茵陈中6,7-二甲氧基香豆素在MDCK模型中的吸收机制研究

摘要

目的：基于马丁达比犬的肾近曲小管上皮( MDCK)细胞模型研究茵陈中6,7-二甲氧基香豆素的吸收机制。方法考察时间、药物浓度(12.5、25、50、100、200μmol/L)、温度(4、37℃)和抑制剂(碘乙酰胺、维拉帕米、MK571)对6,7-二甲氧基香豆素吸收和转运的影响。采用高效液相色谱法(HPLC)检测6,7-二甲氧基香豆素的浓度,计算出表观渗透系数(Papp),并分析其吸收机制。结果根据Papp得出6,7-二甲氧基香豆素在MDCK细胞模型上的转运量呈时间和浓度依赖性且不同浓度下的Papp(B-A)/Papp (A-B)≈1,4、37℃和加入抑制剂碘乙酰胺后,6,7-二甲氧基香豆素的吸收Papp (A-B)之间差异无统计学意义,37℃和加入外排蛋白抑制剂维拉帕米、MK571后,6,7-二甲氧基香豆素的外排Papp(B-A)之间差异无统计学意义。结论6,7-二甲氧基香豆素在MDCK细胞模型上表现为浓度依赖的单纯扩散。%Objective To study absorption of 6 ,7-dimethylesculetin in capillary artemisia in MDCK cell membrane model. Methods The effects of time, drug concentration, temperatuer and inhibitor on the absorption and transport of 6,7-dimethylesculetin were studied systematically in the MDCK cell membrane. The drug concentration was de-termined by high performance liquid chromatography to calculate the apparent permeability coefficient ( Papp ) . Re-sults 6, 7-dimethylesculetin transport in MDCK cell monolayer was time and concentration dependent. The Papp(B-A)/Papp(A-B)≈1. With the 4℃,37℃ and presence of iodoacetamide,the Papp (A-B) of 6,7-dimethylesculetin had no significant difference. With the 37 ℃ and presence of verpamil,MK571, the Papp(B-A) of 6,7-dimethylescu-letin also had no significant difference. Conclusion The transport of 6,7-dimethylesculetin in MDCK cell mem-brane model is passive diffusion.