(-)-Epiafzelechin: cyclooxygenase-1 inhibitor and anti-inflammatory agent from aerial parts of Celastrus orbiculatus.

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.
Authors	K R Min, B Y Hwang, H S Lim, B S Kang, G J Oh, J Lee, S H Kang, K S Lee, J S Ro, Y Kim
Journal	Planta medica (Planta Med) Vol. 65 Issue 5 Pg. 460-2 (Jun 1999) ISSN: 0032-0943 [Print] Germany
PMID	10418338 (Publication Type: Letter, Research Support, Non-U.S. Gov't)
Chemical References	Anti-Inflammatory Agents, Non-Steroidal Cyclooxygenase Inhibitors Isoenzymes Membrane Proteins Plant Extracts epiafzelechin Catechin Carrageenan Cyclooxygenase 1 Prostaglandin-Endoperoxide Synthases Ptgs1 protein, mouse
Topics	Animals Anti-Inflammatory Agents, Non-Steroidal (chemistry, isolation & purification, pharmacology) Carrageenan Catechin (analogs & derivatives, chemistry, isolation & purification, pharmacology) Cyclooxygenase 1 Cyclooxygenase Inhibitors (chemistry, isolation & purification, pharmacology) Edema (chemically induced, drug therapy) Isoenzymes (metabolism) Male Medicine, Chinese Traditional Membrane Proteins Mice Mice, Inbred ICR Molecular Structure Plant Extracts (chemistry, pharmacology) Plants, Medicinal Prostaglandin-Endoperoxide Synthases (metabolism)

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