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Suppressive effects of furonaphthoquinone NFD-37 on the production of lipopolysaccharide-inducible inflammatory mediators in macrophages RAW 264.7.

Abstract
2-Methyl-2-(2-methylpropenyl)-2,3-dihydronaphthoquinone[2,3-b]furan-4,9-dione (NFD-37) is a synthetic furonaphthoquinone compound. In this study, we determined that NFD-37 could inhibit the lipopolysaccharide (LPS)-induced production of inflammatory mediators in macrophages RAW 264.7. This compound inhibited LPS-induced nitric oxide (NO) or prostaglandin (PG) E2 production in dose-dependent manners, with IC50 values of 7.2 microM and 5.3 microM, respectively. As the positive controls, pyrrolidine dithiocarbamate (30 microM) exhibited a 57% inhibition of NO production, and NS-398 (1 microM) manifested a 48% inhibition of PGE2 production. The inhibitory effects of NFD-37 on NO and PGE2 production were determined to occur in conjunction with the suppression of inducible NO synthase or cyclooxygenase-2 expression. NFD-37 also inhibited the production of LPS-inducible tumor necrosis factor-alpha, interleukin (IL)-1beta and IL-6, at IC50 values of 4.8-8.9 microM. We also determined the anti-inflammatory efficacy of NFD-37 using carrageenin-induced paw edema in experimental mice.
AuthorsMin-Hee Kim, Hyun-Mo Shin, Yong Rok Lee, Eun Yong Chung, Yoon Sook Chang, Kyung Rak Min, Youngsoo Kim
JournalArchives of pharmacal research (Arch Pharm Res) Vol. 28 Issue 10 Pg. 1170-6 (Oct 2005) ISSN: 0253-6269 [Print] Korea (South)
PMID16276975 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • 2-methyl-2-(2-methylpropenyl)-2,3-dihydronaphtho(2,3-b)furan-4,9-dione
  • Furans
  • Inflammation Mediators
  • Interleukin-1
  • Interleukin-6
  • Lipopolysaccharides
  • Naphthoquinones
  • Tumor Necrosis Factor-alpha
  • Nitric Oxide
  • Nitric Oxide Synthase Type II
  • Cyclooxygenase 2
  • Dinoprostone
Topics
  • Animals
  • Blotting, Western
  • Cell Line
  • Cell Survival (drug effects)
  • Cyclooxygenase 2 (genetics, metabolism)
  • Dinoprostone (metabolism)
  • Dose-Response Relationship, Drug
  • Furans (chemistry, pharmacology)
  • Inflammation Mediators (metabolism)
  • Interleukin-1 (metabolism)
  • Interleukin-6 (metabolism)
  • Lipopolysaccharides (pharmacology)
  • Macrophages (cytology, drug effects, metabolism)
  • Molecular Structure
  • Naphthoquinones (chemistry, pharmacology)
  • Nitric Oxide (metabolism)
  • Nitric Oxide Synthase Type II (genetics, metabolism)
  • Reverse Transcriptase Polymerase Chain Reaction
  • Transcription, Genetic (drug effects)
  • Tumor Necrosis Factor-alpha (metabolism)

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