Ethnopharmacological relevance: Ligustrum purpurascens, named as "Ku ding cha", has been used as a kind of functional tea in southern China for about two thousand years, Which has the effects on diuresis, anti-hypertension, weight-loss and anti-inflammation. The aim of the study: This study was aimed to investigate the immune enhancement effects of the crude phenylethanoid glycosides (CPGs) from Ligustrum. Purpurascens on mice and analyze the chemical profiles of phenylethanoid glycosides in the CPGs. Materials and methods: The immune functions enhancing potential of CPGs was determined using serum hemolysin antibody, phagocytosis, splenocyte antibody production, and NK cells activity assays. The contents of five major constituents in the crude glycosides of Ligustrum purpurascens were determined by using liquid chromatography, other five glycosides were deduced according to their UV and MS spectra compared with the literature as well. Results: In the immunizing experiment, mice treated with different doses of CPGs showed an increase (p < 0.01) in the haemagglutination titre compared with the control group. The increases (p < 0.05) were found to be significant at doses of 440 mg/kg and 132 g/kg in the experiments of antibody production of spleen cells, M Phi phagocytosis of chicken RBCs and NK cell activity. Further chemical characterization yielded 10 constituents from CPGs, five glycosides were quantified by HPLC and the structures of other five compounds were speculated according to their UV and MS spectra. Conclusion: The results suggested that phenylethanoid glycosides from Ligustrum purpurascens have immunomodulatory effects on mice. Crown Copyright (C) 2012 Published by Elsevier Ireland Ltd. All rights reserved.