Knaup Bastian, Oehme Anett, Valotis Anagnostis, Schreier Peter
Food Chemistry, University of Würzburg, Am Hubland, Würzburg, Germany.
Mol Nutr Food Res. 2009 May;53(5):617-24. doi: 10.1002/mnfr.200800234.
Health benefits associated with diets rich in anthocyanins are ascribed to multilevel biological activities including antioxidative and anti-inflammatory effects. The present study addresses lipoxygenase inhibition as a mechanism by which anthocyanins may exert health promoting effects. The inhibitory potential of delphinidin (Dp), cyanidin (Cy), peonidin (Pn), and malvidin (Mv) glycosides, i.e., 3-O-glucosides, 3-O-galactosides, and 3-O-arabinosides as well as their aglycons was analyzed by using soybean lipoxygenase-1 and human neutrophil granulocyte 5-lipoxygenase. The determined IC(50) values comprised a wide range, i.e., from the sub-microM level until practically no effect of inhibition (Mv and its glycosides). With IC(50) values of 0.43 and 0.49 microM Dp 3-O-glucoside (Dp3glc) and Dp 3-O-galactoside (Dp3gal) were found to be the most effective soybean lipoxygenase-1 inhibitors; their strong inhibitory potential was also reflected by the IC(50) values determined for these anthocyanins in the 5-lipoxygenase inhibition exhibiting 2.15 and 6.9 microM, respectively. As to the mechanism of inhibition, experiments carried out with lipoxygenase-1 revealed the uncompetitive type. Considering the powerful inhibitory properties of Dp glycosides in relation to their currently known availability in human metabolism, in vivo prevention of inflammatory diseases by these anthocyanins could be envisaged.
富含花青素的饮食对健康有益，这归因于其包括抗氧化和抗炎作用在内的多层次生物活性。本研究探讨了脂氧合酶抑制作用，这是花青素可能发挥健康促进作用的一种机制。通过使用大豆脂氧合酶 -1 和人中性粒细胞 5-脂氧合酶，分析了飞燕草素（Dp）、矢车菊素（Cy）、芍药色素（Pn）和锦葵色素（Mv）的糖苷（即 3 -O-葡萄糖苷、3 -O-半乳糖苷和 3 -O-阿拉伯糖苷）及其苷元的抑制潜力。所测定的半数抑制浓度（IC50）值范围很广，即从亚微摩尔水平到几乎没有抑制作用（Mv 及其糖苷）。Dp 3 -O-葡萄糖苷（Dp3glc）和 Dp 3 -O-半乳糖苷（Dp3gal）的 IC50 值分别为 0.43 和 0.49 微摩尔，被发现是最有效的大豆脂氧合酶 -1 抑制剂；它们在 5-脂氧合酶抑制实验中测定的 IC50 值分别为 2.15 和 6.9 微摩尔，也反映出其强大的抑制潜力。关于抑制机制，对脂氧合酶 -1 进行的实验显示为非竞争性类型。鉴于 Dp 糖苷相对于其目前已知在人体代谢中的可利用性具有强大的抑制特性，可以设想这些花青素在体内预防炎症性疾病的作用。
