The study aims to illustrate the effect of diphenylheptane A on the glycerophospholipids metabolism in the inflammatory process through analyzing glycerophospholipids components of RAW264.7 cells under different status(control，inflammation，administration) and screening potential pathological and pharmacological biomarkers.RAW264.7 cells were randomly divided into four groups：control group(C)，inflammation group(L)，diphenylheptane A(D)，ibuprofen(B，positive control).C and L were treated with fresh medium while D and B were treated with medium containing 20μg/mL diphenylheptane A or 100μg/mL ibuprofen，respectively.1 h later，lipopolysaccharide(LPS) was added to L，D and B at a final concentration of 0.5μg/mL.24 h later，glycerophospholipids in RAW264.7 cells of four groups were extracted by modified Bligh-Dyer method and analyzed by ultra performance liquid chromatography tandem quadrupole time-of-flight mass spectrometry(UPLC-Q/TOF MS) in both positive and negative ion modes.Then，glycerophospholipids components were identified by combination of MS/MS fragment ions information，element composition in MassLynx 4.1 and the Lipid Maps database.Finally，potential pathological and pharmacological biomarkers were screened by unsupervised principal component analysis(PCA)，supervised partial least squares-discriminate analysis(PLS-DA)，supervised orthogonal partial least squares discriminate analysis(OPLS-DA)，and Student’s t-test(P<0.05).The results showed that 27 potential pathological biomarkers were found by comparing C and L，23 potential pharmacological biomarkers were found by comparing D and L，and 17 potential pharmacological biomarkers were found by comparing B and L.The biomarkers mainly included phosphatidylcholine(PC)，lysophosphatidylcholine(lysoPC)，phosphatidylethanolamine(PE) and lysophosphatidylethanolamine(lysoPE).It was found that diphenylheptane A led to obvious changes of glycerophospholipids metabolism during the process of inflammation，which were closely related to the occurrence and development of inflammation.