Antithrombotic Action of the Kava Pyrone (+)-Kavain Prepared fromPiper methysticumon Human Platelets*
- 1 February 1997
- journal article
- research article
- Published by Georg Thieme Verlag KG in Planta Medica
- Vol. 63 (01) , 27-30
- https://doi.org/10.1055/s-2006-957597
Abstract
(+)-Kavain, a 4-methoxy-α-pyrone prepared from Piper methysticum Forst. (Piperaceae), was investigated regarding its assumed antithrombotic action on human platelets which was deduced from its ability to suppress arachidonic acid (AA)-induced aggregation, exocytosis of ATP, and inhibition of cyclooxygenase (COX) and thromboxane synthase (TXS) activity, the latter two effects being estimated from the generation of prostaglandin E2 (PGE2) and thromboxane A2 (TXA2), respectively. Exogenously applied AA (100 µmol/l) provoked a 90% aggregation of platelets, the release of 14pmol ATP, and the formation of either 220 pg TXA2 or 43 pg PGE2, each parameter being related to 106 platelets. An application of (+)-kavain 5 min before AA, dose-dependently diminished aggregation, ATP-release, and the synthesis of TXA2 and PGE2 with IC50 values of 78, 115, 71, and 86 µmol/l, respectively. The similarity of the IC50 values suggest an inhibition of COX by (+)-kavain as primary target, thus suppressing the generation of TXA2 which induces aggregation of platelets and exocytosis of ATP by its binding on TXA2-receptors.Keywords
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