ArticleScientific reports2017
Betulinic acid is a PPARγ antagonist that improves glucose uptake, promotes osteogenesis and inhibits adipogenesis.
Article in Scientific reports, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 43 papers.
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Who cites it
43 citing papers in PubMed, 74 citations in OpenAlex.
- Article
- Evaluation of 3',4'-Di-Biomolecules · 2026Article
- Distinctive Behavior and Selective Modulation of PPARγ by Pentacyclic Triterpenoid Pomolic Acid and Hederagenin fromJournal of agricultural and food chemistry · 2026Article
- Metabolic dysfunction‑associated steatotic liver disease: Pathogenesis, model and treatment (Review).International journal of molecular medicine · 2025Review
- Combined Metabolomics and Network Pharmacology to Reveal Anti-Diabetic Mechanisms and Potential Pharmacological Components ofPlants (Basel, Switzerland) · 2025Article
- Dual Modulation of Adipogenesis and Apoptosis by PPARG Agonist Rosiglitazone and Antagonist Betulinic Acid in 3T3-L1 Cells.Biomedicines · 2025Article
- Pharmacology of Non-Psychoactive Phytocannabinoids and Their Potential for Treatment of Cardiometabolic Disease.Handbook of experimental pharmacology · 2025Review
- Integrative in-silico and in-vitro analysis of taurine and vitamin B12 in modulating PPARγ and Wnt signaling in hyperhomocysteinemia-induced osteoporosis.Biology direct · 2024Article
- Ziziphus jujuba (Jujube) in Metabolic Syndrome: From Traditional Medicine to Scientific Validation.Current nutrition reports · 2024Review
- Complex Inhibitory Activity of Pentacyclic Triterpenoids against Cutaneous Melanoma In Vitro and In Vivo: A Literature Review and Reconstruction of Their Melanoma-Related Protein Interactome.ACS pharmacology & translational science · 2024Review
- Betulin Stimulates Osteogenic Differentiation of Human Osteoblasts-Loaded Alginate-Gelatin Microbeads.Bioengineering (Basel, Switzerland) · 2024Article
- A Systematic Review ofLife (Basel, Switzerland) · 2023Review
- Lupenone-Rich Fraction Derived fromLife (Basel, Switzerland) · 2023Article
- Review
- Effects of Betulinic Acid on the Proliferation, Cellular Senescence, and Type 1 Interferon-Related Signaling Pathways in Human Dermal Fibroblasts.Journal of agricultural and food chemistry · 2023Article
- Biological Screening and Crystallographic Studies of Hydroxy γ-Lactone Derivatives to Investigate PPARγ Phosphorylation Inhibition.Biomolecules · 2023Article
- The role of PPARγ in prostate cancer development and progression.British journal of cancer · 2023Review
- Article
- Astrocytes in the Neuropathology of Bipolar Disorder: Review of Current Evidence.Brain sciences · 2022Review
- Recent Advances Regarding the Molecular Mechanisms of Triterpenic Acids: A Review (Part II).International journal of molecular sciences · 2022Review
Corrections and comments
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Authors and funding
12 authors at 6 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
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 already known for its anti-inflammatory, anti-tumour and antidiabetic properties, as a PPARγ and PPARα antagonist. Cell differentiation assays showed that BA inhibits adipogenesis and promotes osteogenesis; either down-regulates or does not affect the expression of a series of adipogenic markers; and up-regulates the expression of osteogenic markers. Moreover, BA increases basal glucose uptake in 3T3-L1 adipocytes. The crystal structure of the complex of BA with PPARγ sheds light, at the molecular level, on the mechanism by which BA antagonizes PPARγ, and indicates a unique binding mode of this antagonist type. The results of this study show that the natural compound BA could be an interesting and safe candidate for the treatment of type 2 diabetes and bone diseases.
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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.