Transport Analysis of Active Ingredients Compatibility Between Aconiti Lateralis Radix Praeparata and Rhei Radix et Rhizoma in Caco-2 Cell Model

Objective: Transport behaviors of rhein and emodin in Rhei Radix et Rhizoma and higenamine in Aconiti Lateralis Radix Praeparata were studied on Caco-2 cell model,and the change of transport behaviors after the compatibility of rhein,emodin with higenamine was inspected. Method: HPLC was used to analyzed the concentration of rhein,emodin and higenamine,then apparent permeability coefficients (P_app) and cumulative transport amounts were calculated.So as to investigate the bi-directional transport behavior of rhein,emodin and higenamine on Caco-2 cell,as well as the change of the transport behaviors of emodin and rhein. Result: P_app of higenamine with different concentrations was >1×10^-7 cm · s^-1,the ratio of permeability in the basolateral to apical direction was about 1.5 times that of the apical to basolateral direction.The transport amount of higenamine was significantly (P<0.05) increase in the presence of rhein and emodin.Whereas the transport amount of rhein and emodin was significantly (P<0.05) decrease in the presence of higenamine. Conclusion: Higenamine can be mediumly absorbed on the Caco-2 monolayer model by a passive transportation.Rhein and emodin can promote the intestinal absorption of higenamine,but higenamine can inhibit the intestinal absorption of rhein and emodin.