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Inhibition of 5-lipoxygenase activity by the natural anti-inflammatory compound aethiopinone
R Benrezzouk1, M C Terencio, M L Ferrandiz
1Department of Pharmacology, University of Valencia, Faculty of Pharmacy, Spain.
Objective And Design:
We have investigated the mechanisms of action of aethiopinone, an anti-inflammatory compound from Salvia aethiopis L. roots.
Material And Subjects:
Human neutrophils from healthy volunteers and murine peritoneal macrophages. Swiss mice were randomly divided into groups of six animals.
Treatment:
Test compounds were applied topically in the mouse ear oedema test. In the air pouch, mice received aethiopinone (0.001-0.5 pmol/pouch or 12.5-50 mg/kg p.o.).
Methods:
LTB4 production was assayed in human neutrophils and COX-2 and iNOS activities in murine macrophages. Air pouches were induced subcutaneously in mice and injected with zymosan on the day six. Mouse ear oedema was induced by arachidonic acid. Dunnett's t-test was employed for statistical analysis.
Results:
We have observed potent inhibitory effects on human neutrophil LTB4 production without effects on COX or NOS activities. Aethiopinone is an in vitro inhibitor of 5-LO from human neutrophils (IC50 = 0.11 microM). In addition, aethiopinone reduced leukocyte accumulation and showed in vivo inhibitory activity on this enzyme.
Conclusions:
Our results indicate that inhibition of 5-LO could participate in the anti-inflammatory properties of this natural product.
