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目的:探讨大黄酸对人结肠腺癌上皮细胞(Caco-2)多药耐药蛋白mRNA表达的影响。方法:用大黄酸作用于Caco-2细胞,采用荧光定量PCR(real time PCR)法检测转运体MRP1-5 mRNA的表达量,数据分析采用2-ΔΔCT法。结果:高(5.00 mg.L-1)低(2.50 mg.L-1)质量浓度大黄酸均可以显著上调Caco-2细胞MRP3 mRNA表达(P<0.05或P<0.01);低浓度大黄酸可以显著下调Caco-2细胞MRP5 mRNA表达(P<0.05);大黄酸对MRP1,MRP2和MRP4 mRNA的表达没有显著影响。结论:大黄酸可能通过上调Caco-2细胞MRP3 mRNA的表达和下调MRP5 mRNA的表达而影响其口服药物的生物利用度。
Objective: To investigate the effect of rhein on the expression of Caco-2 multidrug resistance protein mRNA in human colon adenocarcinoma. Methods: The expression of MRP1-5 mRNA in transporters was detected by real-time PCR with rhein on Caco-2 cells. The data were analyzed by 2-ΔΔCT method. RESULTS: MRP3 mRNA expression in Caco-2 cells was significantly increased (P <0.05 or P <0.01) with high concentrations of 5.00 mg.L-1 and 2.50 mg.L-1 respectively. Low concentrations of rhein could up- MRP5 mRNA expression was significantly down-regulated in Caco-2 cells (P <0.05). Rhein had no significant effect on MRP1, MRP2 and MRP4 mRNA expression. Conclusion: Rhein may affect the bioavailability of oral drug by up-regulating MRP3 mRNA expression and down-regulating MRP5 mRNA expression in Caco-2 cells.