白花蛇舌草抗炎机制的网络药理学分析及实验研究  

Anti-inflammatory Mechanism of Hedyotis diffusa:A Study Based on Network Pharmacology and Experiment Verification

作　　者：李曼[1] 张露蓉[1,2] 金顺琪 侯文跃 梁国强 LI Man;ZHANG Lurong;JIN Shunqi;HOU Wenyue;LIANG Guoqiang(Central Laboratory,Suzhou Hospital of Traditional Chinese Medicine Affiliated to Nanjing University of Chinese Medicine,Suzhou 215000,China;Department of Research and Development of Chinese Medicine,Suzhou Academy of Wumen Chinese Medicine,Suzhou 215000,China)

机构地区：[1]南京中医药大学附属苏州市中医医院中心实验室,苏州215000 [2]苏州市吴门医派研究院中药研究与开发部,苏州215000

出　　处：《世界中医药》2022年第18期2535-2540,共6页World Chinese Medicine

基　　金：2019年度江苏省第五期“333工程”科研资助项目(BRA2019141)。

摘　　要：目的:基于网络药理学分析及实验研究验证探究白花蛇舌草潜在的抗炎靶点。方法:通过中药系统药理学数据库与分析平台(TCMSP)筛选符合条件的活性成分及相关作用靶点,并取得成分靶点和抗炎靶点的交集,构建靶点间的PPI网络图,Metascape平台对关键靶点进行基因本体(GO)富集分析和京都基因和基因组百科全书(KEGG)通路富集分析,AutoDock软件对关键成分及靶点进行分子对接。通过小鼠耳缘肿胀和扭体实验模型,进行药效学观察,酶联免疫吸附试验法检测网络药理学涉及部分关键靶点。结果:共筛得相关活性成分6个,匹配到相关靶点信息173个,获得成分和疾病交集靶点99个,潜在治疗靶点有AKT1、IL-6、TNF、VEGFA、PTGS2等,主要参与TNF信号通路发挥抗炎作用。分子对接结果显示,β-谷甾醇,Poriferasterol、2-methoxy-3-methyl-9,10-anthraquinone、豆甾醇与靶点结合性较强。动物实验验证了白花蛇舌草干预后可减轻小鼠耳肿胀度和减少扭体次数,降低血清中肿瘤坏死因子-α、白细胞介素-6因子水平。结论:白花蛇舌草具有抗炎效应,主要与抑制肿瘤坏死因子-α、白细胞介素-6等因子有关,网络药理学结果还显示白花蛇舌草中β-谷甾醇、Poriferasterol、2-methoxy-3-methyl-9,10-anthraquinone和豆甾醇等成分可能通过AKT1、IL-6、TNF、VEGFA等关键靶点作用于TNF信号通路发挥抗炎作用。Objective:To explore the potential anti-inflammatory targets of Hedyotis diffusa based on network pharmacology and experiment verification.Methods:The active components and the corresponding targets of the herb were searched against the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform(TCMSP).The common targets shared by the active components and inflammation were identified and the protein-protein interaction(PPI)network between targets was constructed.Metascape was employed to perform gene ontology(GO)annotation and Kyoto Encyclopedia of Genes and Genomes(KEGG)pathway enrichment for the key targets.AutoDock was employed to simulate the docking between key components and targets.Pharmacodynamics observation was carried out with mouse models of ear edema and writhing.Enzyme-linked immunosorbent assay(ELISA)was employed to determine the expression of some key targets predicted based on network pharmacology.Results:A total of 6 active components were screened out,which corresponded to 173 targets,and 99 targets shared by the active components and inflammation were identified.The potential therapeutic targets included AKT serine/threonine kinase 1(AKT1),interleukin-6(IL-6),tumor necrosis factor(TNF),vascular endothelial growth factor A(VEGFA),and prostaglandin-endoperoxide synthase 2(PTGS2),which mainly participated in the TNF signaling pathway to play an anti-inflammatory role.The molecular docking results showed thatβ-sitosterol,poriferasterol,2-methoxy-3-methyl-9,10-anthraquinone,and stigmasterol had strong binding ability with the targets.The animal experiments verified that H.diffusa alleviated the ear edema and the number of writhing and lowered the levels of TNF-αand IL-6 in the serum of mice.Conclusion:H.diffusa mainly exerts the anti-inflammatory effect by inhibiting the expression of TNF-α,IL-6 and other cytokines.The results of network pharmacology indicate thatβ-sitosterol,poriferasterol,2-methoxy-3-methyl-9,10-anthraquinone,and stigmasterol in H.diffusa may regulate th

关 键 词：白花蛇舌草 抗炎 网络药理学 靶点 作用机制 分子对接 动物实验 

分 类 号：R285[医药卫生—中药学]