Department of Chemistry and Biochemistry, The University of North Carolina Greensboro, Box 26170, Greensboro, NC 27402, USA.
Int Immunopharmacol. 2010 Oct;10(10):1268-78. doi: 10.1016/j.intimp.2010.07.009. Epub 2010 Jul 30.
The goal of this study was to determine whether extracts and isolated alkylamides from Echinacea purpurea would be useful for prevention of the inflammatory response that accompanies infections with H1N1 influenza A. Seventeen extracts and 4 alkylamides were tested for the ability to inhibit production of cytokines, chemokines, and PGE₂ from RAW 264.7 macrophage-like cells infected with the H1N1 influenza A strain PR/8/34. The alkylamides undeca-2Z,4E-diene-8,10-diynic acid isobutylamide, dodeca-2E,4E,8Z,10E/Z-tetraenoic acid isobutylamide, dodeca-2E,4E-dienoic acid isobutylamide, and undeca-2E-ene-8,10-diynoic acid isobutylamide suppressed production of TNF-α and PGE₂ from infected cells. Dodeca-2E,4E-dienoic acid isobutylamide was especially effective at inhibiting production of these mediators and also strongly inhibited production of G-CSF, CCL2/MCP-1, CCL3/MIP-1α and CCL5/RANTES. In contrast, the ethanol extracts (75%), which were prepared from dormant roots of E. purpurea grown in different locations throughout North Carolina, displayed a range of effects from suppression to stimulation of mediator production. Precipitation of the extracts with ethanol removed the stimulatory activity, however, even after precipitation; many of the extracts did not display any suppressive activity. Analysis of the extracts revealed slight variations in concentration of alkylamides, caftaric acid, and cichoric acid, but the activity of the extracts did not strongly correlate with concentrations of these compounds. Our in vitro experiments suggest that E. purpurea extracts have the potential for use in alleviating the symptoms and pathology associated with infections with influenza A; however, further study will be necessary to define procedures necessary to unmask the alkylamide activity in crude extracts.
本研究旨在确定来自紫锥菊的提取物和分离的烷酰胺是否可用于预防甲型 H1N1 流感感染伴随的炎症反应。我们测试了 17 种提取物和 4 种烷酰胺抑制 RAW 264.7 巨噬细胞样细胞感染甲型 H1N1 流感 PR/8/34 株后细胞因子、趋化因子和 PGE₂产生的能力。烷酰胺十一碳-2Z,4E-二烯-8,10-二炔酸异丁酰胺、十二碳-2E,4E,8Z,10E/Z-四烯酸异丁酰胺、十二碳-2E,4E-二烯酸异丁酰胺和十一碳-2E-烯-8,10-二炔酸异丁酰胺抑制感染细胞 TNF-α和 PGE₂的产生。十二碳-2E,4E-二烯酸异丁酰胺尤其能有效地抑制这些介质的产生，也能强烈抑制 G-CSF、CCL2/MCP-1、CCL3/MIP-1α 和 CCL5/RANTES 的产生。相比之下，从北卡罗来纳州不同地区生长的休眠紫锥菊根部制备的 75%乙醇提取物显示出从抑制到刺激介质产生的一系列作用。然而，用乙醇沉淀提取物去除了刺激活性，即使在沉淀后，许多提取物也没有显示任何抑制活性。对提取物的分析表明烷酰胺、咖啡酸和菊苣酸的浓度略有差异，但提取物的活性与这些化合物的浓度没有很强的相关性。我们的体外实验表明，紫锥菊提取物有可能用于缓解甲型流感感染引起的症状和病理学；然而，需要进一步研究以确定揭示粗提取物中烷酰胺活性所需的程序。
