ArticleInflammation2023
Betulin and Its Derivatives Reduce Inflammation and COX-2 Activity in Macrophages.
Article in Inflammation, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 28 citations in OpenAlex.
- Phytochemical Profile and Antioxidant Potential ofAntioxidants (Basel, Switzerland) · 2026Article
- New Synthetic Approach to C‑30 Ethers, Esters, and Amines of Betulin Using the Mitsunobu Reaction and Biological Evaluation of the Products.ACS omega · 2026Article
- Natural extract-derived compounds for the treatment of hematological diseases through modulation of the bone marrow microenvironment.Frontiers in chemistry · 2026Review
- Insights into the Recent Breakthroughs in Nanotechnological Outlook of Pentacyclic Triterpenoids: An Updated Approach.Current pharmaceutical design · 2026Review
- Article
- Phytotherapy with Fruit Seed Extracts as a Promising Approach for the Treatment of Inflammation.Current nutrition reports · 2025Review
- The Role of Triterpenoids in Gastric Ulcer: Mechanisms and Therapeutic Potentials.International journal of molecular sciences · 2025Review
- sRNA113 regulatesZoological research · 2025Article
- Molecular docking analysis of PI3K/AKT with betulin fromBioinformation · 2025Article
- Tuning of the Anti-Breast Cancer Activity of Betulinic Acid via Its Conversion to Ionic Liquids.Pharmaceutics · 2024Article
- Exploring the Action Mechanism and Validation of the Key Pathways ofCombinatorial chemistry & high throughput screening · 2024Article
- Synthesis, Pharmacological Properties, and Potential Molecular Mechanisms of Antitumor Activity of Betulin and Its Derivatives in Gastrointestinal Cancers.Pharmaceutics · 2023Review
- The Influence of Betulin Derivatives EB5 and ECH147 on the Expression of Selected TGFβ Superfamily Genes,Current issues in molecular biology · 2023Article
Corrections and comments
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Authors and funding
14 authors at 4 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Betulin is a heavily studied natural compound for its use as an anticancer or pro-regenerative agent. The structural similarity between betulin to steroids gives rise to the idea that the substance may as well act as an anti-inflammatory drug. This study is the first to describe the anti-inflammatory properties of betulinic acid, betulin, and its derivatives with amino acids 1,4-diaminebutane (Dab), 1,3-diaminepropane (Dap), Ornithine (Orn), and lysine (Lys) on murine macrophages from lymphoma site. The compounds were compared to dexamethasone. To establish the response of the macrophages to the natural compounds, we tested the viability as well as sensitivity to the inflammatory signaling (IFNγR). IL-6 secretory properties and HSP-70 content in the cells were examined. Furthermore, we characterized the effects of compounds on the inhibition of cyclooxygenase-2 (COX-2) activity both in the enzymatic assays and molecular docking studies. Then, the changes in COX-2 expression after betulin treatment were assessed. Betulin and betulinic acid are the low-cytotoxicity compounds with the highest potential to decrease inflammation via reduced IL-6 secretion. To some extent, they induce the reorganization of IFNγR with nearly no effect on COX-2 activity. Conversely, Bet-Orn and Bet-Lys are highly cytotoxic and induce the aggregation of IFNγR. Besides, Bet-Lys reduces the activity of COX-2 to a higher degree than dexamethasone. Bet-Orn is the only one to increase the HSP-70 content in the macrophages. In case of IL-6 reduction, all compounds were more potent than dexamethasone.
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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.