脱水穿心莲内酯在Caco-2细胞单层模型中的吸收机制  

Absorption mechamism of dehydroandrographolide in human Caco-2 cell monolayer model

作　　者：姚媛[1,2] 廖琼峰[1] 谢智勇[3] 曾元儿[1] 马燕[1] 

机构地区：[1]广州中医药大学中药学院,广东广州510006 [2]广州中医药大学第一附属医院,广东广州510405 [3]中山大学药学院,广东广州510006

出　　处：《中草药》2011年第6期1154-1157,共4页Chinese Traditional and Herbal Drugs

基　　金：国家自然科学基金资助项目(30600823)

摘　　要：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。Objective To study the absorption mechanism of dehydroandrographolide （DAL） in human Caco-2 cell monolayer model. Methods Caco-2 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 Caco-2 cell monolayer model was of time and concentration dependence, without saturation. And it was not influenced by the change of temperature transport of DAL are passive diffusion as the dominating process in and the presence of Verapamil. Conclusion The absorption and Caco-2 cell monolayer model.

关 键 词：脱水穿心莲内酯 CACO-2细胞模型 被动转运 维拉帕米 LC/MS/MS 

分 类 号：R285.61[医药卫生—中药学]