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目的:研究原儿茶酸(PA)对HepG2.2.15细胞和大鼠原代肝细胞细胞膜上P糖蛋白(P-gp)、阴离子转运蛋白(Oatp1A1)和阳离子转运蛋白(Oct1)mRNA表达水平的影响。方法:HepG2.2.15细胞和大鼠原代肝细胞经不同浓度PA处理后,用荧光定量PCR检测细胞膜上P-gp、Oatp1A1和Oct1 mRNA的表达量。结果:HepG2.2.15细胞经PA处理48h后,低浓度PA(0.5μg/mL)显著下调P-gp和Oatp1A1 mRNA的表达,高浓度PA(50μg/mL)显著上调P-gp和Oatp1A1 mRNA的表达;低、中、高浓度PA均显著上调Oct1 mRNA的表达。大鼠原代肝细胞经PA处理48h后,低浓度PA(0.5μg/mL)显著下调Oatp1A1和Oct1 mRNA的表达,高浓度PA(50μg/mL)显著上调Oatp1A1和Oct1 mRNA的表达。结论:PA对HepG2.2.15细胞和大鼠原代肝细胞膜上P-gp、Oatp1A1和Oct1 mRNA的表达有显著影响,提示当PA与上述转运体底物药物共用时,可能会发生药物吸收相互作用。
Objective: To investigate the effect of protocatechuic acid (PA) on the mRNA expression of P-gp, Oatp1A1 and Oct1 in HepG2.2.15 cells and rat primary hepatocytes influences. Methods: HepG2.2.15 cells and rat primary hepatocytes were treated with different concentrations of PA, and the expression of P-gp, Oatp1A1 and Oct1 mRNA was detected by real-time PCR. Results: The expression of P-gp and Oatp1A1 mRNA in HepG2.2.15 cells treated with PA for 48 h decreased the expression of P-gp and Oatp1A1 mRNA significantly (P <0.05) Low, medium and high concentrations of PA significantly up-regulated the expression of Oct1 mRNA. The rat primary hepatocytes were treated with PA for 48h, and the low concentrations of PA (0.5μg / mL) significantly decreased the expression of Oatp1A1 and Oct1 mRNA. The high concentration of PA (50μg / mL) significantly upregulated the expression of Oatp1A1 and Oct1 mRNA. CONCLUSION: PA has a significant effect on the expression of P-gp, Oatp1A1 and Oct1 mRNA in HepG2.2.15 cells and rat primary hepatocytes, suggesting that drug-absorption interaction may occur when PA is co-administered with the above transporter substrate drugs .