Network-guided Evaluation of β-sitosterol in Inflammatory and Profibrotic Mesangial-Cell Models Relevant to Chronic Glomerulonephritis

Chronic glomerulonephritis (CGN) is characterized by persistent inflammatory injury and progressive fibrotic remodeling, yet compound-target relationships underlying natural-product-based interventions remain incompletely defined. This study integrated network pharmacology, validated molecular docking, and in vitro experiments to evaluate candidate constituents of Cordyceps sinensis (C. sinensis) in CGN-related pathological processes. Candidate constituents of C. sinensis were screened, and the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform-derived compound-associated targets were intersected with CGN-associated genes. Functional enrichment and protein-protein interaction analyses were used to prioritize biological processes and hub targets. PTGS2 was identified as a key overlapping target. Molecular docking was performed using a celecoxib-bound COX-2 structure. Re-docking of the co-crystallized celecoxib ligand reproduced the crystallographic pose with an RMSD of 0.876 Å, supporting the docking protocol. β-Sitosterol and linoleyl acetate showed predicted compatibility with the COX-2 docking region, with binding affinities of -7.2 and -7.5 kcal/mol, respectively. β-Sitosterol was selected for compound-level validation in HBZY-1 rat glomerular mesangial cells. At 0.5-10 µM, β-sitosterol did not markedly reduce cell viability. In Lipopolysaccharide (LPS)-stimulated cells, β-sitosterol reduced Tnf, Il6, and Ptgs2 expression, decreased prostaglandin E2 (PGE2) production, and reduced cyclooxygenase-2 (COX-2) protein abundance. In transforming growth factor β1 (TGF-β1)-treated cells, β-sitosterol reduced Col1a1 and Acta2 expression and decreased alpha-smooth muscle actin (α-SMA) protein abundance. These findings provide hypothesis-generating evidence that β-sitosterol modulates inflammatory and profibrotic activation in mesangial-cell models, but they do not establish direct COX-2 enzymatic inhibition or therapeutic efficacy in CGN.

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Journal
Journal of Visualized Experiments
Published
2026-08-28
DOI
https://doi.org/10.3791/73000
Primary Topic
Cholesterol and Lipid Metabolism
Type
article
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article

Network-guided Evaluation of β-sitosterol in Inflammatory and Profibrotic Mesangial-Cell Models Relevant to Chronic Glomerulonephritis

Lian He, Zhen Huang, Haipeng He, Jie Cen et al.
Journal of Visualized Experiments
Cholesterol and Lipid Metabolism
article

Network-guided Evaluation of β-sitosterol in Inflammatory and Profibrotic Mesangial-Cell Models Relevant to Chronic Glomerulonephritis

Lian He, Zhen Huang, Haipeng He, Jie Cen, Fei Chen
article en

Abstract

Chronic glomerulonephritis (CGN) is characterized by persistent inflammatory injury and progressive fibrotic remodeling, yet compound-target relationships underlying natural-product-based interventions remain incompletely defined. This study integrated network pharmacology, validated molecular docking, and in vitro experiments to evaluate candidate constituents of Cordyceps sinensis (C. sinensis) in CGN-related pathological processes. Candidate constituents of C. sinensis were screened, and the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform-derived compound-associated targets were intersected with CGN-associated genes. Functional enrichment and protein-protein interaction analyses were used to prioritize biological processes and hub targets. PTGS2 was identified as a key overlapping target. Molecular docking was performed using a celecoxib-bound COX-2 structure. Re-docking of the co-crystallized celecoxib ligand reproduced the crystallographic pose with an RMSD of 0.876 Å, supporting the docking protocol. β-Sitosterol and linoleyl acetate showed predicted compatibility with the COX-2 docking region, with binding affinities of -7.2 and -7.5 kcal/mol, respectively. β-Sitosterol was selected for compound-level validation in HBZY-1 rat glomerular mesangial cells. At 0.5-10 µM, β-sitosterol did not markedly reduce cell viability. In Lipopolysaccharide (LPS)-stimulated cells, β-sitosterol reduced Tnf, Il6, and Ptgs2 expression, decreased prostaglandin E2 (PGE2) production, and reduced cyclooxygenase-2 (COX-2) protein abundance. In transforming growth factor β1 (TGF-β1)-treated cells, β-sitosterol reduced Col1a1 and Acta2 expression and decreased alpha-smooth muscle actin (α-SMA) protein abundance. These findings provide hypothesis-generating evidence that β-sitosterol modulates inflammatory and profibrotic activation in mesangial-cell models, but they do not establish direct COX-2 enzymatic inhibition or therapeutic efficacy in CGN.

Journal of Visualized Experiments(234)
Integrated Chinese Medicine (China) (CN), Ezhou Central Hospital (CN), Shanghai Traditional Chinese Medicine Hospital (CN), Qiqihar Medical University (CN)
Good health and well-being
Openalex Percentile: Top 8%
Cholesterol and Lipid Metabolism
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