Curcumol exhibits anti-inflammatory properties by interfering with the JNK-mediated AP-1 pathway in lipopolysaccharide-activated RAW264.7 cells
Curcumol exhibits anti-inflammatory properties by interfering with the JNK-mediated AP-1 pathway in lipopolysaccharide-activated RAW264.7 cells
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Curcumol 通过干扰脂多糖激活的 RAW264.7 细胞中 JNK 介导的 AP-1 通路而表现出抗炎特性
DOI：
10.1016/j.ejphar.2013.11.007
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发表时间：
2014-01-15
影响因子：
5
通讯作者：
Qi, Yun
中科院分区：
文献类型：
--
作者：
Chen, Xi;Zong, Chuanjie;Qi, Yun
丹皮酚是中药大黄挥发油的主要成分之一，具有抗炎作用。然而，这种化合物的抗炎活性和潜在的分子机制仍不清楚。本研究探讨莪术醇对脂多糖（LPS）诱导的RAW264.7细胞的抗炎作用沿着机制。我们发现莪术醇通过抑制iNOS mRNA表达和蛋白水平而不是iNOS活性来抑制PS诱导的NO产生。此外，莪术醇在转录和翻译水平上抑制PS诱导的TNF-α、IL-1 β和IL-6的产生。进一步的研究表明这些作用主要是通过抑制JNK介导的AP-1而不是NF-κ B通路发挥作用;这些作用包括降低JNK的磷酸化水平和直接抑制p-JNK的活性。这些数据提供了科学的分子证据，莪术醇可能是一个潜在的先导化合物的一种新型抗炎药物，因为它的抑制活性的各种炎症介质的产生。(C)2013爱思唯尔有限公司版权所有。
Curcumol is one of the major components of the essential oil of Rhizoma Curcumae, a common traditional Chinese medicine with anti-inflammatory properties. However, the anti-inflammatory activity and the underlying molecular mechanisms of this compound remain unclear. In the present study, the anti-inflammation effect of curcumol on lipopolysaccharide (LPS)-induced RAW264.7 cells is demonstrated along with its underlying mechanisms. We show that curcumol inhibits [PS-induced NO production by suppressing iNOS mRNA expression and protein level but not iNOS activity. Moreover, curcumol inhibits [PS-induced production of TNF-alpha, IL-1 beta and IL-6 at both the transcriptional and translational levels. Further investigations reveal that these effects mainly act via suppressing JNK-mediated AP-1 rather than the NF-kappa B pathway; these effects include a decrease in the phosphorylation level of JNK and a direct inhibition of the activity of p-JNK. These data provide scientific molecular evidence that curcumol may be a potential lead compound for a novel anti-inflammatory drug because of its inhibitory activity on the production of various inflammatory mediators. (C) 2013 Elsevier B.V. All rights reserved.