Preventive effect of bis-eugenol, a eugenol ortho dimer, on lipopolysaccharide-stimulated nuclear factor kappa B activation and inflammatory cytokine expression in macrophages
Preventive effect of bis-eugenol, a eugenol ortho dimer, on lipopolysaccharide-stimulated nuclear factor kappa B activation and inflammatory cytokine expression in macrophages
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DOI：
10.1016/s0006-2952(03)00419-2
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发表时间：
2003-09-15
影响因子：
5.8
通讯作者：
Fujisawa, S
中科院分区：
文献类型：
--
作者：
Murakami, Y;Shoji, M;Fujisawa, S
丁香酚具有抗氧化和抗炎活性，但在较高浓度时可作为氧化剂和有效的过敏原。早期的研究表明，丁香酚氧化合成的双丁香酚比丁香酚具有更低的细胞毒性和更高的抗氧化性。但其抗炎机制尚不清楚。由于核因子-kappaB(NF-kappaB)是炎性细胞因子表达的关键转录因子，我们研究了丁香酚和双丁香酚是否能抑制核因子-kappaB的激活。我们观察到，双丁香酚，而不是丁香酚，能明显抑制脂多糖刺激的RAW264.7小鼠巨噬细胞中抑制的kappaB-α的降解，从而抑制刺激的核因子-kappaB在细胞中的转录活性。此外，双丁香酚实际上在基因和蛋白水平上抑制了内毒素刺激的炎性细胞因子的表达。这些发现表明，双丁香酚是一种有效的核因子-kappaB抑制剂。(C)2003 Elsevier Inc.保留所有权利。
Eugenol exhibits antioxidant and anti-inflammatory activities, but at higher concentrations acts as an oxidant and potent allergen. It was earlier shown that bis-eugenol synthesized by the oxidation of eugenol was less cytotoxic and more highly antioxidative than eugenot. But its anti-inflammatory mechanism remains yet unclear. Since nuclear factor-kappaB (NF-kappaB) is a key transcriptional factor in the expression of inflammatory cytokines, we examined whether eugenol and bis-eugenol are inhibitors of NF-kappaB activation. We observed that bis-eugenol, but not eugenol, clearly inhibited the degradation of inhibitory kappaB-alpha in RAW264.7 murine macrophages stimulated with lipopolysaccharide and, consequently, the transcriptional activity of the stimulated NF-kappaB in the cells. In addition, bis-eugenol actually inhibited LPS-stimulated expression of inflammatory cytokines at both gene and protein levels. These findings suggest that bis-eugenol acts as a potent inhibitor of NF-kappaB. (C) 2003 Elsevier Inc. All rights reserved.