Abstract
The effects of MMHD [(S,E)-2-methyl-1-(2-methylthiazol-4-yl) hexa-1,5-dien-ol], a novel synthetic compound derived from epothilone, was investigated for its effects on the expression of proinflammatory mediators in lipopolysaccharide-stimulated BV-2 microglia. MMHD attenuated the expressions of inducible nitric oxide synthase and cyclooxygenase-2 mRNA and protein without affecting cell viability. Moreover, MMHD suppressed nuclear factor-kappaB (NF-kappaB) activation via the translocation of p65 into the nucleus. These results indicate that MMHD exerts anti-inflammatory properties by suppressing the transcription of proinflammatory cytokine genes through the NF-kappaB signaling pathway.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Anti-Inflammatory Agents / pharmacology*
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Cell Survival / drug effects
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Cyclooxygenase 2 / drug effects
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Cyclooxygenase 2 / genetics
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Cytokines / drug effects*
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Cytokines / metabolism
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Gene Expression Regulation / drug effects
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Inflammation Mediators / metabolism
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Lipopolysaccharides / pharmacology
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Mice
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Microglia / drug effects*
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Microglia / metabolism
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NF-kappa B / metabolism
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Nitric Oxide Synthase Type II / drug effects
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Nitric Oxide Synthase Type II / genetics
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Protein Transport / drug effects
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RNA, Messenger / drug effects
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RNA, Messenger / metabolism
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Thiazoles / pharmacology*
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Transcription Factor RelA / metabolism
Substances
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2-methyl-1-(2-methylthiazol-4-yl)hexa-1,5-dienol
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Anti-Inflammatory Agents
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Cytokines
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Inflammation Mediators
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Lipopolysaccharides
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NF-kappa B
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RNA, Messenger
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Thiazoles
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Transcription Factor RelA
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Nitric Oxide Synthase Type II
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Cyclooxygenase 2