Effect of paeonol on expression and function of drug transporters BCRP and SLCO1 B1 in HepG2 cell / 中国生化药物杂志

ABSTRACT

Objective To investigate influences of paeonol on mRNA expression and function of drug transporters BCRP and SLCO1B1 in HepG2 cell.Methods Cell counting Kit-8 assay was used to detect the viability of HepG2 cells;Real-time fluorescent quantitative PCR (qPCR) was performed to measure the expressions of BCRP and SLCO1B1 mRNAs; flow cytometry was applied to determine the transport functions of BCRP and SLCO1B1. Results Paeonol (2-8μg/mL) did not decrease HepG2 cell survival rate, but 16 μg/mL paeonol significantly reduced cell survival rate (P<0.05). Paeonol(2-8μg/mL)significantly induced the mRNA expression and function of drug transporters BCRP and SLCO1B1(P <0.05).Compared with control group, transcription level of paeonol group’s BCRP and SLCO1B1 drug transporters obviously up-regulated, the of translocation efficiency of substrate specificity increased significantly (P <0.05).Conclusion Paeonol can induce drug hepatocellular transporters BCRP and SLCO1B1 gene expression, thereby promote the substrate transport the transmembrane.It is indicated that the drug combination of paeonol and BCRP and SLCO1B1 transporters, there may be a risk of drug interactions.