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目的:研究5-氨基水杨酸(5-ASA)的跨膜转运是否涉及P-糖蛋白和多药耐药蛋白(MRP2)。方法:以Caco-2、L-MDR1、MRP2等三种细胞为模型,测定5-ASA跨膜转运的转运率和表观渗透常数。此外还研究了5-ASA对地高辛在Caco-2细胞转运的影响。结果:在Caco-2、L-MDR1和MRP2细胞,5、50、500μmol·L-15-ASA从底端(B)→顶端(A)方向和A→B方向的转运率和表观渗透系数(Papp)均无统计学差异(P>0.05)。在Caco-2细胞,与未用5-ASA组相比,各浓度5-ASA组(50μmol·L-1~5mmol·L-1)对地高辛的Papp和B→A方向的净转运率无明显影响(P>0.05)。结论:5-ASA可能不是P-糖蛋白和MRP2的底物,也不能提示5-ASA是P-糖蛋白的抑制剂或诱导剂。
AIM: To investigate whether transmembrane transport of 5-aminosalicylic acid (5-ASA) involves P-glycoprotein and multidrug resistance protein (MRP2). Methods: Caco-2, L-MDR1, MRP2 and other three kinds of cells as a model to measure 5-ASA transmembrane transport rate and apparent permeability constant. In addition, the effect of 5-ASA on digoxin transport in Caco-2 cells was also studied. Results: In Caco-2, L-MDR1 and MRP2 cells, the transport rates of 5,50 and 500μmol·L-15-ASA from the basal side to the top side and the direction of A → B and the apparent permeability coefficient (Papp) were no significant difference (P> 0.05). In Caco-2 cells, the net transfer rate of digoxin to Papp and B → A in each concentration of 5-ASA group (50μmol·L-1 ~ 5mmol·L-1) No significant effect (P> 0.05). CONCLUSIONS: 5-ASA may not be a substrate for P-glycoprotein and MRP2 nor does it suggest that 5-ASA is an inhibitor or inducer of P-glycoprotein.