The present invention provides acetylated derivatives of the compound puerarin that have enhanced bioavailability and are particularly suitable for oral administration. The present invention also teaches the use of medicaments containing acetylated derivatives of puerarin that are suitable for the treatment of myocardial ischemia and for modulating blood lipid levels, dilating coronary and cerebral arteries, reducing oxygen consumption of cardiomyocytes, improving microcirculation and preventing aggregation of blood platelets.