Objective: To investigate the modulating effect of β-glycyrrhetic acid(β-GA) on the activity of farnesoid X receptor(FXR).Methods: FXR was transiently transfected into HepG2 cells,and the effect of β-GA on FXR activity was determined.The effect of β-GA on HepG2 cell viability was detected by Celltiter-Glo.The effect of β-GA on FXR target genes was determined by real-time q-PCR.Results: β-GA specifically and does-dependently decreased the activity of FXR induced by CDCA,and selectively down-regulated the expressions of FXR target genes.Conclusion: β-GA can selectively modulate the activity of FXR.