[关键词]
[摘要]
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。
[Key word]
[Abstract]
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.
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[基金项目]
国家自然科学基金资助项目(30600823);“重大新药创制”国家科技重大专项(2009ZX09304-003, 2009ZX09501-017)