穿心莲内酯在Caco-2细胞单层模型中的吸收机制

Absorption mechanism of andrographolide in human Caco-2 cell monolayer model

目的研究穿心莲内酯在Caco-2细胞单层模型中的吸收机制。方法观察穿心莲内酯在Caco-2细胞模型中的双向转运,考察时间、药物浓度、温度和抑制剂对穿心莲内酯吸收的影响。用LC/MS/MS检测药物浓度,计算其表观渗透系数(Papp)。结果穿心莲内酯在Caco-2细胞模型中,随时间和浓度的增加,药物吸收呈饱和趋势,且受温度和碘乙酰胺影响,但不受外排抑制剂维拉帕米和MK-571的影响。结论穿心莲内酯在Caco-2细胞中的吸收主要是由载体介导的主动转运。

Objective To study the absorption of andrographolide in human Caco-2 cell monolayer model.Methods Caco-2 cell monolayer model was applied to investigating the bidirectional transport of andrographolide.The effects of time,drug concentration,temperature,and inhibitor on the absorption of andrographolide were observed.Drug concentration was measured by LC/MS/MS and the apparent permeability coefficients（Papp） were calculated.Results Time and concentration saturation were observed for the absorptive transport of andrographolide across Caco-2 monolayers.The transport of andrographolide was influenced by the change of temperature and the presence of iodoacetamide,but not Verapamil or MK-571.Conclusion The absorption and transport mechanism of andrographolide in Caco-2 cell monolayers are active transportation mediated by transporter.