OBJECTIVE: To study the preventive effect and mechanism of butylphthalide on myocardial ischemia-reperfusion injury in rats. METHODS: SD rats were randomly divided into sham operation group, model group, butylphthalide low-dose, medium-dose, high-dose groups (50, 75, 100 mg/lg), 10 in each group. All rats were intragastrically administrated related drugs once a day, sham operation group and model group were intragastrically administrated equal amount of normal saline, for 3 d. After last administration, except for sham operation group, 120 min of repertusion was conducted. Ratio of myocardial infarction area, apoptosis rate of myocardial cells, expressions of apoptosis-related protein [proapoptotic proteins (Caspase-3, Fas, Caspase-9), apoptotic protein (Bcl-2)], left ventricular ejection fraction (LVEF), and content of vascular endothelial growth factor (VEGF) in serum of rats in other groups were detected. RESULTS: Compared with sham operation group, myocardial infarction area and apoptosis rate of myocardial cells in model group were obviously increased; expressions of Caspase-3, Fas, Caspase-9 protein in myocardial cells were obviously enhanced, Bcl-2 protein expression was obviously weakened; LVEF and serum VEGF content were obviously reduced (P<0.01). Compared with model group, except that LVEF in butylphthalide low-dose group didn’t changed obviously (P>0.05), above indexes in other administration groups improved obviously (P<0.05). Compared with butylphthalide low-dose group, myocardial infarction area and apoptosis rate of myocardial cells in butylphthalide high-dose group were obviously decreased (P<0.05); expressions of Caspase-3, Fas, Caspase-9 protein in myocardial cells in butylphthalide medium-dose, high-dose groups were obviously weakened, and Bcl-2 protein expression was obviously enhanced (P<0.05). CONCLUSIONS: Butylphthalide can effectively reduce myocardial ischemia-reperfusion injury in rats, protect cardiac functions, and its mechanism may be related with up-regulating VEGF.