Synergistic immunomopharmacological effects of N-alkylamides in Echinacea purpurea herbal extracts
Synergistic immunomopharmacological effects of N-alkylamides in Echinacea purpurea herbal extracts
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DOI：
10.1016/j.intimp.2009.03.006
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发表时间：
2009-07-01
影响因子：
5.6
通讯作者：
Gertsch, Juerg
中科院分区：
文献类型：
--
作者：
Chicca, Andrea;Raduner, Stefan;Gertsch, Juerg
紫锥菊提取物用于生产用于预防和治疗上呼吸道感染的标准化草药。不饱和 N-烷基酰胺脂质是能够激活 2 型大麻素受体 (CB2) 的 E. purpurea 和 E. angustifolia 制剂的主要成分，已被认为具有潜在的抗炎和免疫调节原理的作用。在这里，我们表明乙醇乙醇 E. purpurea radix 和草药提取物在体外对内源性大麻素系统产生协同药理作用。在细胞内钙释放水平上观察到 N-烷基酰胺组合的超加和作用作为 CB2 受体激活的函数。同样，在测量 LPS 刺激的人 PBMC 细胞因子表达的实验中观察到了根和草药酊剂的协同作用。虽然抗炎细胞因子 IL-10 的表达被显着过度刺激，但促炎性 TNF-α 蛋白的表达在提取物组合后受到更强烈的抑制。我们发现，N-烷基酰胺通过同时靶向 CB2 受体、内源性大麻素转运和降解，协同作用并发挥多效性调节内源性大麻素系统。 (C) 2009 Elsevier B.V. 保留所有权利。
Echinacea purpurea extracts are used in the production of standardized herbal medicines for the prevention and treatment of upper respiratory infections. Unsaturated N-alkylamide lipids, the main constituent of E purpurea and E angustifolia preparations capable of activating the cannabinoid receptor type-2 (CB2) have been suggested to play a role as potential anti-inflammatory and immune-modulatory principles.Here we show that ethanolic E. purpurea radix and herba extracts produce synergistic pharmacological effects on the endocannabinoid system in vitro. Superadditive action of N-alkylamide combinations was seen at the level of intracellular calcium release as a function of CB2 receptor activation. Likewise, synergism of the radix and herba tinctures was observed in experiments measuring LPS-stimulated cytokine expression from human PBMCs. While the expression of the anti-inflammatory cytokine IL-10 was significantly super-stimulated, the expression of the pro-inflammatory TNF-alpha protein was inhibited more strongly upon combination of the extracts. We show that N-alkylamides act in concert and exert pleiotropic effects modulating the endocannabinoid system by simultaneously targeting the CB2 receptor, endocannabinoid transport and degradation. (C) 2009 Elsevier B.V. All rights reserved.