Department of Pharmacology, School of Medicine, and Institute of Health Sciences, Gyeongsang National University, 92 Chilam-dong, Jinju 660-751, Republic of Korea.
J Ethnopharmacol. 2011 Jan 27;133(2):524-30. doi: 10.1016/j.jep.2010.10.029. Epub 2010 Oct 20.
The methanol extracts of Carthamus tinctorius (MEC) have long been used in traditional medicine as anti-inflammatory agent, however, the molecular mechanism by which MEC shows anti-inflammatory action is not investigated.
Induction of heme oxygenase-1 (HO-1) by many medicinal herbs has been reported excellent anti-inflammatory action. Thus, the aim of the study is to explore whether anti-inflammatory action of MEC is related with HO-1 induction in RAW 264.7 cells.
The present study was designed to investigate as to MEC induces HO-1 expression so that it reduces inflammation by suppression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) expression in cells activated with lipopolysaccharide (LPS).
Expression of HO-1 protein by MEC in macrophages was increased in a concentration- and time-dependent manner. Treatment with MEC significantly inhibited upregulation of both iNOS and COX-2 in LPS-activated macrophages and consequently reduced production of NO and PGE(2), respectively. The reduced expression of iNOS and COX-2 by MEC was reversed by siHO-1 RNA transfection. In addition, NF-E2-related factor (Nrf2) was translocated from cytosol to nucleus by MEC. The binding of NF-κB as well as NF-κB luciferase activity was also significantly diminished by MEC. Finally, tumor necrosis factor (TNF)-α-mediated VCAM-1 expression in endothelial cell was significantly inhibited by MEC.
The present results show that MEC induces HO-1 expression via Nrf2 translocation and inhibits NF-κB activity, which may be responsible for anti-inflammatory action. Therefore, we propose that anti-inflammatory action of MEC involves at least HO-1 induction.
红花（Carthamus tinctorius）的甲醇提取物在传统医学中一直被用作抗炎剂，然而，其发挥抗炎作用的分子机制尚未得到研究。
许多草药诱导血红素加氧酶-1（HO-1）的表达已被报道具有出色的抗炎作用。因此，本研究旨在探讨红花甲醇提取物（MEC）的抗炎作用是否与 RAW 264.7 细胞中 HO-1 的诱导有关。
本研究旨在研究 MEC 是否通过诱导 HO-1 表达来减轻炎症，从而通过抑制脂多糖（LPS）激活的细胞中诱导型一氧化氮合酶（iNOS）和环氧化酶-2（COX-2）的表达来减轻炎症。
MEC 在巨噬细胞中诱导 HO-1 蛋白的表达呈浓度和时间依赖性增加。MEC 处理可显著抑制 LPS 激活的巨噬细胞中 iNOS 和 COX-2 的上调，并分别降低 NO 和 PGE2 的产生。MEC 逆转了 siHO-1 RNA 转染对 iNOS 和 COX-2 表达的下调。此外，MEC 将核因子-E2 相关因子 2（Nrf2）从细胞质易位到细胞核。MEC 还显著减弱了 NF-κB 的结合以及 NF-κB 荧光素酶活性。最后，MEC 显著抑制了肿瘤坏死因子（TNF）-α介导的内皮细胞 VCAM-1 的表达。
本研究结果表明，MEC 通过 Nrf2 易位诱导 HO-1 表达，并抑制 NF-κB 活性，这可能是其抗炎作用的原因。因此，我们提出 MEC 的抗炎作用至少涉及 HO-1 的诱导。
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