Apigenin-7-O-β-D-glucuronide inhibits modified low-density lipoprotein uptake and foam cell formation in macrophages

Cirsium japonicum DC is a perennial thistle widely distributed in China and has been reported to exhibit various pharmacological activities. Little research has been reported about its chemical constituents with anti-atherosclerotic activity. We investigated the active compounds in C. japonicum through ox-LDL-induced macrophages cell model, and identified an effective compound, apigenin-7-O-β-D-glucuronide, which is first reported in C. japonicum. The anti-atherosclerotic activity of apigenin-7-O-β-D-glucuronide was determined by measuring ox-LDL-induced foam cell formation in RAW 264.7 macrophages. Apigenin-7-O-β-D-glucuronide inhibited the uptake of ox-LDL by macrophage and the accumulation of triglyceride in cells. Further research showed that apigenin-7-O-β-D-glucuronide inhibited the scavenger receptor CD36 mRNA and protein expression, and enhanced the expression of scavenger receptor class B type 1, likely resulting from inhibiting the phosphorylation of ERK1/2. Taken together, these results suggest that apigenin-7-O-β-D-glucuronide may be a therapeutic candidate for treating atherosclerosis as well as a dietary complement for health promotion.