Artesunate attenuates foam cell formation by enhancing cholesterol efflux

Background Atherosclerosis is the main cause of many cardiovascular diseases and the second leading cause of death in elderly people. The formation of intimal macrophage-derived foam cells is a major feature of early atherosclerotic lesions. Little is known about the effects of artesunate (ART) on macrophage-derived foam cell formation. Methods Oil red O staining was employed to detect foam cell formation; colorimetric analysis was employed for cholesterol measurement; quantitative real time polymerase chain reaction (qRT-PCR) and western blot analysis were employed to assess messenger RNA (mRNA) and protein expression, respectively; enzyme-linked immunosorbent assay (ELISA) analyses were used to observe interleukin 6 (IL-6) and tumor necrosis factor-α (TNF-α) release; and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assays were used to examine cell viability. Results It was revealed that ART attenuated oxidized low-density lipoprotein (ox-LDL)-induced foam cell formation from THP-1-derived macrophages by decreasing cholesterol accumulation, and the effect might have occurred via enhanced cholesterol efflux. Additionally, ART decreased toll-like receptor 4 (TLR4) expression, increased adenosine triphosphate (ATP)-binding cassette transporter A1 (ABCA1) and ATP-binding cassette transporter G1 (ABCG1) expression, and reduced the secretion of IL-6 and TNF-α. Conclusions This study showed that ART attenuated the ox-LDL-induced formation of foam cells from THP-1-derived macrophages by increasing ABCA1 and ABCG1 expression via inhibiting TLR4 expression and reducing TNF-α and IL-6 secretion from macrophages induced by ox-LDL, which ultimately decreased the accumulation of cholesterol. It is worthwhile further investigate ART as a potential drug for the treatment of atherosclerosis.