Effects of fatty acid-ethanol amine (FA-EA) derivatives on lipid accumulation and inflammation

IF 1.8 4区 医学 Q4 BIOCHEMISTRY & MOLECULAR BIOLOGY Lipids Pub Date : 2023-03-21 DOI:10.1002/lipd.12368
Mengyu Li, Xiaoqing Huang, Mengxian Huang, Wenhui Jin, Zhuan Hong, Yucang Zhang, Hua Fang, Weizhu Chen
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Abstract

This study aimed to investigate the effect of fatty acid-ethanol amine (FA-EA) derivatives (L1L10) on the mitigation of intracellular lipid accumulation and downregulation of pro-inflammatory cytokines in vitro. First, the series of FA-EA derivatives were synthesized and characterized. Then, their cytotoxic, intracellular lipid accumulation and inhibition of pro-inflammatory cytokines were evaluated. The oil red O staining experiment showed that the tested compounds L4, L6, L8, L9, and L10 could reduce intracellular lipid accumulation induced by palmitic acid (PA). Moreover, ω-3/ω-6 PUFA-EA derivatives showed inhibitory effect on the production of pro-inflammatory cytokines in lipopolysaccharide (LPS) -stimulated RAW 264.7 cells. ω-3/ω-6 PUFA-EA derivatives at a concentrations of 10 μM could significantly decrease mRNA levels of IL-6, IL-1β, and TNF-α, inhibit NO production, and alleviate the protein expression of IL-1β in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells. These data suggest that ω-3 PUFA-EA derivatives can be beneficial for further pharmaceutical development to treat chronic low-grade inflammation diseases such as obesity.

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脂肪酸-乙醇胺(FA-EA)衍生物对脂质积累和炎症的影响
本研究旨在探讨脂肪酸-乙醇胺(FA-EA)衍生物(L1-L10)在体外减轻细胞内脂质积累和下调促炎细胞因子的作用。首先,合成了一系列FA-EA衍生物并进行了表征。然后,评估它们的细胞毒性、细胞内脂质积累和促炎细胞因子的抑制作用。油红O染色实验表明,所测化合物L4、L6、L8、L9、L10均能降低棕榈酸(PA)诱导的细胞内脂质积累。此外,ω-3/ω-6 PUFA-EA衍生物对脂多糖(LPS)刺激的RAW 264.7细胞中促炎细胞因子的产生有抑制作用。ω-3/ω-6 PUFA-EA衍生物在10 μM浓度下可显著降低脂多糖(LPS)刺激的RAW 264.7细胞中IL-6、IL-1β和TNF-α的mRNA水平,抑制NO的产生,减轻IL-1β的蛋白表达。这些数据表明ω-3 PUFA-EA衍生物可能有利于进一步的药物开发,以治疗慢性低度炎症疾病,如肥胖。
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来源期刊
Lipids
Lipids 生物-生化与分子生物学
CiteScore
4.20
自引率
5.30%
发文量
33
审稿时长
4-8 weeks
期刊介绍: Lipids is a journal of the American Oil Chemists'' Society (AOCS) that focuses on publishing high-quality peer-reviewed papers and invited reviews in the general area of lipid research, including chemistry, biochemistry, clinical nutrition, and metabolism. In addition, Lipids publishes papers establishing novel methods for addressing research questions in the field of lipid research.
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