食品科学 ›› 2020, Vol. 41 ›› Issue (5): 152-158.doi: 10.7506/spkx1002-6630-20190124-309

• 营养卫生 • 上一篇    下一篇

6 种5,7-二羟基黄酮对巨噬细胞M1极化的影响

郑梦菲,刘健,屈玮   

  1. (合肥工业大学食品与生物工程学院,安徽 合肥 230009)
  • 出版日期:2020-03-15 发布日期:2020-03-23
  • 基金资助:
    安徽省自然科学基金项目(1508085MC58)

Inhibitory Effects of Six 5,7-Dihydroxyflavones on M1 Polarization of Macrophages

ZHENG Mengfei, LIU Jian, QU Wei   

  1. (School of Food and Biological Engineering, Hefei University of Technology, Hefei 230009, China)
  • Online:2020-03-15 Published:2020-03-23

摘要: 目的:探究木犀草素、槲皮素、杨梅素、芹菜素、山柰酚及白杨素这6 种黄酮对RAW264.7巨噬细胞极化的抑制活性及构效关系。方法:选择100 ng/mL脂多糖刺激RAW264.7巨噬细胞建立炎症模型;利用噻唑蓝法检测细胞增殖活性;流式细胞术检测细胞表面蛋白CD274和CD38表达;Western blot检测炎性信号通路中相关蛋白的表达;定量聚合酶链式反应检测M1型巨噬细胞标记基因水平。结果:6 种黄酮在20 μmol/L下均不影响细胞正常生长;6 种黄酮对巨噬细胞CD274和CD38表达均有抑制作用,其中木犀草素、芹菜素和白杨素的抑制作用强于槲皮素、杨梅素和山柰酚;木犀草素对核因子κB信号通路激活的抑制活性强于芹菜素和槲皮素,而杨梅素、山柰酚和白杨素没有明显抑制效果;木犀草素、芹菜素和白杨素抑制iNOS mRNA表达的活性强于其他3 种化合物,木犀草素、槲皮素和芹菜素抑制IL-1β及MCP1 mRNA表达的活性强于其他3 种化合物。结论:C环上3 位的羟基取代不利于黄酮类化合物抑制巨噬细胞M1极化的活性,而B环上3’、4’位羟基取代有利于增强其活性。

关键词: 黄酮类化合物, 巨噬细胞, 极化, 炎性, 构效关系

Abstract: Purpose: The aim of this study was to evaluate the inhibitory effects of six flavonoids (luteolin, quercetin, myricetin, apigenin, kaempferol and chrysin) on M1 polarization of RAW264.7 macrophages and to delineate the structural determinants involved in their activity. Methods: Lipopolysaccharide (LPS) at 100 ng/mL was used to stimulate RAW264.7 macrophages to establish an inflammation model. Cell proliferation activity was detected by 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide assay. The expression of CD274 and CD38 was detected by flow cytometry. The expression of proteins involved in the inflammatory signaling pathway was detected by Western blotting. The expression levels of M1-type macrophage marker genes were detected by real-time polymerase chain reaction (PCR). Results: All these flavonoids had no significant effect on cell proliferation at 20 μmol/L, but inhibited the expression of CD274 and CD38, with luteolin, apigenin and chrysin being more effective than quercetin, myricetin and kaempferol. The inhibitory activity of luteolin on activation of the nuclear factor κB signaling pathway was stronger than that of apigenin and quercetin, while the other flavonoids had no significant effect. The inhibitory effect of luteolin, apigenin and chrysin on the mRNA expression of inducible nitric oxide synthase (iNOS) was stronger than that of the other three compounds, and the inhibitory effect of luteolin, quercetin and apigenin on the mRNA expression of interleukin-1β (IL-1β) and monocyte chemotactic protein 1 (MCP1) was stronger than that of the other compounds. Conclusion: Hydroxylation at position 3 on the C ring is not conducive to the inhibition of flavonoids on macrophage polarization, while hydroxylation at positions 3’ and 4’ on the B ring are beneficial to enhance their activity.

Key words: flavonoids, macrophages, polarization, inflammation, structure-activity relationship

中图分类号: