六种5,7-二羟基黄酮对巨噬细胞M1极化的影响

摘要/Abstract

摘要： 目的：探究木犀草素、槲皮素、杨梅素、芹菜素、山奈酚及白杨素这六种黄酮对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的脂多糖（lipopolysaccharide，LPS）刺激RAW264.7巨噬细胞建立炎症模型，实验分为空白对照组、LPS组和六种药物处理组。利用MTT检测细胞增殖活性；流式细胞术检测细胞表面蛋白CD274和CD38的表达；Western blot检测炎性信号通路中相关蛋白的表达；定量PCR检测M1型巨噬细胞标记基因的水平。结果：六种黄酮类化合物在20 μM下均不影响细胞正常生长；六种黄酮对巨噬细胞CD274和CD38表达均有抑制作用，其中木犀草素、芹菜素和白杨素的作用显著强于槲皮素、杨梅素和山奈酚；木犀草素抑制NF-κB信号通路激活的活性强于芹菜素和槲皮素，而槲皮素、杨梅素和山奈酚没有显著效果；木犀草素、芹菜素和白杨素抑制Nos2 mRNA表达的活性强于其他三种化合物，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三种化合物。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 inhibition effects of six flavonoids (luteolin, quercetin, myricetin, apigenin, kaempferol and chrysin) on M1 polarization in RAW264.7 macrophages and to delineate the structural determinants involved in their activity. Methods: 100 ng/mL of lipopolysaccharide (LPS) was used to stimulate RAW264.7 macrophages to establish an inflammatory model. Macrophages were divided into 8 groups: control, LPS, LU, QU, MY, AP, KA and CH groups. Cell proliferation activity was detected by MTT assay. The expressions of CD274 and CD38 were detected by flow cytometry. The expression of related protein in the inflammatory signaling pathway was detected by western blot. The levels of M1-type macrophage marker genes were detected by real-time PCR. Results: These flavonoids were no significant effect on cell proliferation at 20 μM. All the six flavonoids showed inhibition effects on the expression of CD274 and CD38, of which the effects of luteolin, apigenin and chrysin were significantly stronger than that of quercetin, myricetin and kaempferol. The inhibitory activity of luteolin on NF-κB signaling pathway was stronger than that of apigenin and quercetin. The effects of luteolin, apigenin and chrysin in inhibiting the expression of Nos2 mRNA was stronger than that of the other three compounds, and the effects of luteolin, quercetin and apigenin in inhibiting the expression of IL-1β and MCP1 mRNA was stronger than that of others. Conclusions: Hydroxylation at position 3 on ring C is not conducive to its activity on macrophage polarization, while the hydroxylations at positions 3' and 4' on the B ring are beneficial to enhance its activity.

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

中图分类号:

R151.4

郑梦菲刘健屈玮. 六种5,7-二羟基黄酮对巨噬细胞M1极化的影响[J]. 食品科学, 0, (): 0-0.

Jian LIU. Inhibition Effects of Six 5,7-Dihydroxyflavones on M1 Polarization in Macrophages[J]. FOOD SCIENCE, 0, (): 0-0.

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