To investigate the effect and possible mechanism of total flavonoids of Penthorum chinense Pursh (TFPCP) on activated hepatic stellate cells,human hepatic stellate cell LX-2(HSC-LX-2) was cultured,TGF-β1 was used to active LX-2,MTT method was used to detect the effect of TFPCP on LX-2 proliferation rate,the cell migration rate was detected by scarification test and the collagen contraction was detected by collagen contraction test,enzyme-linked immunosorbent assay (ELISA) was adopted to detect the content of collagen I (Col I) and fibronectin (FN),Smad2,Smad3,p-Smad2,p-Smad3,Smad7 protein expressions in LX-2 was determined by Western blot.The results showed that the proliferation and migration of LX-2 were suppressed by TFPCP at three concentrations of 5,9 and 13 mg/L,and the effect was most significant at 13 mg/L (P<0.01).In addition,TFPCP could inhibit collagen contraction and reduce the deposition of Col I and FN (P<0.01).Further study indicated that treated with TFPCP suppressed the protein expressions of Smad3,phospho-Smad2 and phospho-Smad3(P<0.05),while significantly promoted the expressions of Smad7.In general,TFPCP inhibited the proliferation and migration of LX-2,reduced the secretion of ECM,the mechanism may be related to its inhibition of TGF-β1/Smads signaling pathway.