异甘草素在Caco-2细胞的摄取特性

Uptake of Isoliquiritigenin in Caco-2 Cell Monolayer

目的:研究异甘草素(ISL)在Caco-2细胞的摄取特性。方法:以Caco-2细胞单层模型研究异甘草素的细胞摄取规律。采用高效液相色谱法测定细胞中ISL浓度,考察时间、pH值、药物浓度及抑制剂对Caco-2细胞摄取ISL的影响。结果:ISL在Caco-2细胞中的摄取呈时间依赖性;ISL在4～15 mg.L-1浓度范围内的摄取呈线性增加,符合被动扩散过程;pH 8.0条件下药物的细胞摄取量(0.48±0.006)μg.mg-1显著低于pH 5.0药物的细胞摄取量(0.98±0.03)μg.mg-1(P<0.01);加入维拉帕米,叠氮化钠及2,4-二硝基酚后,与对照组相比,ISL的细胞摄取量显著高,分别为(1.19±0.030)μg.mg-1(P<0.01),(1.10±0.004)μg.mg-1(P<0.05),(1.17±0.020)μg.mg-1(P<0.01)。结论:ISL的细胞摄取机制主要是被动转运;P-糖蛋白参与了ISL的转运过程。

Objective：To observe uptake process of Isoliquiritigenin（ISL） in Caco-2 cell.Method：The concentration of ISL in cells was detected by HPLC and the mechanism of ISL absorption in cells was explored by studying the time,pH,drug concentration and inhibitors on the uptake of ISL in cells.Result：ISL in Caco-2 cells uptake was time-dependent.ISL at 4-15 mg.L-1 concentration range of uptake increased linearly,consistent with passive diffusion process.The drug intake amount（0.48 ± 0.006） μg.mg-1 under pH 8.0 was significantly lower than pH 5.0（0.98 ± 0.03） μg.mg-1（P 0.01）.Compared with the control group,ISL cell uptake was signifi-cantly higher after additional treatment with verapamil（1.19 ± 0.030） μg.mg-1,（P 0.01）,sodium azide（1.10 ± 0.004） μg.mg-1（P 0.05） and 2,4-dinitrophenol（1.17 ± 0.020） μg.mg-1（P 0.01）.Conclu-sion：The mechanism of ISL absorption in cells mainly was passive transport and P-glycoproteins participates in the conveying process of ISL in Caco-2 cells.