Study on screening of active components from Desmodium styracifolium（ Osb.） Merr. extract against cholestatic liver injury and its mechanism of action
- VernacularTitle: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
- Author:
Tao HUANG
1
;
Chao CHEN
1
;
Wenhua WEI
1
;
Liuting WEI
1
;
Bo LI
1
;
Ya GAO
1
;
Houkang CAO
2
Author Information
1. Key Laboratory of Pharmacology for Prevention and Treatment of High-incidence Diseases of Guangxi Higher Education Institutions，Guangxi Guilin 541199，China;Institute of Materia Medica，Guilin Medical University，Guangxi Guilin 541199，China
2. Key Laboratory of Pharmacology for Prevention and Treatment of High-incidence Diseases of Guangxi Higher Education Institutions，Guangxi Guilin 541199，China
- Publication Type:Journal Article
- Keywords:
cholestatic liver injury;
spectrum-effect relationship;
schaftoside;
FXR/BSEP pathway;
active components
- From:
China Pharmacy
2026;37(17):2241-2247
- CountryChina
- Language:Chinese
-
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 80 μg/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.
