摘要
目的:建立体外模拟体内肠道细胞的Caco-2细胞Transwell模型,以此研究雷公藤甲素在Caco-2细胞模型上的跨膜转运特征。方法:采用聚酯碳酸酯膜连续培养Caco-2细胞21天,形成致密的单层细胞模型。然后对影响雷公藤甲素在Caco-2细胞模型上转运特征的因素包括浓度、时间及跨膜转运蛋白(P-糖蛋白,多药耐药蛋白,乳腺癌耐药蛋白)进行考察;同时采用LC-MS对溶液中的雷公藤甲素的含量进行测定。结果:雷公藤甲素主要以主动转运的方式进行吸收,且随着时间和药物浓度的增加,转运量明显增加。结论:雷公藤甲素在Caco-2细胞上转运存在一定的浓度及时间依赖性,且P-gp介导雷公藤甲素在Caco-2细胞上转运。
Objective: To develop a Caco-2 cell monolayer transwell model and then used it to investi gate the intestinal transport mechanism of triptolide. Methods: Caco-2 cells were seeded on the permeable polycarbonate membranes and incubated for 21 days, and then the influencing factors were investigated us ing Caco-2 cell model, including time, concentration, and different membrane transport proteins(P-gp,MRP1 and BCRP). A sensitive and reliable LC-MS method was developed and applied to determine the concentration of triptolide in HBSS samples. Results: The results suggested that triptolide was transported mainly as active diffusion. The flux of triptolide was time- and concentration-dependent. Conclusion: Trip tolide was transported mainly in an active transport mode, and P-gp was involved in its transport.
出处
《药学与临床研究》
2016年第1期15-18,共4页
Pharmaceutical and Clinical Research
