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Aim: To investigate the effects of triptolide, a diterpenoid triepoxide from Tripterygium wilfordii Hook F (TWHF), on the co-stimulatory molecule expression and interleukin- 12 (IL-12) production from THP-1 cells. Methods: THP-1 cells were differentiated into macrophage-like cells by Me2SO, and then cultured with IFN-γ(500 kU/L) and lipopolysaccharide (LPS) (1 mg/L) with or without triptolide. The surface molecule expressions were analyzed on a FACScan flow cytometer. IL-12p40, IL-12p70 were assayed by ELISA. Results: Tripolide suppressed CD80 and CD86 expressions on IFN-γ (500 kU/L) and LPS (1 mg/L) activated THP-1 cells at nontoxic dosages of 2.5-0.625 μg/L. Furthermore, the production of IL-12p40 and IL-12p70 were also significantly reduced in THP-1 cells exposed to triptolide. Conclusion: Triptolide impairs the antigen-presenting function by inhibiting CD80 and CD86 expressions and decreased IL-12p40 and IL-12p70 (bioactive form) pro ductions from the activated THP-1 cells.