Asiaticoside has been tested for the ability as an anti-inflammatory drug using lipopolysaccharide (LPS)-stimulated macrophage cell line (RAW 264.7 cell). LPS treatment induced dramatically inducible nitric oxide synthase (iNOS) in RAW cells. However, asiaticoside inhibited LPS-stimulated iNOS induction in a concentration-dependent manner. Especially, higher concentrations (＞50 $mu extrm{M}$) of asiaticoside completely blocked iNOS induction. In addition, LPS-stimulated expression of inducible cyclooxygenase (COX-2) and interleukin-1 $alpha$ (IL-1 $alpha$) was inhibited by asiaticoside treatment. Asiaticoside up to 50 $mu extrm{M}$ still required to inhibit COX-2 and IL-1 $alpha$ induced by LPS. Consistent with these findings, treatment with asiaticoside suppressed do novo synthesis and cellular accumulation of prostaglandin $E_2$ to a lesser extent, suggesting that asiaticoside blocked the induction as well as the activity of COX-2 These results suggest the possibility that asiaticoside may be effective therapeutic agents for septic shock and other inflammatory diseases.