Ergolide

SKU: orb1308823

Description

Ergolide, a sesquiterpene lactone from Inula britannica, suppresses iNOS and COX-2 expression in RAW 264.7 macrophages via NF-κB inhibition. This activity supports its research use in studying inflammation pathways, with applications in both in vitro and in vivo models of inflammatory diseases.

Research Area

Signal Transduction

Key Properties

• CAS Number: 54999-07-4
• MW: 306.35
• Purity: 99.64% (May vary between batches)
• Formula: C₁₇H₂₂O₅
• SMILES: [H][C@]12C[C@@H](C)[C@]3([H])CCC(=O)[C@@]3(C)[C@@H](OC(C)=O)[C@]1([H])C(=C)C(=O)O2
• Target: NF-κB
• Solubility: 10% DMSO+90% Corn Oil:2.5 mg/mL (8.16 mM);DMSO:50 mg/mL (163.21 mM)

Bioactivity

• In Vitro:
  Ergolide markedly decreased the production of prostaglandin E(2) (PGE(2)) in cell-free extract of LPS/IFN-gamma-stimulated RAW 264.7 macrophages in a concentration-dependent manner, without alteration of the catalytic activity of COX-2 itself. Ergolide decreased the level of iNOS and COX-2 protein, and iNOS mRNA caused by stimulation of LPS/IFN-gamma in a concentration-dependent manner, as measured by Western blot and Northern blot analysis, respectively. Ergolide inhibited nuclear factor-kappaB (NF-kappaB) activation, a transcription factor necessary for iNOS and COX-2 expression in response to LPS/IFN-gamma. This effect was accompanied by the parallel reduction of nuclear translocation of subunit p65 of NF-kappaB as well as IkappaB-alpha degradation. In addition, these effects were completely blocked by treatment of cysteine, indicating that this inhibitory effect of ergolide could be mediated by alkylation of NF-kappaB itself or an upstream molecule of NF-kappaB. Ergolide also directly inhibited the DNA-binding activity of active NF-kappaB in LPS/IFN-gamma-pretreated RAW 264.7 macrophages. These results demonstrate that the suppression of NF-kappaB activation by ergolide might be attributed to the inhibition of nuclear translocation of NF-kappaB resulted from blockade of the degradation of IkappaB and the direct modification of active NF-kappaB, leading to the suppression of the expression of iNOS and COX-2, which play important roles in inflammatory signalling pathway.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Ergolide, Inhibitor, inhibit, NF-κB, NFkB, NF-kB, NFκB, Nuclear factor-kappaB, Nuclear factor-κB

Compound Identifiers

PubChem CID

185786