Betulinic acid is a PPARγ antagonist that improves glucose uptake, promotes osteogenesis and inhibits adipogenesis

@article{Brusotti2017BetulinicAI,
  title={Betulinic acid is a PPAR$\gamma$ antagonist that improves glucose uptake, promotes osteogenesis and inhibits adipogenesis},
  author={Gloria Brusotti and Roberta Montanari and Davide Capelli and Giulia Cattaneo and Antonio Laghezza and Paolo Tortorella and Fulvio Loiodice and Franck Peiretti and Bernadette Bonardo and Alessandro Paiardini and Enrica Calleri and Giorgio Pochetti},
  journal={Scientific Reports},
  year={2017},
  volume={7}
}
PPAR antagonists are ligands that bind their receptor with high affinity without transactivation activity. Recently, they have been demonstrated to maintain insulin-sensitizing and antidiabetic properties, and they serve as an alternative treatment for metabolic diseases. In this work, an affinity-based bioassay was found to be effective for selecting PPAR ligands from the dried extract of an African plant (Diospyros bipindensis). Among the ligands, we identified betulinic acid (BA), a compound… 
Betulinic acid lowers lipid accumulation in adipocytes through enhanced NCoA1-PPARγ interaction.
TLDR
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The Rosmarinus Bioactive Compound Carnosic Acid Is a Novel PPAR Antagonist That Inhibits the Browning of White Adipocytes
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It is shown here that CA inhibits the browning of white adipocytes and favors decreased gene expression of thermogenic markers, which shed some light on the development of natural PPAR antagonists and their potential effects on thermogenic response.
Betulinic acid decreases lipid accumulation in adipogenesis-induced human mesenchymal stem cells with upregulation of PGC-1α and UCP-1 and post-transcriptional downregulation of adiponectin and leptin secretion
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A wide group of natural compounds (flavonoids, stilbenes, neolignans and others) has been identified as Peroxisome Proliferator-Activated Receptor (PPAR) agonists, with a large variety of chemical
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Betulinic Acid Inhibits RANKL-Induced Osteoclastogenesis via Attenuating Akt, NF-κB, and PLCγ2-Ca2+ Signaling and Prevents Inflammatory Bone Loss.
TLDR
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TXN, a Xanthohumol Derivative, Attenuates High-Fat Diet Induced Hepatic Steatosis by Antagonizing PPARγ
TLDR
Molecular docking simulations demonstrated XN and TXN bind in the PPARγ ligand-binding domain pocket, consistent with XNand TXN acting as antagonists of PParγ.
Insights into Dynamic Mechanism of Ligand Binding to Peroxisome Proliferator-Activated Receptor γ toward Potential Pharmacological Applications.
  • Y. Miyamae
  • Medicine
    Biological & pharmaceutical bulletin
  • 2021
TLDR
An overview of the peculiar characteristics of the PPARγ LBD is provided by examining a series of structural studies focused on the dynamic mechanism of binding and the potential applications of strategies for ligand screening and chemical labeling.
Tetrahydroxanthohumol, a xanthohumol derivative, attenuates high-fat diet-induced hepatic steatosis by antagonizing PPARγ
TLDR
Findings are consistent with XN and TXN acting as antagonists of PPARγ, and a peroxisome proliferator activated receptor gamma (PPARγ) competitive binding assay showed that XNand TXN bind to PPARα with an IC50 similar to pioglitazone and 8–10 times stronger than oleate.
Protective effect of triterpenes against diabetes-induced β-cell damage: An overview of in vitro and in vivo studies.
TLDR
This review summarises most relevant effects of various triterpenes on improving pancreatic β-cell function in both in vitro and in vivo experimental models and reports on the ameliorative properties of these compounds against insulin resistance, oxidative stress and inflammation.
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