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维拉帕米对胡桃醌Caco-2细胞转运特性的影响

             

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目的:研究维拉帕米对胡桃醌Caco-2细胞转运特性的影响。方法应用Caco-2细胞模型考察时间、浓度对胡桃醌转运吸收特性的影响,应用P-糖蛋白抑制剂维拉帕米对胡桃醌转运吸收机制进行研究,采用高效液相色谱(HPLC)法测定胡桃醌的浓度,计算其表观渗透系数( Papp )。结果 Caco-2细胞模型,随浓度增加和时间延长,胡桃醌的累积转运量逐渐增加;加用维拉帕米(100μmol/L )后,使AP侧到BL侧的表观渗透系数 PappAP→BL显著增加,而从BL侧到AP侧的表观渗透系数 PappBL→AP降低。结论胡桃醌的转运以被动转运为主,存在P-糖蛋白参与的主动外排,加用维拉帕米后胡桃醌经吸收转运增加,提示维拉帕米可能促进吸收。%Objective To investigate the influence of verapamil on transport characteristics of juglone Caco-2 cells model. Methods The juglone Caco-2 cells model was adopted to investigate the influence of time and concentration on juglone transport and absorption char-acteristics. The P-glycoprotein ( P-gp ) inhibitor verapamil was used to investigate the juglone transport mechanism. The HPLC method was adopted to detect the juglone concentration. The apparent permeability coefficient ( Papp ) was calculated. Results In the Caco-2 cells model, the cumulative transport quantity of juglone was gradually increased with the concentration increase and the time extend-ing. After adding verapamil ( 100 μmol/L ) , Papp(AP→BL) was significantly increased, while Papp(BL→AP) was decreased. Conclusion The ab-sorption of juglone in Caco-2 cells model is dominated by the passive transference, and the active efflux participated by P-gp exists, after adding juglone in Caco-2 cells, the absorption and transference of juglone, which suggesting that verapamil could promote the ab-sorption.

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