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系统药理学和体外研究鉴定牛膝中活性化合物治疗骨关节炎的作用。

A Systematic Pharmacology and In Vitro Study to Identify the Role of the Active Compounds of Achyranthes bidentata in the Treatment of Osteoarthritis.

机构信息

Academy of Integrative Medicine, Fujian University of Traditional Chinese Medicine, Fuzhou, Fujian, China (mainland).

Department of Clinical Medicine, Fujian Health College, Fuzhou, Fujian, China (mainland).

出版信息

Med Sci Monit. 2020 Sep 14;26:e925545. doi: 10.12659/MSM.925545.

DOI:10.12659/MSM.925545
PMID:32925869
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7513678/
Abstract

BACKGROUND Achyranthes bidentata is a Chinese traditional herbal medicine widely used to treat osteoarthritis (OA). This study aimed to identify active compounds from Achyranthes bidentata through systematic pharmacology and in vitro experiments to find the targets of Achyranthes bidentata in the treatment of OA. MATERIAL AND METHODS We screened the active compounds of Achyranthes bidentata from the Traditional Chinese Medicine Systems Pharmacology (TCMSP) database. Then, we used STITCH and Open Targets Platform databases to screen the active components and predict the potential targets of Achyranthes bidentata in the treatment of OA. Subsequently, we studied the compound-target network and protein interaction network and analyzed the enrichment of potential target proteins. Finally, we used Western blot analysis to verify the therapeutic effect of Achyranthes bidentata extract on the expression of OA-related target proteins. RESULTS There were 7 active components in Achyranthes bidentata, which were strongly related to the 74 targets of OA. Quercetin, baicalein, and berberine are the critical active compounds of Achyranthes bidentata in the treatment of OA. Protein interaction analysis and in vitro experiments suggested that TNF, IL-6, and TP53 are the critical targets of Achyranthes bidentata in the treatment of OA. Functional enrichment analysis showed that Achyranthes bidentata plays a pharmacological role in OA through apoptosis, inflammation, and immune regulation. CONCLUSIONS Quercetin, baicalein, and berberine are the critical active compounds of Achyranthes bidentata in the treatment of OA. TNF, IL-6, and TP53 may be potential targets for the treatment of OA.

摘要

背景

牛膝是一种广泛用于治疗骨关节炎(OA)的中药。本研究旨在通过系统药理学和体外实验从牛膝中鉴定出活性化合物,以找到牛膝治疗 OA 的作用靶点。

材料和方法

我们从中药系统药理学(TCMSP)数据库中筛选牛膝的活性化合物。然后,我们使用 STITCH 和 Open Targets Platform 数据库筛选牛膝治疗 OA 的活性成分和预测潜在靶点。随后,我们研究了化合物-靶点网络和蛋白质相互作用网络,并分析了潜在靶点蛋白的富集情况。最后,我们使用 Western blot 分析验证牛膝提取物对 OA 相关靶蛋白表达的治疗作用。

结果

牛膝中有 7 种活性成分,与 OA 的 74 个靶点密切相关。槲皮素、黄芩素和小檗碱是牛膝治疗 OA 的关键活性化合物。蛋白质相互作用分析和体外实验表明,TNF、IL-6 和 TP53 是牛膝治疗 OA 的关键靶点。功能富集分析表明,牛膝通过细胞凋亡、炎症和免疫调节发挥治疗 OA 的药理作用。

结论

槲皮素、黄芩素和小檗碱是牛膝治疗 OA 的关键活性化合物。TNF、IL-6 和 TP53 可能是治疗 OA 的潜在靶点。

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PIM1, CYP1B1, and HSPA2 Targeted by Quercetin Play Important Roles in Osteoarthritis Treatment by .
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Mechanistic prospective and pharmacological attributes of quercetin in attenuation of different types of arthritis.槲皮素在减轻不同类型关节炎中的作用机制、前瞻性研究及药理学特性
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Osteoarthritis related epigenetic variations in miRNA expression and DNA methylation.骨关节炎相关的 miRNA 表达和 DNA 甲基化的表观遗传变化。
BMC Med Genomics. 2023 Jul 11;16(1):163. doi: 10.1186/s12920-023-01597-6.
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