AimThe effect of tanshinoneⅡA on cholesterol homeostasis in foam cells was studied in vitro.MethodsThe foam cell induced from RAW264.7 macrophage with oxidized low density lipoprotein (ox-LDL) were treated with different concentration of tanshinoneⅡA.The relative cell viability were detected by MTT methods, and the change of total cholesterol and cholesterol ester in the cells were detected with the enzyme colorimetric quantifies.The lipid accumulation in cell was observed by oil red O dyeing, then the expressions of CD36, ATP binding cassette transporter A1(ABCA1), liver X receptor α (LXRα) and peroxisome proliferator activated receptors γ (PPARγ), PPARα were detected with the methods of fluorescent quantitation PCR and Western Blot.ResultsThe cell viability was not affected when tanshinone ⅡA concentrations were in the range of 0～20 mg/L.The ratio of cholesterol ester and total cholesterol decreased and lipid accumulation decreased when the foam cells were treated with 20 mg/L tanshinone ⅡA.Meanwhile, the expression of ABCA1, LXRα, PPARα were increased，but the expression of CD36 had no obvious variance.ConclusionTanshinoneⅡA can inhibit the formation of foam cells induced from RAW264.7 by ox-LDL，the mechanism is possibly related to inducing the expressions of PPARα, LXRα and ABCA1 and promoting the excretion of cholesterol.