Objective To observe the effect of resveratrol on proliferation and TGF-β1 signaling pathway of human prostate cancer cell line PC-3. Methods Human prostate cancer cell line PC-3 was cultured and treated with resveratrol at different concentrations and different time points． The effect of resveratrol on PC-3 cell proliferation was studied by means of MTT. The cell cycle was detected with flow cytometry. RT-PCR and Western blot were used to detect the expressions of TGF-β1 and Smad2 at mRNA and protein levels. Results The viability of Huh-7 cells treated with resveratrol was obviously decreased. Analysis of the cell cycle revealed that resveratrol induced a significant decrease in cells in the S phase and increase in cells in the G1 phase. Furthermore, the expressions of TGF-β1 and its downstream factor-Smad2 were inhibited at mRNA and protein levels by resveratrol in a concentration- and time-dependent manner. Conclusions Resveratrol perhaps plays inhibitory effect on PC-3 cells through inhibiting the activity of TGF-β1 signaling pathway.