In this study we explored that whether PDE inhibitor rolipram affected cholesrterol efflux and ABCA1 expression in THP-1 macrophage foam cells. Cholesterol efflux in THP-1 macrophage-derived foam cells were detected by FJ-2107P type liquid scintillator. The expression of ABCA1 mRNA and protein were determined by RT-PCR and Western blotting respectively. The levels of cAMP were analysed by low PH EIA. The method of liquid scintillator confirmed PDE inhibitor rolipram promoted cholesterol efflux in THP-1 macrophage foam cells with a time-dependent manner. The results of RT-PCR and Western blotting proved that in THP-1 macrophage-derived foam cells, rolipram increased the levels of ABCA1 mRNA and protein with time, respectively, HPLC testified that rolipram time-dependent decreased the levels of cholesterol and cholesterol ester and upgratulated cAMP in THP-1 macrophage-derived foam cells. Therefore, PDE specific inhibitor rolipram may increase cholesterol efflux and promote ABCA1 expression in THP-1 macrophage-derived foam cells. This study reveals a novel therapy strategy for atherosclerosis.