AimTo investigate the effect and mechanism of berberine on ATP-binding cassette transporter A1(ABCA1) expression and cholesterol efflux in THP-1 macrophage.MethodsTHP-1 macrophage foam cell were exposed to berberine with different levels(0, 5, 10, 20 μmol/L） for 24 h or treated with berberine(20μmol/L) for increasing periods of time( 0, 6, 12, 24 h).Western Blot was used to determine protein levels for ABCA1, liver X receptor-α (LXR-α) and acetylated LXR-α.Cellular lipid accumulation was determined by high performance liquid chromatography analysis.Cholesterol efflux was determined by liquid scintillator. ResultsCompared with control group, berberine increased the expression of ABCA1 in dose (0～20 μmol/L）and time（0～24 h）dependent manner while decreased the acetylation of LXR-α.In addition, berberine increased the levels of cholesterol efflux and decreased the accumulation of cholesterol in THP-1 macrophage foam cells when the content of the berberine was 20 μmol/L and treated time was 24 h, the blends had the maximum impact.ConclusionBerberine may upregulate ABCA1 expression and cholesterol efflux via deacetylation of LXR-α.