The medicinal part ofAucklandia lappa (Asteraceae) is its dried root,which is one of the commonly used Chinese medicinal materials.Here we reviewed sesquiterpene lactones isolated from A.lappa over the past ten years in the following aspects of pharmacological activities,pharmacokinetics,toxicology,struc-ture-activity relationship.Pharmacological activities consist of anti-cancer,anti-inflammatory activity,anti-immunity activity,anti-oxidant activity,antimicrobial activity,spasmolytic activity and so on.The extractive,showing similar pharmacokinetics parameters,may exert their various biological activities by the interaction of their α-methylene-γ-butyrolactone moiety with the thiol groups of biomacro-molecules through Michael-addition.However,the poor aqueous solubility,non-selective binding as a Michael acceptor at undesired targets limited clinical translation of this class.In order to evaluate the potential effect of the extractive applied in clinical trial,the present review outlines information on phar-macological activities,pharmacokinetics,toxicology,and structure-activity relationship,as well as the future research directions of the extractive for further development and utilization ofA.lappa.