Research Center of New Drug Development, Guangzhou University of Chinese Medicine, Guangzhou 510006, China.
Chin J Integr Med. 2013 Mar;19(3):206-11. doi: 10.1007/s11655-012-1098-7. Epub 2012 Aug 18.
To investigate the absorption and transport mechanism of magnolol in Caco-2 cell model.
A human intestinal epithelial cell model Caco-2 cell in vitro cultured was applied to study the absorption and transport of magnolol, the effects of time, donor concentration, P-gp inhibitor verapamil, pH and temperature on the absorption and transport of magnolol were investigated. The determination of magnolol was performed by high performance liquid chromatography, then the values of apparent permeability coefficient (P app ) and P ratio Basolateral-to-Apical (BL-to-AP)/Apical-to-Basolateral (AP-to-BL) were calculated.
In Caco-2 cell model, comparing the amounts of transport of AP-to-BL and BL-to-AP, the latter was larger. At the same donor concentration, either the amounts of transport of AP-to-BL or BL-to-AP increased with increase in donor concentration and incubation time. Verapamil could significantly improve the amounts of transport of AP-to-BL. The transport of AP-to-BL and BL-to-AP depended on temperature, and there was no significant effect of pH on the transport of AP-to-BL.
Magnolol could be transported through the intestinal mucosa via a passive diffusion mechanism primarily, coexisting with a carrier-mediated transport, at the same time, the efflux mechanism could be involved.
研究厚朴酚在 Caco-2 细胞模型中的吸收和转运机制。
采用体外培养的人肠上皮细胞模型 Caco-2 细胞，研究厚朴酚的吸收和转运，考察时间、供体浓度、P-糖蛋白抑制剂维拉帕米、pH 值和温度对厚朴酚吸收和转运的影响。采用高效液相色谱法测定厚朴酚的含量，计算表观渗透系数（P app ）和 P 比值 Basolateral-to-Apical（BL-to-AP）/Apical-to-Basolateral（AP-to-BL）。
在 Caco-2 细胞模型中，比较 AP-to-BL 和 BL-to-AP 的转运量，后者较大。在相同的供体浓度下，AP-to-BL 或 BL-to-AP 的转运量均随供体浓度和孵育时间的增加而增加。维拉帕米可显著增加 AP-to-BL 的转运量。AP-to-BL 和 BL-to-AP 的转运依赖于温度，pH 值对 AP-to-BL 的转运没有显著影响。
厚朴酚主要通过被动扩散机制通过肠黏膜转运，同时存在载体介导的转运，可能涉及外排机制。
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