The exploration of active components of 701 Dieda Zhentong patch and analgesic properties on chronic constriction injury rats.

IF 3 4区医学 Q2 NEUROSCIENCES Purinergic Signalling Pub Date : 2024-11-04 DOI:10.1007/s11302-024-10056-5

Jun Meng, Zhenglang Zhang, Yujie Wang, Lina Long, Anqi Luo, Zhenhui Luo, Kexin Cai, Xi Chen, Hong Nie

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Abstract

An increasing number of traditional Chinese medicine(TCM) have been confirmed to possess analgesic bioactivity. 701 Dieda Zhentong patch(701-DZP) which includes 14 kinds of TCMs exhibited excellent efficacy in alleviating back or leg pain after a soft-tissue injury. In this study, UPLC/MS was used to construct the fingerprint of 701-DZP and excavate the potential bioactive ingredients of it. 21 compounds were detected and identified in the fingerprint including 12 compounds that pass through the skin and 6 compounds observed in the plasma. Then, the role of 701-DZP in neuropathic pain(NPP) was assessed by network pharmacology and CCI rats. 701-DZP inhibited pain sensitization(MWT and TWL) and the release of inflammation mediators(IL-1β and IL-6) in CCI rats which were in keeping with the core targets of the PPI network. The results of IHC and Western blot showed that the expression of the P2X3 receptor in the DRG and SC of CCI rats was significantly reduced after the treatment with 701-DZP. Moreover, the 701-DZP down-regulated the level of phosphorylation of ERK1/2 MAPK instead of P38 MAPK in the DRG of CCI rats. In conclusion, this study has clarified 6 potential analgesic active compounds of 701-DZP and explored the analgesic properties, which may inhibit the expression of the P2X3 receptor to reduce the release of inflammatory mediators based on the ERK1/2 MAPK pathway to alleviate the NPP.

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701地达镇痛贴有效成分及对慢性收缩性损伤大鼠镇痛作用的探讨

越来越多的传统中药被证实具有镇痛生物活性。由 14 种中药组成的 701 Dieda Zhentong 贴片（701-DZP）在缓解软组织损伤后的腰腿痛方面表现出卓越的疗效。本研究采用UPLC/MS构建了701-DZP的指纹图谱，并挖掘了其中潜在的生物活性成分。在指纹图谱中检测并确定了 21 种化合物，包括 12 种通过皮肤的化合物和 6 种在血浆中观察到的化合物。然后，通过网络药理学和 CCI 大鼠评估了 701-DZP 在神经病理性疼痛（NPP）中的作用。701-DZP抑制了CCI大鼠的痛敏化（MWT和TWL）和炎症介质（IL-1β和IL-6）的释放，这与PPI网络的核心目标一致。IHC和Western blot结果显示，701-DZP治疗后，CCI大鼠DRG和SC中P2X3受体的表达明显减少。此外，701-DZP还能下调CCI大鼠DRG中ERK1/2 MAPK而非P38 MAPK的磷酸化水平。总之，本研究阐明了 701-DZP 的 6 种潜在镇痛活性化合物，并探讨了其镇痛特性，这些化合物可能会抑制 P2X3 受体的表达，从而减少基于 ERK1/2 MAPK 通路的炎症介质的释放，从而缓解 NPP。

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来源期刊

Purinergic Signalling 医学-神经科学

CiteScore

6.60

自引率

17.10%

发文量

审稿时长

6-12 weeks

期刊介绍： Nucleotides and nucleosides are primitive biological molecules that were utilized early in evolution both as intracellular energy sources and as extracellular signalling molecules. ATP was first identified as a neurotransmitter and later as a co-transmitter with all the established neurotransmitters in both peripheral and central nervous systems. Four subtypes of P1 (adenosine) receptors, 7 subtypes of P2X ion channel receptors and 8 subtypes of P2Y G protein-coupled receptors have currently been identified. Since P2 receptors were first cloned in the early 1990’s, there is clear evidence for the widespread distribution of both P1 and P2 receptor subtypes in neuronal and non-neuronal cells, including glial, immune, bone, muscle, endothelial, epithelial and endocrine cells.