Abstract
The activation of peroxisome proliferator-activated receptor gamma (PPARgamma) has been shown to inhibit the production and the effects of proinflammatory cytokines. Since interleukin-1beta (IL-1beta) directly mediates cartilage degradation in osteoarthritis, we investigated the capability of PPARgamma ligands to modulate IL-1beta effects on human chondrocytes. RT-PCR and Western blot analysis revealed that PPARgamma expression was decreased by IL-1beta. 15-deoxy-Delta12,14-prostaglandin J2 (15d-PGJ2), in contrast to troglitazone, was highly potent to counteract IL-1beta-induced cyclooxygenase-2 and inductible nitric oxide synthase expression, NO production and the decrease in proteoglycan synthesis. Western blot and gel-shift analyses demonstrated that 15d-PGJ2 inhibited NF-kappaB activation, while troglitazone was ineffective. Although 15d-PGJ2 attenuated activator protein-1 binding on the DNA, it potentiated c-jun migration in the nucleus. The absence or the low effect of troglitazone suggests that 15d-PGJ2 action in human chondrocytes is mainly PPARgamma-independent.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Active Transport, Cell Nucleus / drug effects
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Blotting, Western
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Cell Nucleus / drug effects
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Cell Nucleus / metabolism
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Cells, Cultured
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Chondrocytes / cytology
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Chondrocytes / drug effects*
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Chondrocytes / metabolism
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Chromans / pharmacology*
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Cyclooxygenase 2
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DNA / genetics
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DNA / metabolism
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Enzyme Induction / drug effects
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Gene Expression Regulation / drug effects*
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Humans
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Interleukin-1 / antagonists & inhibitors
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Interleukin-1 / pharmacology*
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Isoenzymes / genetics
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Ligands
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Membrane Proteins
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NF-kappa B / metabolism*
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Nitric Oxide / metabolism
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Nitric Oxide Synthase / genetics
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Nitric Oxide Synthase Type II
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Prostaglandin D2 / analogs & derivatives
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Prostaglandin D2 / pharmacology*
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Prostaglandin-Endoperoxide Synthases / genetics
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Prostaglandins / biosynthesis
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Protein Binding / drug effects
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Proteoglycans / biosynthesis
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Proto-Oncogene Proteins c-jun / metabolism
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RNA, Messenger / genetics
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RNA, Messenger / metabolism
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Receptors, Cytoplasmic and Nuclear / genetics
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Receptors, Cytoplasmic and Nuclear / metabolism
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Signal Transduction / drug effects
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Thiazoles / pharmacology*
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Thiazolidinediones*
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Transcription Factor AP-1 / metabolism*
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Transcription Factors / genetics
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Transcription Factors / metabolism
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Troglitazone
Substances
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15-deoxy-delta(12,14)-prostaglandin J2
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Chromans
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Interleukin-1
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Isoenzymes
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Ligands
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Membrane Proteins
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NF-kappa B
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Prostaglandins
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Proteoglycans
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Proto-Oncogene Proteins c-jun
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RNA, Messenger
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Receptors, Cytoplasmic and Nuclear
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Thiazoles
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Thiazolidinediones
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Transcription Factor AP-1
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Transcription Factors
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Nitric Oxide
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DNA
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NOS2 protein, human
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Nitric Oxide Synthase
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Nitric Oxide Synthase Type II
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Cyclooxygenase 2
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PTGS2 protein, human
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Prostaglandin-Endoperoxide Synthases
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Troglitazone
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Prostaglandin D2