Department of Pharmacy, Affiliated Hospital of Inner Mongolia Medical University, Hohhot, 010059, Inner Mongolia, People's Republic of China.
Department of Pathology, Affiliated Hospital of Inner Mongolia Medical University, Hohhot, 010059, Inner Mongolia, People's Republic of China.
Mol Divers. 2021 Feb;25(1):233-248. doi: 10.1007/s11030-020-10055-9. Epub 2020 Mar 4.
Piperine is the main active component of Piper longum L., which is also the main component of anti-sciatica Mongolian medicine Naru Sanwei pill. It has many pharmacological activities such as anti-inflammatory and immune regulation. This paper aims to preliminarily explore the potential mechanism of piperine in the treatment of sciatica through network pharmacology and molecular docking. TCMSP, ETCM database and literature mining were used to collect the active compounds of Piper longum L. Swiss TargetPrediction and SuperPred server were used to find the targets of compounds. At the same time, CTD database was used to collect the targets of sciatica. Then the above targets were compared and analyzed to select the targets of anti-sciatica in Piper longum L. The Go (gene ontology) annotation and KEGG pathway of the targets were enriched and analyzed by Metascape database platform. The molecular docking between the effective components and the targets was verified by Autodock. After that, the sciatica model of rats was established and treated with piperine. The expression level of inflammatory factors and proteins in the serum and tissues of rat sciatic nerve were detected by ELISA and Western blot. HE staining and immunohistochemistry were carried out on the sciatica tissues of rats. The results showed that Piper longum L. can regulate the development of sciatica and affect the expressions of PPARG and NF-kB1 through its active ingredient piperine, and there is endogenous interaction between PPARG and NF-kB1.
胡椒碱是胡椒（Piper longum L.）的主要活性成分，也是蒙药那如三味丸治疗坐骨神经痛的主要成分，具有抗炎、免疫调节等多种药理活性。本研究旨在采用网络药理学和分子对接的方法初步探讨胡椒碱治疗坐骨神经痛的潜在作用机制。通过 TCMSP、ETCM 数据库和文献挖掘收集胡椒的活性成分，利用 Swiss TargetPrediction 和 SuperPred 服务器寻找化合物的作用靶点，同时利用 CTD 数据库收集坐骨神经痛的作用靶点，将上述靶点进行对比分析，筛选出胡椒治疗坐骨神经痛的作用靶点。利用 Metascape 数据库平台对靶点进行 GO 注释和 KEGG 通路富集分析。采用 Autodock 软件对有效成分与靶点进行分子对接验证。然后建立大鼠坐骨神经痛模型，用胡椒碱进行治疗，通过 ELISA 和 Western blot 检测大鼠血清和坐骨神经组织中炎症因子和蛋白的表达水平，对大鼠坐骨神经痛组织进行 HE 染色和免疫组化。结果表明，胡椒通过其活性成分胡椒碱调节坐骨神经痛的发生发展，影响 PPARG 和 NF-kB1 的表达，且 PPARG 和 NF-kB1 之间存在内源性相互作用。
