Anacardic acid derived salicylates are inhibitors or activators of lipoxygenases
Copyright policy )Anacardic acid derived salicylates are inhibitors or activators of lipoxygenases
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.
- University of Groningen Netherlands
Glycine max, Enzyme activation, Lipoxygenase, Soybean lipoxygenase-1, Anacardic acid, Structure-Activity Relationship, INFLAMMATION, 5-LIPOXYGENASE, Lipoxygenase Inhibitors, Solanum tuberosum, Potato 5-LOX, Arachidonate 5-Lipoxygenase, Dose-Response Relationship, Drug, Molecular Structure, POTENT, OXYGENATION, LINOLEIC-ACID, Salicylates, Anacardic Acids, Enzyme Activation, Enzyme inhibition, 15-LIPOXYGENASE, SOYBEAN LIPOXYGENASE-1, ATHEROSCLEROSIS, FATTY-ACIDS, STEADY-STATE KINETICS
Glycine max, Enzyme activation, Lipoxygenase, Soybean lipoxygenase-1, Anacardic acid, Structure-Activity Relationship, INFLAMMATION, 5-LIPOXYGENASE, Lipoxygenase Inhibitors, Solanum tuberosum, Potato 5-LOX, Arachidonate 5-Lipoxygenase, Dose-Response Relationship, Drug, Molecular Structure, POTENT, OXYGENATION, LINOLEIC-ACID, Salicylates, Anacardic Acids, Enzyme Activation, Enzyme inhibition, 15-LIPOXYGENASE, SOYBEAN LIPOXYGENASE-1, ATHEROSCLEROSIS, FATTY-ACIDS, STEADY-STATE KINETICS
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