Abstract: OBJECTIVE To investigate the effects of Guanxinping (GXP) on RAW264.7 macrophage polarization induced by LPS. METHODS Macrophages were divided into control group， model group and low-， mid-， high-dose of GXP groups. Cells were starved for 24 hours before intervention with drug-containing serum of rats. The characteristic molecules of macrophage polarization in cell supernatant， including tumor necrosis factor α (TNF-α) and transforming growth factor β(TGF-β) were detected by ELISA; the expression levels of M1 and M2 macrophage surface molecules CD86 and CD206 were detected by flow cytometry; the expression of mRNA of CD86 and CD206 were detected by qPCR. RESULTS Compared to the model group， high-dose of GXP decreased the secretion of TNF-α (P<0.01); low-， mid-， high-dose of GXP decreased the secretion of TGF-β1 (P<0.01) in macrophage supernatant. Low- and high- dose of GXP decreased the expressions of CD86 (P<0.05) and increased the expression of CD206 (P<0.01). There were no significant difference in the mRNA expression of CD86 between the GXP groups and model group， but GXP increased the mRNA expression of CD206. CONCLUSION GXP can inhibit the polarization of macrophages towards M2， which may be one of the mechanisms of GXP in the treatment of atherosclerosis.