Department of Biochemistry and Biotechnology, University of Thessaly, Larissa, Greece.
PLoS One. 2012;7(3):e32214. doi: 10.1371/journal.pone.0032214. Epub 2012 Mar 2.
Legumes and the polyphenolic compounds present in them have gained a lot of interest due to their beneficial health implications. Dietary polyphenolic compounds, especially flavonoids, exert antioxidant properties and are potent inhibitors of xanthine oxidase (XO) activity. XO is the main contributor of free radicals during exercise but it is also involved in pathogenesis of several diseases such as vascular disorders, cancer and gout. In order to discover new natural, dietary XO inhibitors, some polyphenolic fractions and pure compounds isolated from two legume plant extracts were tested for their effects on XO activity. The fractions isolated from both Vicia faba and Lotus edulis plant extracts were potent inhibitors of XO with IC(50) values range from 40-135 µg/mL and 55-260 µg/mL, respectively. All the pure polyphenolic compounds inhibited XO and their K(i) values ranged from 13-767 µM. Ten of the compounds followed the non competitive inhibitory model whereas one of them was a competitive inhibitor. These findings indicate that flavonoid isolates from legume plant extracts are novel, natural XO inhibitors. Their mode of action is under investigation in order to examine their potential in drug design for diseases related to overwhelming XO action.
豆类及其所含有的多酚化合物因其对健康的有益影响而备受关注。膳食多酚化合物，尤其是类黄酮，具有抗氧化特性，是黄嘌呤氧化酶 (XO) 活性的有效抑制剂。XO 是运动过程中自由基的主要来源，但它也参与了多种疾病的发病机制，如血管疾病、癌症和痛风。为了发现新的天然、膳食 XO 抑制剂，从两种豆类植物提取物中分离出的一些多酚类化合物进行了测试，以评估它们对 XO 活性的影响。从 Vicia faba 和 Lotus edulis 植物提取物中分离出的级分对 XO 具有很强的抑制作用，IC50 值范围分别为 40-135 µg/mL 和 55-260 µg/mL。所有的纯多酚化合物都抑制了 XO，其 K(i) 值范围为 13-767 µM。其中 10 种化合物遵循非竞争性抑制模型，而有一种化合物是竞争性抑制剂。这些发现表明，豆类植物提取物中的类黄酮分离物是新型的天然 XO 抑制剂。正在研究它们的作用方式，以检验它们在针对与 XO 作用过度相关的疾病的药物设计中的潜力。
