Aim To investigate whether angiopoietin-1 (Ang-1) regulates ATP-binding cassette transporter A1 (ABCA1), ABCG1 expression and cholesterol efflux through liver X receptor α (LXRα) in THP-1 derived macrophages. Methods THP-1 cells were incubated with 160 nmol/L phorbol ester to transform into macrophages. Subsequently, THP-1 derived macrophages were exposed to 50 mg/L oxidized low density lipoprotein (ox-LDL) and cultured with typical approaches. The experimental groups were divided into control group and Ang-1 group. Liquid scintillation counter was used to determine the efficiency of cholesterol efflux. Lipids contents were tested with high performance liquid chromatogram (HPLC). Real-time PCR and Western blot were used to quantify the expression of ABCA1, ABCG1. THP-1 derived macrophages were pretreated with LXRα angonists T0901317 or inhibitors GGPP, respectively. Results Ang-1 obviously reduced cholesterol efflux, and downregulated ABCA1, ABCG1 expression. LXRα angonists T0901317 interfered Ang-1-inhibited ABCA1, ABCG1 expression and cholesterol efflux. Conclusion Ang-1 decreased THP-1 derived macrophages cholesterol efflux in a LXRα dependent manner and downregulated ABCA1, ABCG1 expression.