原儿茶酸对HepG2.2.15细胞和大鼠原代肝细胞膜转运蛋白mRNA表达的影响  

Effects of protocatechuic acid on the mRNA expression of three transport proteins in HepG2.2.15 cell and rat primary hepatocyte

作　　者：孟沫然[1] 王俊俊[1] 蔡文涛[1] 陈勇[1] 韩凤梅[1] 

机构地区：[1]湖北大学中药生物技术省重点实验室,武汉430062

出　　处：《中华中医药杂志》2011年第11期2555-2558,共4页China Journal of Traditional Chinese Medicine and Pharmacy

基　　金：科技部重大专项(No.2008ZX10002-009);湖北省发改委生物产业专项(No.2008-1365-2);武汉市科技局攻关项目(No.201060623264)~~

摘　　要：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 study the effects of protocatechuic acid（PA） on the mRNA expression of transporters P-gp,Oatp1A1 and Oct1 in HepG2.2.15 cell and rat primary hepatocyte.Methods： HepG2.2.15 cells and rat primary hepatocytes were treated in vitro by different concentration of PA respectively,the mRNA expression levels of P-gp,Oatp1A1 and Oct1 were detected by real-time fluorescence quantitative PCR.Reaults： After HepG2.2.15 cells were treated by PA for 48h,low concentration of PA（0.5μg/mL） significantly decreased the mRNA expression of P-gp and Oatp1A1,whereas a reverse changes were observed at the high concentration of PA（50μg/mL）.Meanwhile,PA at low,medium and high concentration caused marked increase of Oct1 mRNA expression.For rat primary hepatecytes treated by PA for 48h,low concentration of PA caused significant decrease of the mRNA expression of OatplAl and Oct1,whereas high concentration of PA caused marked increase of the mRNA expression of Oatp1A1 and Oct1.Conclusion： The effects of PA on the mRNA expression of P-gp,Oatp1A1 and Oct1 in HepG2.2.15 cell and rat primary hepatocyte suggested that the drug-drug interaction between PA and other drugs,which were transported by the above transporters,should occurred.

关 键 词：原儿茶酸 HEPG2.2.15细胞 大鼠原代肝细胞 P糖蛋白 阴离子转运蛋白1A1 阳离子转运蛋白1 

分 类 号：R285.5[医药卫生—中药学]