中国药房2026，Vol.37Issue(17)：2241-2247,7.DOI:10.6039/j.issn.1001-0408.2026.17.05
广金钱草提取物抗胆汁淤积性肝损伤的活性成分筛选及其作用机制研究
Study on screening of active components from Desmodium styracifolium(Osb.)Merr.extract against cholestatic liver injury and its mechanism of action
摘要
Abstract
OBJECTIVE To identify the active components of Desmodium styracifolium(Osb.)Merr.extract(DME)against cholestatic liver injury(CLI),and to verify its target and molecular mechanism,so as to provide scientific evidence for the clinical application of D.styracifolium(Osb.)Merr.and the development of new hepatoprotective agents.METHODS High-performance liquid chromatography was applied to establish fingerprints of 19 batches of DME,followed by similarity evaluation and identification of common peaks.An in vitro CLI model was constructed by lithocholic acid(LCA)-induced injury in HepG2 cells to evaluate the in vitro protective effect of DME against CLI.Spearman correlation analysis,grey relational analysis and partial least-squares regression analysis were adopted to investigate the spectrum-effect relationship of DME against CLI and preliminarily screen the core active components.Molecular docking and surface plasmon resonance technology were used to predict and verify the binding capacity between core active components and farnesoid X receptor(FXR).qRT-PCR,Western blot and immunofluorescence staining tests were performed to validate the influences of core active components on the expression of molecules related to FXR/bile salt export pump(BSEP)pathway in CLI model cells.RESULTS A total of 12 common peaks were calibrated in the fingerprints of 19 batches of DME,and the similarity values were all above 0.990.Four common peaks were identified,namely peak 6(schaftoside),peak 7(isoorientin),peak 11(isoschaftoside)and peak 12(isovitexin).DME at 80μg/mL exerted the optimal protective effect on CLI-model cells,and the cell viability reached(75.66±4.60)%after 24 h of treatment.Spectrum-effect analysis revealed that schaftoside possessed the strongest correlation with the anti-CLI activity of DME and served as the core active component.Target prediction and validation results showed that the binding energy between schaftoside and FXR was-8.1 kcal/mol,and the equilibrium dissociation constant was 27.3 μmol/L.Mechanistic experiments demonstrated that 100 μmol/L schaftoside significantly elevated the expression levels of FXR and BSEP,and mRNA of their encoded genes Nr1h4,Abcb11 in CLI-model cells(P＜0.05).CONCLUSIONS Schaftoside may be the core active component of DME against CLI,and its mechanism may be related to the activation of FXR/BSEP pathway.关键词
广金钱草提取物/胆汁淤积性肝损伤/谱效关系/夏佛塔苷/FXR/BSEP通路/活性成分Key words
Desmodium styracifolium(Osb.)Merr.extract/cholestatic liver injury/spectrum-effect relationship/schaftoside/FXR/BSEP pathway/active components分类
医药卫生引用本文复制引用
黄涛,陈超,韦文华,韦柳婷,李波,高雅,曹后康..广金钱草提取物抗胆汁淤积性肝损伤的活性成分筛选及其作用机制研究[J].中国药房,2026,37(17):2241-2247,7.基金项目
国家自然科学基金青年科学基金项目(No.82505187) （No.82505187）
广西壮族自治区第一批青苗人才普惠性支持政策项目(No.桂人社函[2024]161号) （No.桂人社函[2024]161号）
八桂青年拔尖人才项目(No.桂科发[2025]420号) （No.桂科发[2025]420号）
