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

• Published in: Journal of functional foods Vol. 35; pp. 615 - 621
• Main Authors: Ma, Qin, Zhang, Xi-Mei, Jiang, Jian-Guo, Zhu, Wei
• Format: Journal Article
• Language: English
• Published: Elsevier Ltd 01.08.2017; Elsevier
• Subjects: Apigenin-7-O-β-D-glucuronide; Atherosclerosis; Foam cell; ox-LDL; ox-LDL; Foam cell; Apigenin-7-O-β-D-glucuronide; Atherosclerosis
• ISSN: 1756-4646; 2214-9414
• DOI: 10.1016/j.jff.2017.06.026

•Apigenin-7-O-β-D-glucuronide (APG) is first separated from C. japonicum.•APG strongly inhibited ox-LDL-induced macrophage foam cell formation.•APG suppressed lipid droplets accumulation and LDL uptake in RAW 264.7 cells.•APG displayed anti-atherosclerotic activity by inhibiting ERK1/2 activation. 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.