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Evaluation of Hyperforin Analogues for Inhibition of 5-lipoxygenase

[ Vol. 1 , Issue. 3 ]


Christian Feißt, Dana Albert, Luisella Verotta and Oliver Werz   Pages 287 - 291 ( 5 )


The acylphloroglucinol hyperforin, a constituent of the herb Hypericum perforatum (St. Johns wort), was recently identified as potent and direct inhibitor of 5-lipoxygenase (5-LO), the key enzyme in the biosynthesis of proinflammatory leukotrienes. In this study, naturally occurring analogues of hyperforin, isolated from H. perforatum, as well as a series of synthetic derivatives obtained by chemical modification of hyperforin by acylation, alkylation or oxidation, were analysed for the inhibition of 5-LO. The efficacies of these compounds were evaluated in intact human polymorphonuclear leukocytes, but also the inhibitory effects on isolated recombinant human 5-LO were investigated. Our data show that some of the oxidised hyperforin derivatives possess even improved efficacy, whereas alkylation and acylation have detrimental effects.


hyperforin, hypericum perforatum, 5-lipoxygenase, leukotriene, inflammation, polymorphonuclear leukocyte.


Institute of Pharmaceutical Chemistry, University of Frankfurt, Marie-Curie-Str. 9, D-60439 Frankfurt,Germany.

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