Highly oxygenated ent-abietane diterpenoid lactones from Euphorbia peplus and their anti-inflammatory activity
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View abstract on PubMed
Summary
This summary is machine-generated.Eleven new compounds from Euphorbia peplus show anti-inflammatory effects. Compound 6 significantly reduced inflammatory mediators and may be a potential treatment for inflammation-related diseases.
Area Of Science
- Natural Product Chemistry
- Pharmacology
- Medicinal Chemistry
Background
- Euphorbia peplus is a source of diverse bioactive compounds.
- Ent-abietane diterpenoid lactones possess various biological activities.
- Inflammation is a key factor in numerous diseases.
Purpose Of The Study
- To isolate and characterize new ent-abietane diterpenoid lactones from Euphorbia peplus.
- To evaluate the anti-inflammatory potential of these compounds.
- To identify potential therapeutic agents for inflammation-related diseases.
Main Methods
- Isolation and structure elucidation using NMR, HRESIMS, and single-crystal X-ray diffraction.
- Determination of absolute configurations via ECD and DP4+ calculations.
- In vitro anti-inflammatory assays on LPS-induced RAW 264.7 macrophages, measuring nitric oxide and cytokine mRNA expression.
Main Results
- Eleven new ent-abietane diterpenoid lactones (euphjatrophanes H-R) were identified.
- Compounds 6-9, 12-16, and 19 inhibited nitric oxide production.
- Compounds 6, 9, 11, and 16 suppressed key inflammatory cytokine mRNA expression (IL-6, IL-1β, TNFα).
- Compound 6 showed dose-dependent inhibition and modulated FOXO1 expression and NF-κB p65 phosphorylation.
Conclusions
- New ent-abietane diterpenoid lactones were discovered from Euphorbia peplus.
- Several compounds exhibited significant anti-inflammatory properties.
- Compound 6 is a promising candidate for developing novel anti-inflammatory therapeutics.
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