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  • Title: Anacardic acid derived salicylates are inhibitors or activators of lipoxygenases.
    Author: Wisastra R, Ghizzoni M, Boltjes A, Haisma HJ, Dekker FJ.
    Journal: Bioorg Med Chem; 2012 Aug 15; 20(16):5027-32. PubMed ID: 22789707.
    Abstract:
    Lipoxygenases catalyze the oxidation of unsaturated fatty acids, such as linoleic acid, which play a crucial role in inflammatory responses. Selective inhibitors may provide a new therapeutic approach for inflammatory diseases. In this study, we describe the identification of a novel soybean lipoxygenase-1 (SLO-1) inhibitor and a potato 5-lipoxygenase (5-LOX) activator from a screening of a focused compound collection around the natural product anacardic acid. The natural product anacardic acid inhibits SLO-1 with an IC(50) of 52 μM, whereas the inhibitory potency of the novel mixed type inhibitor 23 is fivefold enhanced. In addition, another derivative (21) caused non-essential activation of potato 5-LOX. This suggests the presence of an allosteric binding site that regulates the lipoxygenase activity.
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