Dan-Shen-Yin (DSY) is a well-known traditional Chinese formula which is widely used in clinical practice for the treatment of coronary heart disease (CHD) and has produced a favorable effect in China. The present study was designed to examine whether or not acute oral DSY can protect the heart against myocardial infarction in acute myocardial ischemic rats. If so, we would then investigate the anti-inflammatory and anti-oxidant mechanisms involved. The left anterior descending coronary artery was occluded to induce myocardial ischemia in the hearts of Sprague-Dawley rats. At the end of the 3-h ischemic period (or 24 h for infarction size), we measured the myocardial infarction size, inflammatory factors and the activities of anti-oxidative enzymes. DSY reduced the infarction size and the serum levels of C-reactive protein, interleukin-6, tumour necrosis factor-α and malondialdehyde and increased the activities of superoxide dismutase and the serum levels of glutathione. The results show that DSY exerts significant cardioprotective effects against acute ischemic myocardial injury in rats, possibly through its anti-inflammatory and anti-oxidant properties, and may thus be used as a potential therapeutic reagent for the treatment of CHD.