Methylophiopogonanone A is a homoisoflavonoid that has been found in O. japonicus roots and has diverse biological activities. It increases the uptake of rosuvastatin (Item Nos. 12029 | 18813) and atorvastatin in HEK293T cells expressing human organic anion transporting polypeptide 1B1 (OATP1B1; EC50s = 11.33 and 6 μM, respectively). Methylophiopogonanone A scavenges 2,2-diphenyl-1-picrylhydrazyl (DPPH; ) and ABTS radicals in cell-free assays. In vivo, methylophiopogonanone A (10 mg/kg) decreases body weight gain and reduces serum and hepatic lipid levels in a rat model of high-fat diet-induced hyperlipidemia. It also reduces infarct size and myocardial apoptosis in mouse model of ischemia-reperfusion injury induced by transient occlusion of the left anterior descending coronary artery.