Inhibition of human platelet cyclic AMP phosphodiesterase and of platelet aggregation by a hemisynthetic flavonoid, amentoflavone hexaacetate

作者: Alain Beretz , Françoise Briançon-Scheid , Anita Stierlé , Gilles Corre , Robert Anton

DOI: 10.1016/0006-2952(86)90523-X

关键词: PharmacologyHEPESMechanism of actionBiflavonoidAmentoflavoneBiochemistryChemistryPhosphodiesteraseProstaglandin EPlateletFlavonoid

摘要: Abstract Amentoflavone hexaacetate (AmAc) was synthesized from natural amentoflavone (Am), a biflavonoid extracted Viburnum lantana L. Am does not inhibit aggregation of intact platelets up to concentration 100 μM but inhibits human platelet cAMP phosphodiesterase ( ic 50 = 22.0 μ M ).AmAc is potent inhibitor the washed induced by ADP 2.3 ) or collagen 4.7 ). AmAc crude 8.6 partially purified 42,2 phosphodiesterase. In presence prostaglandin E1, (10 μM) induces 3.7-fold increase in total cAMP. The characteristics this action suggest role for mechanism AmAc. incubation with 5 min necessary its activity.

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