ArticleDrug design, development and therapy2021
Design, Synthesis, Molecular Modelling, and Biological Evaluation of Oleanolic Acid-Arylidene Derivatives as Potential Anti-Inflammatory Agents.
Article in Drug design, development and therapy, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed, 15 citations in OpenAlex.
- Generation of G9 genotype porcine rotavirus using reverse genetics system and its application for antiviral screen and vaccine development.Virologica Sinica · 2026Article
- Recent Advances in the Development of Selected Triterpenoid-Based Hybrid Molecules and Their Antimicrobial Activities: A Review.Antibiotics (Basel, Switzerland) · 2026Review
- Recent Advancements in Pentacyclic and Other Terpenoid Derivatives as Anti-inflammatory Agents.Mini reviews in medicinal chemistry · 2026Review
- Biological Activities of Novel Oleanolic Acid Derivatives from Bioconversion and Semi-Synthesis.Molecules (Basel, Switzerland) · 2024Review
- Repurposing approved non-oncology drugs for cancer therapy: a comprehensive review of mechanisms, efficacy, and clinical prospects.European journal of medical research · 2023Review
- Evolution of Natural Product Scaffolds as Potential Proteasome Inhibitors in Developing Cancer Therapeutics.Metabolites · 2023Review
- Plant-Derived Natural Compounds for the Treatment of Amyotrophic Lateral Sclerosis: An Update.Current neuropharmacology · 2022Review
- Depression: An Insight into Heterocyclic and Cyclic Hydrocarbon Compounds Inspired from Natural Sources.Current neuropharmacology · 2021Article
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Authors and funding
9 authors at 4 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
introductionOleanolic acid, a pentacyclic triterpenic acid, is widely distributed in medicinal plants and is the most commonly studied triterpene for various biological activities, including anti-allergic, anti-cancer, and anti-inflammatory.
methodsThe present study was carried out to synthesize arylidene derivatives of oleanolic acid at the C-2 position by Claisen Schmidt condensation to develop more effective anti-inflammatory agents. The derivatives were screened for anti-inflammatory activity by scrutinizing NO production inhibition in RAW 264.7 cells induced by LPS and their cytotoxicity. The potential candidates were further screened for inhibition of LPS-induced interleukin (IL-6) and tumour necrosis factor-alpha (TNF-α) production in RAW 264.7 cells.
resultsThe results of in vitro studies revealed that derivatives 3d, 3e, 3L, and 3o are comparable to that of the oleanolic acid on the inhibition of TNF-α and IL-6 release. However, derivative 3L was identified as the most potent inhibitor of IL-6 (77.2%) and TNF-α (75.4%) when compared to parent compound, and compounds 3a (77.18%), 3d (71.5%), and 3e (68.8%) showed potent inhibition of NO than oleanolic acid (65.22%) at 10µM. Besides, from docking score and Cyscore analysis analogs (3e, 3L, 3n) showed greater affinity towards TNF-α and IL-1β than dexamethasone.
conclusionHerein, we report a series of 15 new arylidene derivatives of oleanolic acid by Claisen Schmidt condensation reaction. All the compounds synthesized were screened for their anti-inflammatory activity against NO, TNF-α and IL-6. From the data, it was evident that most of the compounds exhibited better anti-inflammatory activity.
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