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Planta Med. 1998 Dec;64(8):683-5.

Cistifolin, an integrin-dependent cell adhesion blocker from the anti-rheumatic herbal drug, gravel root (rhizome of Eupatorium purpureum).

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1
Department of Physiology and Pharmacology, University of Strathclyde, U.K.

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 beta 1 and beta 2 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 integrin-dependent cell-cell and cell-protein interactions in vitro with EC50 values between 7-20 micrograms/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.

PMID:
10075543
DOI:
10.1055/s-2006-957558
[Indexed for MEDLINE]

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