Inhibition of polymorphonuclear leukocyte 5-lipoxygenase and platelet cyclooxygenase by .ALPHA.-(3,5-di-tert-butyl-4-hydroxybenzylidene)-.GAMMA.-butyrolactone (KME-4), a new anti-inflammatory drug.
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概要
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The effect of α-(3, 5-di-tert-butyl-4-hydroxybenzylidene)-γ-butyrolactone (KME-4), a new anti-inflammatory compound, on arachidonate lipoxygenase and cyclooxygenase was investigated. KME-4 showed a dose-dependent inhibition of 5-lipoxygenase activity in both the cytosol (IC50: 0.85 μM) and ionophore A23187-stimulated cells (IC50: 11.5 μM) of guinea pig peritoneal polymorphonuclear leukocytes. KME-4 was also found to inhibit rabbit platelet cyclooxygenase (IC50: 0.44 μM), but had no inhibitory effect on platelet 12-lipoxygenase at concentrations up to 100 μM, whereas BW755C inhibited both enzymes in the same range of concentrations. The results indicate that KME-4 is a dual 5-lipoxygenase and cyclooxygenase inhibitor which is different from BW755C in affecting 1 2-lipoxygenase. These effects may provide information for understanding the pharmacological activity of KME-4.
- 公益社団法人 日本薬理学会の論文
著者
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WATANABE Kiyoshi
Biochemical Research Laboratories, Kanegafuchi Chemical Industry Co., Ltd.
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Watanabe Kiyoshi
Biochemical Research Laboratories Kanegafuchi Chemical Industry Co. Ltd.
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Yamashita Toshiaki
Biochemical Research Laboratories Kanegafuchi Chemical Industry Co. Ltd.
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Takeo Kazuyuki
Biochemical Research Laboratories Kanegafuchi Chemical Industry Co. Ltd.
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HIDAKA Takayoshi
Biochemical Research Laboratories, Kanegafuchi Chemical Industry Co., Ltd.
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HOSOE Kazunori
Biochemical Research Laboratories, Kanegafuchi Chemical Industry Co., Ltd.
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KATSUMI Ikuo
Biochemical Research Laboratories, Kanegafuchi Chemical Industry Co., Ltd.
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