Mirzoeva O K, Sud'ina G F, Pushkareva M A, Korshunova G A, Sumbatian N V, Varfolomeev S D
Bioorg Khim. 1995 Feb;21(2):143-51.
We have prepared two lipophilic derivatives of caffeic acid at the carboxylic function--caffeic acid phenethyl ester, an active component of propolis, and N,N'-dicyclohexyl-O-(3,4-dihydroxycinnamoyl)-isourea. Both substances inhibit barley 5-lipoxygenase and soybean 15-lipoxygenase at micromolar concentrations. The inhibition is uncompetitive, dose-dependent and reversible. The caffeic acid derivatives also exhibit antioxidant properties and at a concentration 5-10 microM completely block the production of the reactive oxygen species in human neutrophils and in the cell-free xanthine/xanthine oxidase system.
我们已在咖啡酸的羧基官能团处制备了两种亲脂性衍生物——蜂胶的活性成分咖啡酸苯乙酯，以及N,N'-二环己基-O-(3,4-二羟基肉桂酰基)-异脲。这两种物质在微摩尔浓度下均能抑制大麦5-脂氧合酶和大豆15-脂氧合酶。这种抑制是非竞争性的、剂量依赖性的且可逆的。咖啡酸衍生物还具有抗氧化特性，在5-10微摩尔的浓度下能完全阻断人类中性粒细胞和无细胞黄嘌呤/黄嘌呤氧化酶系统中活性氧的产生。
