Arjunolic acid (AA) is a triterpenoid saponin isolated mainly from Terminalia arjuna bark. Arjunolic acid is associated with the various important physiological functions viz. antioxidant, antimicrobial, cardioprotective, hepatoprotective, and plays important role in supramolecular chemistry, etc. Arjunolic acid exhibits important function in maintaining the level of various antioxidant enzymes such as superoxide dismutase (SOD), catalase (CAT), glutathione-S-transferase (GST), glutathione reductase (GR) and glutathione peroxidase (GPx), level of cellular metabolites, reduced glutathione (GSH), oxidized glutathione (GSSG) and thereby reduces the oxidative stress. Its protective effect on liver, pancreas and kidney has also been the key property of arjunolic acid. Hence, arjunolic acid has potential to treat various disorders and this review may provide valuable information about arjunolic acid.