根皮苷和3-羟基根皮苷在Caco-2细胞单层模型中的转运与吸收研究

Study on Absorption and Transportation of Phloridzin and 3-Hydroxy-phloridzin in Caco-2 Cell Monolayer Model

目的:研究根皮苷和3-羟基根皮苷在人克隆结肠腺癌细胞(Caco-2细胞)单层模型中的转运与吸收。方法:采用高效液相色谱法,以表观渗透系数(Papp)为指标,分别考察50、100、200μmol/L的根皮苷和3-羟基根皮苷在Caco-2细胞单层模型中的双向(AP→BL、BL→AP)转运;并通过两药配伍同时混合转运与两药单独转运比较,考察两药转运的相互作用。结果:随着浓度的增加,根皮苷AP→BL和BL→AP的Papp均有一定的上升趋势;3-羟基根皮苷AP→BL的Papp有下降趋势,BL→AP的Papp却略有上升趋势。与单独转运比较,混合转运中根皮苷和3-羟基根皮苷的转运量和Papp均明显下降(P<0.05)。结论:根皮苷和3-羟基根皮苷在Caco-2细胞单层模型的吸收状况良好,两药配伍转运时存在竞争性抑制。

OBJECTIVE：To study absorption and transportation of phloridzin and 3-hydroxy-phloridzin in cloning of human colon adenocarcinoma cells（Caco-2 cell）monolayer model.METHODS：HPLC method was adopted.Using apparent permeation coefficient Papp as index,two-way absorption and transportation（AP→BL and BL→AP）of phloridzin and 3-hydroxy-phloridzin（50,100,200 μmol/L）in Caco-2 cell monolayer model were investigated.Simultaneous transportation of drug combination was compared with that of single drug;the interaction of the two drugs was investigated.RESULTS：With the increase of concentration,Papp of phloridzin（AP→BL and BL→AP）increased to some extent;Papp of 3-hydroxy-phloridzin（AP→BL）decreased to some extent,while that of 3-hydroxy-phloridzin（BL→AP）increased slightly.Compared with single transportation,transportation amount and Papp of phloridzin combined with 3-hydroxy-phloridzin decreased significantly（P0.05）.CONCLUSIONS：Phloridzin and 3-hydroxy-phloridzin have good permeability coefficient on Caco-2 cell monolayer model.When transport together,competitive inhibition is found between two drugs.