Abstract: Background and Objective: Myocardial infarction (heart attack) owing to ischemia is the primary contributor to most of the death caused by cardiovascular diseases (CVDs). This pre-clinical study was framed to investigate the beneficial efficacy of Asiatic acid (AA) against isoproterenol (ISO)-induced myocardial infraction (MI) in experimental rats. Materials and Methods: Healthy male rats (n = 32), were separated into four groups with 8 rats in each group. Group I rats were given only saline (control), group II rats were orally administrated with AA (20 mg kg–1) for 7 days (AA alone), group III rats were induced with ISO (100 mg kg–1, s.c) for 2 consecutive days (MI model), group IV rats were pre-treated (5 days) and co-treated (6th and 7th day) with AA (20 mg kg–1 via orally) and followed by induction of ISO (AA+ISO). Results: Rats pre and co-treated with AA for 7 days and followed by ISO induction (group IV rats)results in considerable increase in the activities of ATPases (Na2+/K+ and Mg2+) and endogenous antioxidants (CAT, SOD, GPx) as well as substantial decrease in the levels of heart weight, heart to body weight ratio, lipid peroxidation product (MDA), Ca2+ ATPases, cardiac markers (cTnT, CK-MB, LDH) and inflammatory markers (IL-6, IL-1β, TNF-α).Moreover, administration with AA greatly reduced the pathological changes (edema, necrosis, neutrophil infiltration) in cardiac tissue and lookalike as a control group. Conclusion: Taken together, that treatment with AA considerably attenuated the ISO-induced cardiotoxicity or MI by exhibiting potent antioxidant and anti-inflammatory activity. However, further studies (clinical trials) are required to support its importance against Myocardial infarction.