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

Abstract

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

CLC Number:

R965.2
R966

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.

References

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