Suzuki H, Ueda T, Juránek I, Yamamoto S, Katoh T, Node M, Suzuki T
Department of Biochemistry, Tokushima University School of Medicine, Kuramoto-cho, Tokushima, 770-8503, Japan.
Biochem Biophys Res Commun. 2000 Sep 7;275(3):885-9. doi: 10.1006/bbrc.2000.3390.
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.
扁柏酚（4-异丙基环庚三烯酚酮）是日本扁柏的一种成分，它以0.1微摩尔的半数抑制浓度可逆地抑制血小板型12-脂氧合酶，在1微摩尔时酶活性几乎完全丧失。该化合物对其他脂氧合酶的活性要低得多，半数抑制浓度更高（白细胞型12-脂氧合酶，50微摩尔；大豆脂氧合酶，17微摩尔；15-脂氧合酶-1，大于100微摩尔；5-脂氧合酶，17微摩尔）。高达100微摩尔的扁柏酚对环氧化酶-1和-2几乎没有影响。用各种环庚三烯酚酮衍生物研究它们的构效关系表明，2-羟基和4-烷基对于有效和选择性抑制血小板型12-脂氧合酶是必需的。
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