蛇床子素在Caco-2细胞模型中的转运机制研究

Study on Transport Mechanisms of Osthol in Caco-2 Cell Model

目的研究蛇床子素在Caco-2细胞模型中的转运机制。方法通过研究蛇床子素在Caco-2细胞模型中的转运,考察蛇床子素浓度、PEG600、P-gp抑制剂维拉帕米(verapamil)及温度对蛇床子素转运的影响。结果随着蛇床子素溶液浓度和温度的升高,蛇床子素在Caco-2细胞中AP-BL的转运量增加;PEG600对蛇床子素在Caco-2细胞中的AP-BL的转运量有显著增加;P-gp抑制剂维拉帕米对蛇床子素在Caco-2细胞中转运的表观通透系数PAP和PBL无显著影响。结论蛇床子素表观通透系数PAP大于10×10-6cm.s-1,较易被Caco-2细胞吸收,但由于3个浓度蛇床子素溶液的PAP和PBL比值无明显变化、P-gp抑制剂对PAP和PBL无明显影响及转运的活化能较低(17.31 kJ.mol-1),因此,蛇床子素在Caco-2细胞模型中的转运机制主要是被动转运。

OBJECTIVE To study the transport mechanisms of osthol by using Caco-2 cell model. METHODS The effect of concentration, PEG600, verapamil （P-gp inhibitor）and temperature on transport of osthol in Caco-2 cell model was studied. RESULTS Osthol amount transported in the apical（AP） to basolateral（BL） in Caco-2 cell cell model was increased with loading concen- tration and temperature. PEG600 enhanced the rate of osthol transport. The PAP and PBLOf osthol in Caco-2 model were not affected by verapamil. CONCLUSION The PAP of osthol in Caco-2 model was above 10 x 10-6 and osthol was absorbed easily by Caco-2 cell. Further, there were no significant differences in the ratios of P^L to PAP at three concentrations. Activation energy was quite moderate at 17. 31 kJ · mol^-1. The ratio of PBL to PAP of osthol transport were not affected by verapamil, suggesting that the absorption is via passive diffusion.