Inhibitory effect of 2'-hydroxycinnamaldehyde on nitric oxide production through inhibition of NF-κB activation in RAW 264.7 cells
Inhibitory effect of 2'-hydroxycinnamaldehyde on nitric oxide production through inhibition of NF-κB activation in RAW 264.7 cells
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DOI：
10.1016/j.bcp.2004.11.013
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发表时间：
2005-03-01
影响因子：
5.8
通讯作者：
Hong, JT
中科院分区：
文献类型：
--
作者：
Lee, SH;Lee, SY;Hong, JT
肉桂已广泛用于治疗消化不良、胃炎和炎症性疾病。在本研究中，基于从肉桂树皮中分离的 2-羟基肉桂醛，从各种肉桂酸合成了几种肉桂醛衍生物。研究比较了它们在 Raw 264.7 细胞中的 NO 产量和 NF-κB 活性，因为一氧化氮 (NO) 和 NF-κB 已被证明是炎症性疾病的相关因素。结果表明，在衍生物中，HCA 以剂量依赖性方式最显着地抑制脂多糖 (LPS) 诱导的 NO 产生和 NF-κB 转录活性，IC50 值分别为 8 和 22 μM。接下来我们研究了 HCA 对 NO 产生抑制作用的可能机制。 HCA 对 NO 的抑制作用与 LPS 诱导的诱导型一氧化氮合酶 (iNOS) 表达的抑制作用一致。此外，HCA 抑制 LPS 诱导的 p50 和 p65 易位，从而抑制 iNOS 的中央调节因子 NF-kappaB 的 DNA 结合活性。目前的结果证明，在肉桂醛衍生物中，HCA 通过抑制 NF-κB 激活对 NO 产生具有最强的抑制作用，因此可以用作抗炎剂。 (C) 2004 Elsevier Inc. 保留所有权利。
Cinnamomum cassia has been widely used for treating dyspepsia, gastritis, and inflammatory disease. In the present study, several of cinnamaldehyde derivatives were synthesized from various cinnamic acid based on the 2-hydroxycinnamaldehyde isolated from the bark C. cassia Blume was investigated to compare their NO production and NF-kappaB activity from Raw 264.7 cell since nitric oxide (NO) and NF-kappaB have been shown to be implicated factors in the inflammatory disease. The results show that HCA, among the derivatives, most significantly inhibited lipopolysaccharide (LPS)-induced NO production and NF-kappaB transcriptional activity in a dose-dependent manner with an IC50 value of 8 and 22 muM, respectively. We next investigated putative possible mechanisms of inhibitory effect of HCA on NO production. The inhibition of NO by HCA was consistent with the inhibitory effect on LPS-induced inducible nitric oxide synthase (iNOS) expression. Moreover, HCA inhibited LPS-induced p50 and p65 translocation resulting in the inhibition of the DNA binding activity of the NF-kappaB, a central regulator of iNOS. The present results provided evidence that HCA, among cinnamaledhyde derivatives, has the most inhibitory effect on NO production through inhibition of NF-kappaB activation, and thus can be used as an anti-inflammatory agent. (C) 2004 Elsevier Inc. All rights reserved.