Anacardic acid derived salicylates are inhibitors or activators of lipoxygenases.

Article Details

Citation

Copy to clipboard

Wisastra R, Ghizzoni M, Boltjes A, Haisma HJ, Dekker FJ

Anacardic acid derived salicylates are inhibitors or activators of lipoxygenases.

Bioorg Med Chem. 2012 Aug 15;20(16):5027-32. doi: 10.1016/j.bmc.2012.06.019. Epub 2012 Jun 21.

PubMed ID

22789707 [ View in PubMed

]

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 muM, 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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Zileuton	Arachidonate 5-lipoxygenase	IC 50 (nM)	500	N/A	N/A	Details