To investigate the effect and mechanism of Zhuanggu Jianxi Formula(ZGJXF) on the polarization of macrophages into classical activation(M1) and alternative activation(M2) types.Methods:Phorbol 12-myristate 13-acetate was used to induce differentiation of human monocytic leukemia cells into non-activated macrophages(M0).Lipopolysaccharide was used to stimulate M0 to replicate the M1 polarization model.Cells were divided into a blank group(M0+blank serum)，a model group(M1+blank serum)，an inhibitor group(M1+NF-κB inhibitor+blank serum)，and a ZGJXF group(M1+medicated serum).After 24 hours of intervention，various indicators were measured，including M1 markers inducible nitric oxide synthase(iNOS)，major histocompatibility complex Ⅱ(MHC-Ⅱ)，monocyte chemotactic protein 1(MCP-1)，M2 markers CD206，CD163，CD209 mRNA expression，pro-inflammatory factors interleukin-1β(IL-1β)，tumor necrosis factor-α(TNF-α)，anti-inflammatory factors IL-4，IL-10 levels and mRNA expression，and key proteins in the NF-κB signaling pathway，such as nuclear NF-κBp65，NF-κBp50，and NF-κB inhibitor α(IκBα).Results:In the model group，M1 markers，pro-inflammatory factors，and NF-κBp65，NF-κBp50 proteins were significantly higher than those in the blank group(P<0.05)，while CD206，IL-4 mRNA，IκBα protein，and IL-4 levels were lower than those in the blank group(P<0.05).In the inhibitor and ZGJXF groups，M1 markers，pro-inflammatory factors，and NF-κBp65，NF-κBp50 proteins were lower than those in the model group(P<0.05)，while M2 markers，anti-inflammatory factors，and IκBα protein were higher than those in the model group(P<0.05).The ZGJXF group had lower levels of MHC-Ⅱ，MCP-1 mRNA，and pro-inflammatory factors than the inhibitor group(P<0.05)，and higher levels of CD206，CD209，IL-10 mRNA，IL-4，and IL-10(P<0.05).Conclusion:ZGJXF can inhibit lipopolysaccharide-induced M1 polarization of macrophages and promote M2 polarization.The mechanism may be related to the reduction of the activity of the NF-κB signaling pathway in cells.