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石楠属植物和 YM 通过调节炎症介质和直接控制钠离子通道的镇痛活性。

The analgesic activities of Stauntonia brachyanthera and YM through regulating inflammatory mediators and directly controlling the sodium channel prompt.

机构信息

Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University), Ministry of Education; School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Wenhua Road 103, Shenyang, 110016, PR China.

School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, Wenhua Road 103, Shenyang, 110016, PR China.

出版信息

Sci Rep. 2017 Aug 8;7(1):7574. doi: 10.1038/s41598-017-07095-x.

DOI:10.1038/s41598-017-07095-x
PMID:28790377
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5548894/
Abstract

The analgesic studies on Stauntonia brachyanthera, a traditional Chinese folk medicine used to treat headache, pains and inflammatory diseases in local areas, showed that the EtOH extracts (EESB) and the characteristic ingredient YM could significantly inhibit the acetic acid-induced writhing responses by 43.1% and 78.95%, and decrease the xylene-induced ear edemas by 48.9% and 21.4%, respectively. EESB could significantly increase pain threshold of mice in hot-plate test, but the effect of YM was not obviously. Further study in formalin test showed the inhibitory effect of YM in 2 phase was more significant than that in 1 phase, revealed the peripheral analgesic activity of YM. The ELISA and Western Blot analysis suggested that the analgesic mechanisms of YM were related to the inhibitions of the expressions of TNF-α, IL-1β and IL-6, and down-regulations of Na1.8 protein in the left side of L4-6 DRG regulated by MAPKs, in which the levels of p-ERK, p-JNK and p-p38 were all decreased. In addition, the electrophysiological experiments indicated YM could reduce the Nav1.8 currents by 46.01% in small-diameter DRG neurons. Therefore, the analgesic activity of S. brachyanthera might be based on the regulation of inflammatory mediators and the directly control of the sodium channel prompt.

摘要

用于治疗头痛、疼痛和炎症的传统中药华千金藤的镇痛研究表明，其乙醇提取物（EESB）和特征成分 YM 可分别显著抑制醋酸诱导的扭体反应 43.1%和 78.95%，并减少二甲苯诱导的耳肿胀 48.9%和 21.4%。EESB 可显著提高热板试验中小鼠的疼痛阈值，但 YM 的作用不明显。在福马林试验中的进一步研究表明，YM 在 2 相的抑制作用比 1 相更显著，揭示了 YM 的外周镇痛活性。ELISA 和 Western Blot 分析表明，YM 的镇痛机制与抑制 TNF-α、IL-1β 和 IL-6 的表达以及 MAPKs 调节的 L4-6DRG 左侧 Na1.8 蛋白的下调有关，其中 p-ERK、p-JNK 和 p-p38 的水平均降低。此外，电生理实验表明 YM 可使小直径 DRG 神经元中的 Nav1.8 电流减少 46.01%。因此，华千金藤的镇痛活性可能基于炎症介质的调节和钠离子通道的直接控制。

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