乌头碱在Caco-2细胞模型上的转运行为

目的:研究乌头碱在Caco-2细胞模型上的转运行为。方法:采用MTT法确定乌头碱在Caco-2细胞转运过程中的安全浓度范围,以乌头碱累积转运量及表观渗透系数Papp为指标,采用高效液相色谱法对成分进行检测,考察不同浓度、不同孵育时间乌头碱在Caco-2细胞模型上的双向转运。结果:乌头碱累积转运量与孵育时间、给药浓度呈正相关,不同浓度乌头碱Papp保持恒定,无统计学差异,且外排作用明显强于吸收,外排比接近1.5,Papp约为1×10-5cm·s-1。结论:乌头碱以被动转运为主,且可能存在外排蛋白的参与,为吸收良好的一类药物。

Transport Behavior of Aconitine in Caco-2 Cell Monolayer Model

Objective: To study the transport behavior of aconitine in the Caco-2 cell monolayer model. Method: MTT method was employed to confirm the safe concentration of aconitine towards Caco-2 cell.Aconitine concentrations in the samples were analyzed by high performance liquid chromatography (HPLC).The apparent permeability(P_app)value and the total amount of transport were calculated. Bi-direction transport behavior of aconitine by incubating in different concentration and time were studied. Result: The transport amount of aconitine was positively correlated with the incubation time and drug concentration on the Caco-2 monolayer model. The P_app values in both apical to basal (AP-BL)and basal to apical (BL-AP) directions were stable with no significant differences in selected concentrations. The BL-AP flux of aconitine was more than 1.5-fold higher than AP-BL flux(P_app 1×10^-5cm·s^-1). Conclusion: The results suggested that the aconitineis well absorbed through the Caco-2 monolayer model by a passive transportation. Besides, efflux protein may be involved in the transport process.