AIM To investigate the effects of oleanolic acid and chlorogenic acid on proliferation and cell cycle of HepG2 cells and its relative CYP450 genes expression. METHODS Rifampicin as the control drug,the MTT method,Flow cytometry,and Real time quantitative PCR technique were used in this study. RESULTS Chlorogenic acid and oleanolic acid could inhibit cell proliferation of HepG2 cells,and arrest cell cycle at S stage. Oleanolic acid induced CYP1A1,CYP3A4 mRNA,but chlorogenic acid inhibited CYP1A1. CONCLUSION Oleanolic acid and chlorogenic acid can inhibit the proliferation of HepG2 cells,but show inconsistent effects on drug metabolic enzyme CYP1A1,CYP3A4 mRNA expression.