Magnesium lithospermate B is the major water-soluble components of Salvia miltiorrhiza, a traditional Chinese medicine known as Danshen. Magnesium lithospermate B possesses extensive pharmacological activities, including protective effects on endothelium, inhibition of the proliferation and migration of vascular smooth muscle cells, reduction of myocardial and cerebral ischemia injury, et al. It has been shown that magnesium lithospermate B exerts satisfactory therapeutic effects on atherosclerosis, myocardial or cerebral ischemia. The beneficial effects of magnesium lithospermate B on cardiovascular system are closely related to its pharmacological actions of anti-oxidation, anti-inflammation and anti-apoptosis.