Abstract
An inhibitor of cyclooxygenase (COX)-1 activity of prostaglandin H2 synthase was isolated from aerial parts of Celastrus orbiculatus Thunb. (Celastraceae), an oriental folk medicine for rheumatoid arthritis by activity-guided column chromatographic methods. The COX inhibitor was identified as (-)-epiafzelechin, a member of flavan-3-ols by the structural analysis with HR-EI-mass, 1H-NMR and 13C-NMR spectral data. The compound exhibited a dose-dependent inhibition on the COX activity with an IC50 value of 15 microM. (-)-Epiafzelechin exhibited about 3-fold weaker inhibitory potency on the enzyme activity than indomethacin as a positive control. (-)-Epiafzelechin exhibited significant anti-inflammatory activity on carrageenin-induced mouse paw edema when the compound (100 mg/kg) was orally administrated at 1 h before carrageenin treatment.
Publication types
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Letter
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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 / chemistry
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Anti-Inflammatory Agents, Non-Steroidal / isolation & purification
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
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Carrageenan
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Catechin / analogs & derivatives*
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Catechin / chemistry
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Catechin / isolation & purification
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Catechin / pharmacology
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Cyclooxygenase 1
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Cyclooxygenase Inhibitors / chemistry
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Cyclooxygenase Inhibitors / isolation & purification
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Cyclooxygenase Inhibitors / pharmacology*
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Edema / chemically induced
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Edema / drug therapy
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Isoenzymes / metabolism*
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Male
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Medicine, Chinese Traditional
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Membrane Proteins
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Mice
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Mice, Inbred ICR
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Molecular Structure
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Plant Extracts / chemistry
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Plant Extracts / pharmacology
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Plants, Medicinal*
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Prostaglandin-Endoperoxide Synthases / metabolism*
Substances
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Anti-Inflammatory Agents, Non-Steroidal
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Cyclooxygenase Inhibitors
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Isoenzymes
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Membrane Proteins
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Plant Extracts
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epiafzelechin
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Catechin
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Carrageenan
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Cyclooxygenase 1
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Prostaglandin-Endoperoxide Synthases
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Ptgs1 protein, mouse