The efficacy of aescin on the liver and cardiac markers, lipid profile, and antioxidant status in rats with myocardial infarction (MI) induced by isoproterenol (ISO) was investigated in this study. Three doses of aescin (5, 10, and 20 mg/kg of b.w) were administered to rats for the first 21 days. After the treatment period, ISO (60 mg/kg of b.w) was given subcutaneously to the rats on the 22nd and 23rdday. Cardiovascular and hepatic markers (CK, ALT, CK-MB, AST, cTnI, and cTnT) have been analyzed to investigate the cardiac and liver damage. The activities of antioxidant enzymes (CAT, GST, SOD, and GPx) were decreased in both cardiac tissue and erythrocytes of ISO rats. The levels of phospholipids (PLs), total cholesterol (TC), free fatty acids (FFA), and triglycerides (TG) were increased significantly in the serum of the rats administrated with ISO. The results of the present study implies that aescin pretreatment reduces oxidative stress and exhibits cardioprotective action by scavenging the free radicals and maintaining the levels of circulatory and cardiac lipids. Hematoxylin and eosin staining method was used to examine the cardiac histological changes in the experimental rats and the results showed that ISO-administered rats pretreated with aescin reduced cardiac tissue damage when compared with ISO alone injected rats.