ArticleThe Journal of clinical endocrinology and metabolism2025
2'-O-Galloylhyperin Prevents Tissue Remodeling in Thyroid Eye Disease: Prospects as a Thyrotropin Receptor Antagonist.
Article in The Journal of clinical endocrinology and metabolism, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers, 1 of them a synthesis that pooled it.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
3 citing papers in PubMed, 1 synthesis or guideline pooled it.
- Protein Spatial Structure Meets Artificial Intelligence: Revolutionizing Drug Synergy-Antagonism in Precision Medicine.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Pooled it
- Targeted Delivery of CD34 Aptamer-Coupled Tocilizumab Microspheres for Effective Treatment of Thyroid-Associated Ophthalmopathy.Investigative ophthalmology & visual science · 2025Article
- 2'-O-Galloylhyperin Prevents Tissue Remodeling in Thyroid Eye Disease: Prospects as a Thyrotropin Receptor Antagonist.The Journal of clinical endocrinology and metabolism · 2025Article
Corrections and comments
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Authors and funding
8 authors.
Funding
Abstract
contextThyroid eye disease (TED) is a challenging condition owing to relentless orbital tissue remodeling, with thyrotropin receptor (TSHR) in orbital fibroblasts (OFs) serving as a promising therapeutic target.
objectiveThis study seeks to discover potential TSHR inhibitors among US Food and Drug Administration (FDA)-approved drugs and evaluate their effects on TED-OFs.
methodsAdipose tissues were sourced from the patients with or without TED. Isolated OFs were cultivated in proliferation medium or stimulated for adipogenic/fibrotic differentiation in 2-dimensional/3-dimenstional models, treated with 2'-O-galloylhyperin (2'-O-GH) (0, 5, 20, and 50 μM). Using structure-based virtual screening (SBVS), potential TSHR antagonists were identified. Cellular proliferation was analyzed by 5-ethynyl-2'-deoxyuridine (EdU) incorporation, flow cytometry, and spheroid size. Adipogenesis was determined by Oil Red O staining, Western blot, and immunofluorescence (IF). Fibrosis was assessed using wound-healing assays, Western blot and IF. Cyclic adenosine monophosphate (cAMP), hyaluronan (HA), and cytokine were quantified by enzyme-linked immunosorbent assay.
resultsHerein, the FDA-approved drug 2'-O-GH dose-dependently decreased cAMP production and the subsequent cAMP-response element binding protein (CREB) phosphorylation stimulated by a TSHR-stimulating monoclonal autoantibody M22, which was reversed by a consistently activated mutation of TSHR (L629F). As expected, 2'-O-GH attenuated lipid accumulation in TED-OFs, along with downregulation of key adipogenic markers, and 2'-O-GH ameliorated HA production during adipogenesis. Notably, 2'-O-GH dampened wound closure and fibrotic differentiation of TED-OF stimulated by transforming growth factor beta 1. Correspondingly, proliferation of TED-OFs was halted by 2'-O-GH.
conclusion2'-O-GH is promising for prevention of tissue remodeling of TED by exerting inhibitory effects on proliferation, differentiation, and HA deposition by inhibiting TSHR activation, implying its potential therapeutic value for TED.
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