首页|仙鹤草干预溃疡性结肠炎的有效活性成分分析及体外作用靶点研究

仙鹤草干预溃疡性结肠炎的有效活性成分分析及体外作用靶点研究

扫码查看
目的 体外水平初步探究仙鹤草有效活性成分治疗溃疡性结肠炎(ulcerative colitis,UC)的作用机制.方法 通过数据库筛选仙鹤草的有效活性成分并获得仙鹤草-UC交集靶点,对其靶点进行KEGG和GO通路富集分析,通过分子对接筛选出结合紧密的靶标蛋白.体外构建RAW264.7和Caco-2细胞模型,验证筛选出来的有效活性成分对炎症因子、巨噬细胞极化和肠紧密连接蛋白表达的影响.结果 仙鹤草主要活性成分为:木犀草素、山柰酚、槲皮素、儿茶素、鞣花酸,以上成分能明显调控巨噬细胞极化和炎症因子IL-1β、IL-6、TNF-α、iNOS、CD86的表达,但是对肠紧密连接蛋白水平没有明显改善.其重要靶标基因为:MMP3、MMP2、BCL2L1、CD40、FOS,主要富集在NF-KB、PI3K-Akt、MAPK、HIF-1、TGF-β等信号通路上.结论 仙鹤草有效成分能降低炎症水平,调节巨噬细胞极化,其机制可能是通过调控MMP3、MMP2、BCL2L1、CD40、FOS等基因从而调控NF-KB、PI3K-Akt、MAPK、HIF-1、TGF-β等信号通路达到治疗UC的作用.
Analysis of Effective Active Ingredients and in vitro Study of the Targets of Action of Agrimoniae Herba in Intervening Ulcerative Colitis
Objective To investigate the mechanism of action of effective active components of Agrimoniae Herba in the treatment of ulcerative colitis(UC)in vitro.Methods We screened the effective active ingredients of Agrimoniae Herba and obtained the Agrimoniae Herba-UC intersecting targets through the database,analyzed the KEGG and GO pathway enrichment of the targets,and screened the tightly bound target proteins through molecular docking.In vitro RAW264.7 and Caco-2 cell models were constructed to verify the effects of the screened active ingredients on inflammatory factors,macrophage polarization and intestinal tight junction protein expression.Results The main active ingredients of Agrimoniae Herba were lignans,kaempferol,quercetin,catechin,and ellagic acid,which significantly regulated macrophage polarization and the expression of inflammatory factors IL-1β,IL-6,TNF-α,iNOS,and CD86,but did not significantly improve intestinal tight junction proteins.The important target genes were MMP3,MMP2,BCL2L1,CD40,and FOS,which were mainly enriched in the signaling pathways such as NF-κB,PI3K-Akt,MAPK,HIF-1,TGF-β,and so on.Conclusion The active ingredients of Agrimoniae Herba can reduce the inflammation level and regulate macrophage polarization,and the mechanism may be through the regulation of MMP3,MMP2,BCL2L1,CD40,FOS,and other genes,thereby regulating the signaling pathways such as NF-κB,PI3K-Akt,MAPK,HIF-1,TGF-β,and so on,to achieve the effect of treatment of UC.

Agrimoniae Herbaulcerative colitisnetwork pharmacologyinflammationmacrophage polarization

王月、王斯、胡雨、段为钢、陈欢

展开 >

云南中医药大学基础医学院,云南省中西医结合慢病防治重点实验室,云南昆明 650500

仙鹤草 溃疡性结肠炎 网络药理学 炎症 巨噬细胞极化

云南省科技厅科技计划项目基础研究专项云南省科技厅科技计划项目基础研究专项云南省"兴滇英才支持计划"项目

202301AT070252202001AU070107

2024

云南中医学院学报
云南中医学院

云南中医学院学报

影响因子:0.933
ISSN:1000-2723
年,卷(期):2024.47(2)
  • 28