ArticleJournal of medicinal chemistry2020
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
Article in Journal of medicinal chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It is linked to trial NCT05343611 (Combining Vitamin E-functionalized CHOcolate With Physical Exercise to Reduce the risK Of Protein Energy Malnutrition in Pre-dementia AGEd People), which is not on this map. Cited by 21 papers.
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.
Combining Vitamin E-functionalized CHOcolate With Physical Exercise to Reduce the risK Of Protein Energy Malnutrition in Pre-dementia AGEd People
Who cites it
21 citing papers in PubMed, 42 citations in OpenAlex.
- Article
- Structure-based machine learning model for discovering pregnane X receptor (PXR) agonists and biological activity validation.Archives of toxicology · 2026Article
- Tocotrienol metabolites redirect lipid mediator production in innate immune cells towards inflammation resolution.Acta pharmaceutica Sinica. B · 2026Article
- The Vitamin E Derivative Garcinoic Acid Suppresses NLRP3 Inflammasome Activation and Pyroptosis in Murine Macrophages.Inflammation · 2025Article
- A two-in-one expression construct for biophysical and structural studies of the human pregnane X receptor ligand-binding domain, a pharmaceutical and environmental target.Acta crystallographica. Section F, Structural biology communications · 2025Article
- Modulation ofMicroorganisms · 2024Article
- Article
- α-Tocopherol-13'-Carboxychromanol Induces Cell Cycle Arrest and Cell Death by Inhibiting the SREBP1-SCD1 Axis and Causing Imbalance in Lipid Desaturation.International journal of molecular sciences · 2023Article
- Vitamin E and Metabolic Health: Relevance of Interactions with Other Micronutrients.Antioxidants (Basel, Switzerland) · 2022Review
- Vitamin E (Alpha-Tocopherol) Metabolism and Nutrition in Chronic Kidney Disease.Antioxidants (Basel, Switzerland) · 2022Review
- Metabolism of natural forms of vitamin E and biological actions of vitamin E metabolites.Free radical biology & medicine · 2022Article
- Review ofFrontiers in endocrinology · 2022Review
- Overcoming the Pregnane X Receptor Liability: Rational Design to Eliminate PXR-Mediated CYP Induction.ACS medicinal chemistry letters · 2021Article
- Exploration of Long-Chain Vitamin E Metabolites for the Discovery of a Highly Potent, Orally Effective, and Metabolically Stable 5-LOX Inhibitor that Limits Inflammation.Journal of medicinal chemistry · 2021Article
- Alpha-Tocopherol Metabolites (the Vitamin E Metabolome) and Their Interindividual Variability during Supplementation.Antioxidants (Basel, Switzerland) · 2021Article
- A Facile Semisynthesis and Evaluation of Garcinoic Acid and Its Analogs for the Inhibition of Human DNA Polymerase β.Molecules (Basel, Switzerland) · 2020Article
- Vitamin E acetate as linactant in the pathophysiology of EVALI.Medical hypotheses · 2020Article
- Weak Microbial Metabolites: a Treasure Trove for Using Biomimicry to Discover and Optimize Drugs.Molecular pharmacology · 2020Article
- Garcinoic acid prevents β-amyloid (Aβ) deposition in the mouse brain.The Journal of biological chemistry · 2020Article
- Diversity of Chromanol and Chromenol Structures and Functions: An Emerging Class of Anti-Inflammatory and Anti-Carcinogenic Agents.Frontiers in pharmacology · 2020Review
Corrections and comments
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Authors and funding
19 authors at 4 institutions in 2 countries.
Funding
Abstract
Pregnane X receptor (PXR) is a master xenobiotic-sensing transcription factor and a validated target for immune and inflammatory diseases. The identification of chemical probes to investigate the therapeutic relevance of the receptor is still highly desired. In fact, currently available PXR ligands are not highly selective and can exhibit toxicity and/or potential off-target effects. In this study, we have identified garcinoic acid as a selective and efficient PXR agonist. The properties of this natural molecule as a specific PXR agonist were demonstrated by the screening on a panel of nuclear receptors, the assessment of the physical and thermodynamic binding affinity, and the determination of the PXR-garcinoic acid complex crystal structure. Cytotoxicity, transcriptional, and functional properties were investigated in human liver cells, and compound activity and target engagement were confirmed in vivo in mouse liver and gut tissue. In conclusion, garcinoic acid is a selective natural agonist of PXR and a promising lead compound toward the development of new PXR-regulating modulators.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.