Aim of work To determine whether talosin A inhibits production of pro-inflammatory cytokines and nitric oxide (NO) in lipopolysaccharide (1 mu g/ml)-stimulated RAW 264.7 macrophages. Talosin A (10 and 50 mu g/ml) significantly reduced LPS-induced overproduction of tumor necrosis factor-alpha, interleukin IL-1 beta, -6 and NO in a dose-dependent manner (P < 0.01). Talosin A had a direct NO-scavenging activity in the cell-free system. In RT-PCR analysis, gene expressions were inhibited at a transcriptional level. Moreover, the activation of nuclear factor-kappa B (NF-kappa B) was significantly suppressed by talosin A in LPS-stimulated macrophage cells (P < 0.05). Therefore, we confirmed anti-inflammatory activity of talosin A was via suppression of pro-inflammatory cytokines, NO production and NF-kappa B activation, suggesting a therapeutic candidate for inflammatory disorders.