Hinokitiol, a Selective Inhibitor of the Platelet-Type Isozyme of Arachidonate 12-Lipoxygenase
Copyright policy )Hinokitiol, a Selective Inhibitor of the Platelet-Type Isozyme of Arachidonate 12-Lipoxygenase
Hinokitiol (4-isopropyltropolone), a constituent of Japanese cypress, reversibly inhibited platelet-type 12-lipoxygenase with an IC(50) of 0.1 microM, and the enzyme activity was almost lost at 1 microM. The compound was much less active with other lipoxygenase enzymes with higher IC(50) values (leukocyte-type 12-lipoxygenase, 50 microM; soybean lipoxygenase, 17 microM; 15-lipoxygenase-1, >100 microM; 5-lipoxygenase, 17 microM). Hinokitiol up to 100 microM had almost no effect on cyclooxygenases-1 and -2. Their structure-activity relationship examined with various tropolone derivatives indicated the requirements of the 2-hydroxyl group and 4-alkyl group for the potent and selective inhibition of platelet-type 12-lipoxygenase.
Blood Platelets, Time Factors, Membrane Proteins, Arachidonate 12-Lipoxygenase, Tropolone, Substrate Specificity, Trees, Isoenzymes, Inhibitory Concentration 50, Structure-Activity Relationship, Anti-Infective Agents, Cyclooxygenase 2, Prostaglandin-Endoperoxide Synthases, Cyclooxygenase 1, Leukocytes, Monoterpenes, Animals, Humans, Lipoxygenase Inhibitors, Enzyme Inhibitors
Blood Platelets, Time Factors, Membrane Proteins, Arachidonate 12-Lipoxygenase, Tropolone, Substrate Specificity, Trees, Isoenzymes, Inhibitory Concentration 50, Structure-Activity Relationship, Anti-Infective Agents, Cyclooxygenase 2, Prostaglandin-Endoperoxide Synthases, Cyclooxygenase 1, Leukocytes, Monoterpenes, Animals, Humans, Lipoxygenase Inhibitors, Enzyme Inhibitors
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