基于Caco-2细胞单层模型研究鞣花酸的转运特性

Transport characteristics of ellagic acid across Caco-2 cell monolayer model

目的研究鞣花酸在Caco-2细胞单层模型上的转运特性。方法利用MTT法确定鞣花酸单体在Caco-2细胞单层模型转运过程的安全浓度区间。以鞣花酸的表观渗透系数(P_(app))和累积转运量为衡量指标,采用高效液相色谱法(HPLC)测定鞣花酸含量,考察不同浓度、不同孵育时间的鞣花酸在Caco-2细胞单层模型上的双向转运过程。结果鞣花酸的累计转运量与孵育时间、给药浓度呈正相关,不同浓度的鞣花酸P_(app)值差异明显且吸收作用明显强于外排作用,外排比均<1.5。结论鞣花酸单体在Caco-2细胞模型的双向转运过程中以主动转运为主,外排蛋白可能未参与转运过程,鞣花酸为难吸收的一类药物。

Objective To study the transport behavior of ellagic acid in Caco-2 cell monolayer model. Methods MTT method was employed to confirm safe concentration range of ellagic acid monomer of transport processes in Caco-2 cell monolayer model. The samples concentrations of ellagic acid were analyzed by high performance liquid chromatography（ HPLC）. The apperent partion coefficient value（ Papp） and the transport total amount were caculated. Bidirection transport behavior of ellagic acid by incubating in different concentration and time were study. Results The transport cumulative amount of ellagic acid with incubation time,the administration concentration was positively correlated,the Pappvalues of different concentration ellagic acid have differences and the absorption effect was stronger than platoon role. The efflux ratio（ ER） values〈 1. 5. Conclusion The active transport of the ellagic acid monomer in the Caco-2 cell model was based on the active transport,Efflux proteins may not be involved in the transport process,ellagic acid belong to the hard absorption drugs.