Paeonol,an effective component of traditional herb Cortex Moutan,has comprehensive pharmacological activities,such as antibacterial,anti-inflammatory,pain-relieving,anticancer and preventing cardiovascular diseases.In recent years,a great amount of work on the structure modification of paeonol was done to synthesize a series of paeonol derivatives as the study on the effect and mechanism of paeonol was increasingly intensively developed.The paper systematically reviewed the research progress on the structure modification of paeonol.