In this study, THP–1 cells were induced into macrophages and THP–1 macrophage–derived foam cell by phorbolmyristate acetate (PMA) and oxidized low–density lipoprotein (ox–LDL), and then treated with different concentrations(5, 10, 15 nmol/L) of ODP–Ia, to investigate the beneficial effects of ODP–Ia on the cholesterol accumulation in the THP–1 macrophage derived foam cell. Meanwhile, the mRNA expression and protein levels of ATP binding cassette transporter ABCA1, ATP binding cassette transporter ABCG1 and scavenger receptor class B type I (SR–BI) that mediate cholesterol efflux were observed. The result showed that, the lipid content and the cholesterol content were increased significantly after the THP–1 cells were induced into the THP–1 macrophage derived foam cell, and then were significantly decreased after treating with 15 nmol/L ODP–Ia. The data also demonstrated that, compared with the ox–LDL treated group, the high dose group (15 nmol/L ODP–Ia treated group)showed significantly increase in the mRNA and protein expressions of ABCA1, ABCG1 and SR–BI(P<0.05). However, the high dose group was inferior to the ezetimibe treated group (P<0.05).And there were no significant differences among the low dose (5 nmol/L) group, the medium dose (10 nmol/L) group and the ox–LDL treated group. In summary, ODP–Ia promoted cholesterol efflux of THP–1 macrophage derived foam cell by up–regulation of ABCA1, ABCG1 and SR–BI.