title: Biological evaluation of isoegomaketone isolated from Perilla frutescens and its synthetic derivatives as anti-inflammatory agents.
abstract: 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.
authors: Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute, Jeongup 580-185, Korea.
authors: Yong Dae
authors: YD
authors: Park
authors: Chang Hyun
authors: CH
authors: Jin
authors: Dae Seong
authors: DS
authors: Choi
authors: Myung-Woo
authors: MW
authors: Byun
authors: Il Yun
authors: IY
authors: Jeong
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry / Q000276:immunology / Q000302:isolation & purification* / Q000494:pharmacology*; D002470:Cell Survival / Q000187:drug effects; D018932:Chemokine CCL2 / Q000378:metabolism; D004353:Drug Evaluation, Preclinical; D005663:Furans / Q000737:chemistry / Q000276:immunology / Q000302:isolation & purification* / Q000494:pharmacology*; D007249:Inflammation / Q000139:chemically induced / Q000188:drug therapy*; D015850:Interleukin-6 / Q000378:metabolism; D007659:Ketones / Q000737:chemistry / Q000276:immunology / Q000302:isolation & purification* / Q000494:pharmacology*; D008156:Luciferases / Q000378:metabolism; D008264:Macrophages; D051379:Mice; D009569:Nitric Oxide / Q000378:metabolism; D031344:Perilla frutescens; D008517:Phytotherapy; D013329:Structure-Activity Relationship
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; C111835:CCL2 protein, human; D018932:Chemokine CCL2; D005663:Furans; D015850:Interleukin-6; D007659:Ketones; C568138:isoegomaketone; D009569:Nitric Oxide; D008156:Luciferases