OBJECTIVE To compare the effect of ginsenoside Rg1 and its metabolite Rh1 on proinflammatory cytokines and their mRNA expression by THP-1 cells. METHODS Human peripheral blood mononuclear cells (PBMC) were incubated with Rg1 and Rh1 at concentrations of 0.1, 1, 10, and 100 mg/L, and the cell proliferation was measured 24 h after incubation. Radioimmunoassay (RIA) was used to detect the production of proinflammatory cytokines, TNF alpha, IL-1 alpha, and IL-8. TNF alpha mRNA level was detected by reverse transcription polymerase chain reaction (RT-PCR) after administration of Rg1 and Rh1. RESULTS Rg1 and Rh1 (at concentration of 0.1, 1, 10, 100 mg/L) had no effect on PBMC proliferation. Rh1 1 mg/L could upregulate the productions of TNF (and IL-8 induced by lipopolysaccharides (LPS) 10 mg/L plus phorbol myristate acetate (PMA) 200 nmol/L, however, Rg1 showed an inhibitory effect on TNF alpha production induced by LPS 100 mg/L. Rg1 1 mg/L and Rh1 100 mg/L enhanced the production of IL-1 alpha level in THP-1 cells in the presence of LPS 10 mg/L. RT-PCR revealed that Rh1 stimulated TNF alpha mRNA expression in suitable stimulatory conditions. CONCLUSIONS Rg1 and Rh1 have different effects on the production of cytokines produced THP-1 cells stimulated by LPS and PMA.