Abstract
(±)-Dispirocochlearoids A-C (1-3), meroterpenoids with a 6/6/5/6/6/6 ring system, were isolated from Ganoderma cochlear. 1-3 are selective COX-2 inhibitors with an IC50 value of (-)-2 at 386 nM. Site-directed mutagenesis identified His351 as a COX-2 active site. In vivo anti-inflammatory activities of (-)-2 were performed against acute lung injury in mice.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Acute Lung Injury / drug therapy*
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Acute Lung Injury / metabolism
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Acute Lung Injury / pathology
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Animals
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Anti-Inflammatory Agents, Non-Steroidal / chemistry
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Anti-Inflammatory Agents, Non-Steroidal / metabolism
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
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Catalytic Domain
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Cyclooxygenase 2 / analysis*
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Cyclooxygenase 2 / genetics
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Cyclooxygenase 2 / metabolism
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Cytokines / antagonists & inhibitors*
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Cytokines / biosynthesis
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Disease Models, Animal
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Ganoderma / chemistry*
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Ganoderma / metabolism
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Lipopolysaccharides / antagonists & inhibitors
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Lipopolysaccharides / pharmacology
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Macrophages / drug effects
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Macrophages / metabolism
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Macrophages / pathology
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Mice
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Molecular Conformation
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Molecular Probes / chemistry
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Molecular Probes / metabolism
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Molecular Probes / pharmacology*
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Stereoisomerism
Substances
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Anti-Inflammatory Agents, Non-Steroidal
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Cytokines
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Lipopolysaccharides
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Molecular Probes
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Cyclooxygenase 2