Background and Aim Telmisartan （Telm）,one of peroxisome proliferator-activated receptor gamma （PPARγ） agonist.To investigate the effects and potential mechanisms of Telmisartan on pro-inflammatory cytokine release and expression from lipopolysaccharide （LPS）-induced THP-1 mononuclear cells.Methods The human THP-1 mononuclear cells were cultured and randomly divided into 3 groups: control group,LPS group,and Telm group.After Telm group pre-incubated with Telm（10 μmol/L）for 2 h,Telm group and LPS group were both stimulated with LPS for 24 h.The expression of PPARγ,p-PPARγ,inhibitor of nuclear factor-kappa B （IκBα）,p-IκBα,NF-κB and p-NF-κB in total protein of cell extract of each group were measured by Western blot.The level of monocyte chemotactic protein 1 （MCP-1）,tumor necrosis factor alpha （TNF-α） and interleukin-6 （IL-6） in supernatant and cell of each group were measured by ELISA and RT-PCR.Results Compared with the control group,the expression of p-PPARγ,p-NF-κB,p-IκBα,MCP-1,TNF-α and IL-6 in the LPS group were significantly increased accompanied with the decrease of IκBα（P<0.05）,but there was no difference on the expression of NF-κB and PPARγ between the two groups（P>0.05）.Compared with the LPS group,the expression of p-NF-κB,p-IκBα,MCP-1,TNF-α and IL-6 in the Telm group were significantly decreased accompanied with the increase of IκBα and p-PPARγ（P<0.05）.There was still no difference on the expression of NF-κB and PPARγ between the two groups （P>0.05）.Conclusion Telmisartan pretreatment can inhibit inflammation induced by LPS-stimulating THP-1 mononuclear cells,and the mechanisms may be related to preventing NF-κB activation through further PPARγ activation.