Abstract
Chalcones and their derivatives were synthesized and evaluated for their anti-inflammatory activity. In vitro, chalcones 2, 4, 8, 10 and 13 inhibited degranulation and 5-lipoxygenase in human neutrophils, whereas 11 behaved as scavenger of superoxide. Only four compounds (4-7) inhibited cyclo-oxygenase-2 activity. The majority of these samples showed anti-inflammatory effects in the mouse air pouch model.
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, Non-Steroidal / chemical synthesis*
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Anti-Inflammatory Agents, Non-Steroidal / chemistry
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology
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Arachidonate 5-Lipoxygenase / blood
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Chalcone / analogs & derivatives*
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Chalcone / chemical synthesis*
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Chalcone / chemistry
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Chalcone / pharmacology
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Cyclooxygenase 2
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Cyclooxygenase 2 Inhibitors
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Cyclooxygenase Inhibitors / chemical synthesis
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Cyclooxygenase Inhibitors / chemistry
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Cyclooxygenase Inhibitors / pharmacology
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Drug Design
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Humans
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Isoenzymes / blood
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Leukotriene B4 / blood
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Lipoxygenase Inhibitors / chemical synthesis
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Lipoxygenase Inhibitors / chemistry
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Lipoxygenase Inhibitors / pharmacology
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Membrane Proteins
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Mice
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Molecular Structure
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Neutrophils / drug effects
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Neutrophils / physiology
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Propiophenones / chemical synthesis*
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Propiophenones / chemistry
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Propiophenones / pharmacology
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Prostaglandin-Endoperoxide Synthases / blood
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Structure-Activity Relationship
Substances
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Anti-Inflammatory Agents, Non-Steroidal
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Cyclooxygenase 2 Inhibitors
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Cyclooxygenase Inhibitors
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Isoenzymes
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Lipoxygenase Inhibitors
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Membrane Proteins
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Propiophenones
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Leukotriene B4
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Chalcone
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Arachidonate 5-Lipoxygenase
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Cyclooxygenase 2
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PTGS2 protein, human
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Prostaglandin-Endoperoxide Synthases