目的研究脱水穿心莲内酯(DAL)在Caco-2细胞单层模型中的吸收机制。方法观察DAL在Caco-2细胞单层模型中的双向转运,考察时间、DAL浓度、温度和P-糖蛋白(P-gp)抑制剂维拉帕米对DAL吸收的影响。采用LC/MS/MS方法检测DAL浓度,计算其表观渗透系数(Papp)。结果 DAL在Caco-2细胞模型中的双向转运,随时间和浓度的增加,DAL的吸收具有时间、浓度依赖性,未出现饱和趋势;不受温度和P-gp抑制剂维拉帕米的影响。结论 DAL在Caco-2细胞模型中的吸收主要是靠浓度扩散的被动转运。

To study the absorption mechanism of dehydroandrographolide (DAL) in human Caco₂ cell monolayer model. Methods Caco₂ cell monolayer model was applied to investigate the bidirectional transport of DAL. The effects of time, drug concentration, temperature, and P-gp inhibitor (Verapamil) on the absorption of DAL were observed. Drug concentration was measured by LC/MS/MS and the apparent permeability coefficients (Papp) were calculated. Results With the time and concentration increasing, the bidirection transport of DAL in Caco₂ cell monolayer model was of time and concentration dependence, without saturation. And it was not influenced by the change of temperature and the presence of Verapamil. Conclusion The absorption and transport of DAL are passive diffusion as the dominating process in Caco₂ cell monolayer model.

国家自然科学基金资助项目(30600823)