Aim To investigate the effect of paeoniflorin (PF) on secretion of inflammatory factors and expression of ATP-binding cassette transporter A1 (ABCA1) in THP-1 cells. Methods After pretreatment with PF (10－8,0－7,0－6,0－5 and 10－4 mol/L) for 0.5 h, THP-1 cells was co-treated by LPS (1 mg/L) and PF for 24 h. Levels of interleukin-1β (IL-1β), interleukin-6 (IL-6), interleukin-8 (IL-8) and tumor necrosis factor-α (TNF-α) in supernatant of cell culture medium were tested by enzyme linked immunosorbent assay (ELISA). Expression of ABCA1 in THP-1 cells were measured by Western blot. Results Compared with control group, the levels of IL-1β, IL-6, IL-8 and TNF-α in supernatant of cell culture medium were significantly increased (all P＜0.05) and expression of ABCA1 was significantly down-regulated in LPS group (P＜0.05). Compared with LPS group, the levels of IL-1β, IL-6, IL-8 and TNF-α in supernatant of cell culture medium were significantly decreased (all P＜0.05) and expression of ABCA1 was significantly up-regulated in LPS＋PF (10－6,0－5 and 10－4 mol/L) group (all P＜0.05). Conclusion Paeoniflorin inhibits the secretion of inflammatory factors and down-regultion of ABCA1 expression induced by LPS in THP-1 cells.