Department of NEUROFARBA, Section of Pharmacology and Toxicology, University of Florence, Viale Pieraccini 6, 50139 Florence, Italy.
Department of Agriculture, Food, Environment and Forestry (DAGRI), University of Florence, Piazzale delle Cascine 18, 50144 Florence, Italy.
Mar Drugs. 2021 Jun 11;19(6):334. doi: 10.3390/md19060334.
In this study, we compared the effects of a F&M-M36 methanolic extract with those of fucoxanthin (FX) at equivalent concentration, on lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. The F&M-M36 methanolic extract contained 4.7 mg of FX and 6.22 mg of gallic acid equivalents of phenols per gram. HPLC analysis revealed the presence of simple phenolic acid derivatives. The F&M-M36 extract exhibited a potent and concentration-dependent inhibitory activity against COX-2 dependent PGE2 production compared to FX alone. Compared to LPS, F&M-M36 extract and FX reduced the expression of IL-6 and of Arg1 and enhanced that of IL-10 and of HO-1; F&M-M36 extract also significantly abated the expression of NLRP3, enhanced mir-223 expression and reduced that of mir-146b, compared to LPS ( < 0.05). These findings indicate that F&M-M36 methanolic extract has a peculiar anti-inflammatory activity against COX-2/PGE2 and NLRP3/mir-223 that might be attributable to the known anti-inflammatory effects of simple phenolic compounds found in the extract that may synergize with FX. Our data suggest that F&M-M36 may serve as a source of anti-inflammatory compounds to be further evaluated in in vivo models of inflammation.
在这项研究中,我们比较了 F&M-M36 甲醇提取物与等量虾青素 (FX) 的作用,研究其对脂多糖 (LPS) 刺激的 RAW 264.7 巨噬细胞的影响。 F&M-M36 甲醇提取物每克含有 4.7 毫克 FX 和 6.22 毫克没食子酸当量的酚类物质。HPLC 分析表明存在简单的酚酸衍生物。与 FX 单独作用相比, F&M-M36 提取物表现出对 COX-2 依赖性 PGE2 产生的强大且浓度依赖性抑制活性。与 LPS 相比, F&M-M36 提取物和 FX 降低了 IL-6 和 Arg1 的表达,增强了 IL-10 和 HO-1 的表达;与 LPS 相比, F&M-M36 提取物还显著降低了 NLRP3 的表达,增强了 mir-223 的表达,降低了 mir-146b 的表达(<0.05)。这些发现表明, F&M-M36 甲醇提取物对 COX-2/PGE2 和 NLRP3/mir-223 具有独特的抗炎活性,这可能归因于提取物中已知的具有抗炎作用的简单酚类化合物,这些化合物可能与 FX 协同作用。我们的数据表明, F&M-M36 可能是抗炎化合物的来源,可以在体内炎症模型中进一步评估。