isoegomaketone and Inflammation

Isoegomaketone (IK) is a known component of

Topics: Animals; Furans; Gene Expression Regulation, Enzymologic; Heme Oxygenase-1; Inflammation; Interferon-beta; Interleukin-6; Ketones; Lipopolysaccharides; Membrane Proteins; Mice; Nitric Oxide; RAW 264.7 Cells

Topics: Animals; Antibodies; Arthritis, Experimental; Arthritis, Rheumatoid; Collagen; Disease Models, Animal; Edema; Furans; Inflammation; Ketones; Male; Mice; Mice, Inbred BALB C

The anti-inflammatory activities of a prepared isoegomaketone 3a and its derivatives 3b-3f were evaluated in RAW 264.7 cells. Among these, the compound 3d was displayed the most potent inhibitory activities against production of nitric oxide, monocyte chemoattractant protein-1 and interleukin-6. Based on these results, the abilities of compounds 3a-3f to modulate NF-κB and AP-1-mediated gene transcription using a luciferase reporter assay were investigated. The transcriptional activities of NF-κB and AP-1 decreased when pretreated with 3a-3f. Interestingly, at 10 μM, compound 3d markedly suppressed the lipopolysaccharide-induced NF-κB and activator protein-1 DNA binding activities. Some preliminary structure-activity relationships were proposed that may provide a direction for further study.

Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Cell Survival; Chemokine CCL2; Drug Evaluation, Preclinical; Furans; Inflammation; Interleukin-6; Ketones; Luciferases; Macrophages; Mice; Nitric Oxide; Perilla frutescens; Phytotherapy; Structure-Activity Relationship