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脱水穿心莲内酯在Caco-2细胞单层模型中的吸收机制
引用本文:姚 媛,廖琼峰,谢智勇,曾元儿,马 燕.脱水穿心莲内酯在Caco-2细胞单层模型中的吸收机制[J].医学教育探索,2011,42(6):1154-1157.
作者姓名:姚 媛  廖琼峰  谢智勇  曾元儿  马 燕
作者单位: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
基金项目: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。

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

Absorption mechamism of dehydroandrographolide in human Caco-2 cell monolayer model
YAO Yuan,LIAO Qiong-feng,XIE Zhi-yong,ZENG Yuan-er,MA Yan.Absorption mechamism of dehydroandrographolide in human Caco-2 cell monolayer model[J].Researches in Medical Education,2011,42(6):1154-1157.
Authors:YAO Yuan  LIAO Qiong-feng  XIE Zhi-yong  ZENG Yuan-er  MA Yan
Institution:1.College of Chinese Traditional Medicine,Guangzhou University of Chinese Medicine,Guangzhou 510006,China 2.The First Affiliated Hospital of Guangzhou University of Chinese Medicine,Guangzhou 510405,China 3.School of Pharmaceutical Science,Sun Yat-sen University,Guangzhou 510006,China
Abstract: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 and the presence of Verapamil. Conclusion The absorption and transport of DAL are passive diffusion as the dominating process in Caco-2 cell monolayer model.
Keywords:Key word: dehydroandrographolide (DAL)  Caco-2 cell monolayer model  passive diffusion  Verapamil  LC/MS/MS
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