Abstract: Background and Objective: Triptolide (TPL) is an extracts of the root of Chinese herb Tripterygium, which have anti-carcinogenesis effects, immunosuppressive and anti-inflammatory response. The present study was designed to evaluate the anti-inflammation effect of triptolide. Methodology: The endotoxemia models were established by intraperitoneally (i.p.) injecting 30 mg kg–1 purified LPS in BALB/c mice. The treatment groups were injected intraperitoneally different doses (1.0, 2.0 and 5.0 mg kg–1 ) of TPL 30 min before LPS infusion. Survival rate was monitored for 7 days and serum TNF-α, ALT and BUN levels were determined. In vitro, endotoxemia cell models were established by given 1 μg mL–1 LPS in RAW 264.7 murine macrophage cell. The concentration of TNF-α and IL-1β was detected and the protein levels of TNF-α and IL-1β were determined. Results: A rise TNF-α and IL-1β level in serum and the increase of BUN and ALT level. While TPL treatment significantly increased survival rate in LPS-induced endotoxemia mice model, decreased the levels of ALT, BUN and serum TNF-α and IL- 1β. In vitro, LPS-induced TNF-α and IL-1β production was inhibited by TPL. Conclusion: These findings suggested that TPL had the ability of antiendotoxemia and protecting LPS-induced organ injuries by decreasing TNF-α and IL-1β level.