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查尔酮衍生物对小鼠表皮脂氧合酶和环氧化酶活性的影响。

Effects of chalcone derivatives on lipoxygenase and cyclooxygenase activities of mouse epidermis.

作者信息

Nakadate T, Aizu E, Yamamoto S, Kato R

出版信息

Prostaglandins. 1985 Sep;30(3):357-68. doi: 10.1016/0090-6980(85)90112-1.

Abstract

The effects of chalcone derivatives on 12-lipoxygenase and cyclooxygenase of mouse epidermis were investigated. The chalcone derivatives which have 3,4-dihydroxycinnamoyl structure in the molecule, such as 3,4-dihydroxychalcone, 3,4,2'-trihydroxychalcone, 3,4,4'-trihydroxychalcone and 3,4,2'4'-tetrahydroxychalcone, potently inhibited epidermal 12-lipoxygenase activity. Although some of them also inhibited cyclooxygenase activity at relatively high concentrations, the inhibitory effects of these chalcone derivatives on 12-lipoxygenase were 10 times or more potent than their effects on cyclooxygenase. The chalcone derivatives which have cinnamoyl or 4-hydroxycinnamoyl structure, instead of 3,4-dihydroxycinnamoyl structure, in the molecule, showed little or no inhibitory effects on either 12-lipoxygenase or cyclooxygenase activities. The inhibitory effects of chalcone derivatives on 12-lipoxygenase and cyclooxygenase of mouse epidermis are dependent on the particular structure, i.e. 3,4-dihydroxycinnamoyl structure, of the chalcone derivatives.

摘要

研究了查尔酮衍生物对小鼠表皮12-脂氧合酶和环氧化酶的影响。分子中具有3,4-二羟基肉桂酰结构的查尔酮衍生物,如3,4-二羟基查尔酮、3,4,2'-三羟基查尔酮、3,4,4'-三羟基查尔酮和3,4,2'4'-四羟基查尔酮,能有效抑制表皮12-脂氧合酶活性。虽然其中一些在相对高浓度时也抑制环氧化酶活性,但这些查尔酮衍生物对12-脂氧合酶的抑制作用比对环氧化酶的作用强10倍或更多。分子中具有肉桂酰或4-羟基肉桂酰结构而非3,4-二羟基肉桂酰结构的查尔酮衍生物,对12-脂氧合酶或环氧化酶活性几乎没有抑制作用。查尔酮衍生物对小鼠表皮12-脂氧合酶和环氧化酶的抑制作用取决于查尔酮衍生物的特定结构,即3,4-二羟基肉桂酰结构。

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