Aim To explore the possible mechanism by which probucol influenced cellular cholesterol efflux,and observe effects of serum from the mice pretreated by probucol on cellular cholesterol efflux. Methods Male C57BL/6J mice （n16） were randomly divided into two groups and treated with either vehicle or 0.5% probucol for 4 weeks respectively,the serum was collected and the lipids profile was detected by enzymatic method. Macrophages were loaded with ac-LDL and labeled with ³H-cholesterol,and treated with different concentrations of probucol,then the efflux of cholesterol was quantitated using the serum mentioned above as the acceptors. mRNA and membrane protein of the treated cells were extracted and used to evaluate the mRNA and protein expression of ABCA1,ABCG1 and SR-BI. Results More cholesterol efflux from the cultured macrophages was mediated by the serum from the mice treated with probucol for 4 weeks than those from the control mice. Probucol dose-dependently promoted cholesterol efflux and up-regulated the mRNA and protein expression of ABCG1 in macrophages,while had no effect on the mRNA and protein expression of SR-BI and ABCA1. Conclusions The serum from the mice pretreated with probucol markedly promoted macrophages cholesterol efflux. Probucol maybe promoted cholesterol efflux from the macrophages through increasing the expression of ABCG1 but had no relation to the expression of ABCA1 and SR-BI.