Aim To study the influence of probucol on the Toll-like receptor 4(TLR4)/nuclear factor-κB(NF-κB) signaling pathway of peripheral blood mononuclear cells in type 2 diabetic mellitus patients with coronary heart disease,so as to further investigate the anti-atherosclerosis mechanism of probucol.Methods 85 patients with type 2 diabetes and carotid atherosclerosis were divided into two groups: probucol treatment group(n=43),and control group(n=42).The treatment group were treated with probucol 0.375 g,2 times a day for 24 weeks.The effect of probucol on TLR4,NF-κB expression of peripheral blood monouclear cells was detected by Real-time PCR and Western blotting analysis before and after probucol treatment.The expression of interleukin-1β(IL-β) was detected by ELISA.Results Probucol obviously decreased levels of total cholesterol(TC),triglyceride(TG),low density lipoprotein cholesterol(LDLC) and oxidized low density lipoprotein(ox-LDL) in plasma of type 2 diabetes.The expressions of TLR4,NF-κB and IL-β of peripheral blood mononuclear cells were significantly lower in probucol treatment group than that in control(P<0.05).Conclusions Probucol can not only regulate serum lipids,but also has the action of anti-atherosclerosis through inhibiting TLR4/NF-κB expression,which indicate that probucol might have the preventive and treatment role in patients with type 2 diabetes and atherosclerosis.