Abstract
During routine screening of medicinal plants for small molecular weight inhibitors of cell adhesion, the crude ethanolic extract of the anti-rheumatic herbal drug gravel root (rhizome of Eupatorium purpureum), was identified as a potent inhibitor of some β1 and β2 integrin-mediated cell adhesions. The active principle of gravel root has now been isolated and identified as 5-acetyl-6-hydroxy-2,3-dihydro-cis-2-isopropenyl-3-tiglinoyloxybenzofuran (1). Compound 1 inhibited integrindependent cell-cell and cell-protein interactions in vitro with EC50 values between 7-20 µg/ml. As with indomethacin, 1 administered orally two hours before induction of inflammation (in rat paw) by carrageenan inhibited oedema formation in a dose (10 and 50 mg/kg)-dependent manner. It appears that 1 has therapeutic potential for diseases where integrin adhesion molecules play a significant role.

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