5-氨基水杨酸在Caco-2 、L-MDR1 和MRP2 细胞中的转运研究

中国临床药理学与治疗学 ›› 2006, Vol. 11 ›› Issue (11): 1265-1269.

5-氨基水杨酸在Caco-2 、L-MDR1 和MRP2 细胞中的转运研究

辛华雯, Matthias Schwab¹, Ulrich Klotz¹

广州军区武汉总医院临床药理科, 武汉 430070, 湖北;
¹Dr.Margarete Fischer-Bosch Institute of Clinical Pharmacology, Stuttgart 70376, Germany

收稿日期:2006-04-03 修回日期:2006-05-12 出版日期:2006-11-26 发布日期:2020-11-06
作者简介:辛华雯, 女, 医学博士, 副主任医师, 主要从事临床药理学研究。Tel:027-68878690 E-mail:hwxin@public.wh.hb.cn
基金资助:
德国Robert Bosch 基金资助项目; 德国Robert Bosch 基金资助项目

Study on transport of 5-aminosalicylate in Caco-2, L-MDR1 and MRP2 cell monolayers

XIN Hua-wen, Schwab Matthias¹, Klotz Ulrich¹

Department of Clinical Pharmacology , Wuhan General Hospital , Wuhan 430070 , Hubei , China ;
¹Dr.Margarete Fischer-Bosch Institute of Clinical Pharmacology , Stuttgart 70376 , Germany

Received:2006-04-03 Revised:2006-05-12 Online:2006-11-26 Published:2020-11-06

摘要/Abstract

摘要： 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 、500 μmol·L^-1 5-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( 50 μmol·L^-1 ~5 mmol·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。

关键词: 5-氨基水杨酸, 肠道转运, P-糖蛋白, 细胞株

Abstract: AIM: To investigate whether P-glycoprotein andMRP2 are involved in transport of 5-aminosalicylate( 5-ASA).METHODS: Permeability coefficients and transport rates of 5-ASA across Caco-2, L-MDR1 and MRP2 monolayers were measured.Trans epithelial transport of digoxin across Caco-2 monolayer with addition of 5-ASA was also studied.RESULTS: No differences of permeability coefficients and transport rates of 5-ASA at 5, 50 and 500 μmol·L^-1between basal-to-apical and apical-to-basal direction were measurable across Caco-2,L-MDR1 and MRP2 monolayers ( P>0.05).Compared with control experiments, no significant differences were observed in basal-to-apical net transport and PapPof digoxin( 5 μmol·L^-1) in the presence of 5-ASA ( 50μmol·L-1 -5 mmol·L^-1) ( P>0.05).CONCLUSION: 5-ASA can not be regarded as a substrate of P-gPor MRP2.Inhibition or induction of P-glycoprotein by 5-ASA could be excluded.Further studies are needed to identify the nature of the involved active carrier system( s)in intestinal secretion of 5-ASA.

Key words: 5-aminosalicylate, intestinal transport, P-glycoprotein, cell lines

中图分类号:

R965.2
R966

辛华雯, Matthias Schwab, Ulrich Klotz. 5-氨基水杨酸在Caco-2 、L-MDR1 和MRP2 细胞中的转运研究[J]. 中国临床药理学与治疗学, 2006, 11(11): 1265-1269.

XIN Hua-wen, Schwab Matthias, Klotz Ulrich. Study on transport of 5-aminosalicylate in Caco-2, L-MDR1 and MRP2 cell monolayers[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2006, 11(11): 1265-1269.

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