Oleanolic acid (OA) is a pentacyclic triterpenoid compound naturally found in plant kingdom. OA possesses several biological activities, which make it an interesting compound for scientists working in the field of pharmacy and new drugs design and development. The compound exhibits anti-inflammatory and anti-oxidative effects in vitro and in vivo, which probably determine its dual function - cytoprotective and cytotoxic/cytostatic activity. In this study, we focused on the presentation of molecular mechanisms of the compound’s action to emphasize its multifunctional character. Due to multiple pharmacological properties of the triterpenoid, it could be used to prevent the majority of the most common diseases of civilization i.e. cancer, cardiovascular diseases, atherosclerosis or diabetes. However, because of its relatively weak activity it may serve as a starting material for the synthesis of more potent chemical compounds.