Atractylodes macrocephala Koidz is a widelyused as a traditional Chinese medicine. Atractylenolides(-I, -II, and -III) are a class of lactone compounds derivedfrom Atractylodes macrocephala Koidz . Research intoatractylenolides over the past two decades has shown thatatractylenolides have anti-cancer, anti-infl ammatory, antiplatelet,anti-osteoporosis, and antibacterial activity; protectthe nervous system; and regulate blood glucose and lipids. Because of structural diff erences, both atractylenolide-I andatractylenolide-II have remarkable anti-cancer activities,and atractylenolide-I and atractylenolide-III have remarkableanti-infl ammatory and neuroprotective activities. Wetherefore recommend further clinical research on the anticancer,anti-infl ammatory and neuroprotective eff ects ofatractylenolides, determine their therapeutic eff ects, aloneor in combination. To investigate their ability to regulateblood glucose and lipid, as well as their anti-platelet, antiosteoporosis,and antibacterial activities, both in vitro andin vivo studies are necessary. Atractylenolides are rapidlyabsorbed but slowly metabolized; thus, solubilization studiesmay not be necessary. However, due to the inhibitory eff ectsof atractylenolides on metabolic enzymes, it is necessaryto pay attention to the possible side eff ects of combiningatractylenolides with other drugs, in clinical application. Inshort, atractylenolides have considerable medicinal valueand warrant further study.