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基于超高效液相色谱-轨道阱质谱联用、网络药理学及细胞实验验证的芍药甘草汤治疗类风湿关节炎的作用机制研究

[Mechanisms of Shaoyao Gancao Decoction in treatment of rheumatoid arthritis based on UPLC-Orbitrap-MS~2, network pharmacology, and cellular experiment verification].

作者信息

Zhu Meng, Guo Hui, Dai Li-Ping, Wang Zhi-Min

机构信息

Henan Collaborative Innovation Center for Research and Development on the Whole Industry Chain of Yu-Yao, Henan University of Chinese Medicine Zhengzhou 450046, China Henan University of Chinese Medicine Zhengzhou 450046, China.

Henan University of Chinese Medicine Zhengzhou 450046, China National Engineering Laboratory for Quality Control Technology of Chinese Herbal Medicines, Institute of Chinese Materia Medica,China Academy of Chinese Medical Sciences Beijing 100700, China.

出版信息

Zhongguo Zhong Yao Za Zhi. 2024 Nov;49(22):6149-6164. doi: 10.19540/j.cnki.cjcmm.20240731.301.

Abstract

Shaoyao Gancao Decoction(SGD) is a classic formula used in the clinical treatment of joint diseases, such as rheumatoid arthritis(RA), though its mechanism of action remains unclear. This study aimed to explore the mechanism of SGD in treating RA through chemical and network pharmacology analyses, combined with cellular experiments. UPLC-Orbitrap-MS~2 was used to qualitatively analyze SGD and drug-containing serum of rats after oral administration of SGD, thereby identifying the chemical composition and plasma components of SGD. Potential targets for the plasma components in treating RA were identified using the SwissTargetPrediction, PharmMapper, GeneCards, and DrugBank databases, and a protein-protein interaction(PPI) network was constructed using the STRING data platform. GO functional enrichment and KEGG pathway enrichment analyses were conducted using the Metascape database. Molecular docking and lipopolysaccharide(LPS)-induced RAW264.7 cell experiments were utilized for in vitro validation. The results identified 95 compounds in SGD, including 15 prototypical absorbed components, i.e., 7 flavonoids, 5 terpenoids, 2 phenolic compounds, and 1 other compound. Network pharmacology analysis revealed that licoisoflavanone, liquiritin apioside, 5-hydroxyferulic acid, albiflorin, hederagenin, and paeoniflorin were the pharmacodynamic components of SGD for treating RA. The core targets of SGD for RA treatment were identified as SRC, MAPK, EGFR, HSP90AA1, and STAT3, with regulation of the NF-κB, PI3K-Akt, and MAPK signaling pathways identified as key mechanisms for anti-RA effects of SGD. Molecular docking results showed that the six core components exhibited high affinity with the key targets SRC, MAPK, and NF-κB. In vitro cellular experiments demonstrated that SGD down-regulated the expression of inflammatory factors, including interleukin-1β(IL-1β), cyclooxygenase-2(COX-2), and tumor necrosis factor-α(TNF-α), in LPS-induced RAW264.7 cells. Western blot analysis revealed that SGD significantly reduced the phosphorylation levels of NF-κB p65 and p38 MAPK proteins. This study provides a scientific basis for further research into the active components and mechanisms of action of SGD in treating RA.

摘要

芍药甘草汤(SGD)是临床用于治疗类风湿关节炎(RA)等关节疾病的经典方剂,但其作用机制尚不清楚。本研究旨在通过化学和网络药理学分析,并结合细胞实验,探讨芍药甘草汤治疗类风湿关节炎的作用机制。采用超高效液相色谱-轨道阱质谱联用技术(UPLC-Orbitrap-MS²)对芍药甘草汤及芍药甘草汤灌胃大鼠后的含药血清进行定性分析,从而确定芍药甘草汤的化学成分和血浆成分。利用SwissTargetPrediction、PharmMapper、GeneCards和DrugBank数据库确定血浆成分治疗类风湿关节炎的潜在靶点,并使用STRING数据平台构建蛋白质-蛋白质相互作用(PPI)网络。利用Metascape数据库进行基因本体(GO)功能富集分析和京都基因与基因组百科全书(KEGG)通路富集分析。通过分子对接和脂多糖(LPS)诱导的RAW264.7细胞实验进行体外验证。结果在芍药甘草汤中鉴定出95种化合物,其中包括15种原型吸收成分,即7种黄酮类化合物、5种萜类化合物、2种酚类化合物和1种其他化合物。网络药理学分析表明,甘草异黄酮、甘草苷芹菜糖苷、5-羟基阿魏酸、芍药苷、常春藤皂苷元、芍药内酯苷是芍药甘草汤治疗类风湿关节炎的药效成分。确定芍药甘草汤治疗类风湿关节炎的核心靶点为Src、丝裂原活化蛋白激酶(MAPK)、表皮生长因子受体(EGFR)、热休克蛋白90α(HSP90AA1)和信号转导和转录激活因子3(STAT3),并确定调节核因子κB(NF-κB)、磷脂酰肌醇3激酶-蛋白激酶B(PI3K-Akt)和MAPK信号通路是芍药甘草汤抗类风湿关节炎作用的关键机制。分子对接结果表明,六种核心成分与关键靶点Src、MAPK和NF-κB具有高亲和力。体外细胞实验表明,芍药甘草汤下调LPS诱导的RAW264.7细胞中炎症因子白细胞介素-1β(IL-1β)、环氧化酶-2(COX-2)和肿瘤坏死因子-α(TNF-α)的表达。蛋白质免疫印迹分析显示,芍药甘草汤显著降低NF-κB p65和p38 MAPK蛋白的磷酸化水平。本研究为进一步研究芍药甘草汤治疗类风湿关节炎的活性成分和作用机制提供了科学依据。

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