Programa de Iniciação Científica da Faculdade de Zootecnia e Engenharia de Alimentos, Universidade de São Paulo, Av. Duque de Caxias Norte, 225, Pirassununga, SP 13635-900, Brazil.
Food Chem. 2013 Dec 1;141(3):2253-62. doi: 10.1016/j.foodchem.2013.05.025. Epub 2013 May 18.
Fisetin, quercetin, luteolin and 7,8-hydroxyflavone show high activity in Leishmania cultures and present low toxicity to mammalian cells. In this work, the structural aspects of 13 flavonoids were analyzed for their inhibition of the arginase enzyme from Leishmania (Leishmania) amazonensis. A higher potency of arginase inhibition was observed with fisetin, which was four and ten times greater than that of quercetin and luteolin, respectively. These data show that the hydroxyl group at position 3 contributed significantly to the inhibitory activity of arginase, while the hydroxyl group at position 5 did not. The absence of the catechol group on apigenin drastically decreased arginase inhibition. Additionally, the docking of compounds showed that the inhibitors interact with amino acids involved in the Mn(+2)-Mn(+2) metal bridge formation at the catalytic site. Due to the low IC50 values of these flavonoids, they may be used as a food supplement in leishmaniasis treatment.
漆黄素、槲皮素、木樨草素和 7,8-二羟基黄酮在利什曼原虫培养物中表现出高活性，并且对哺乳动物细胞的毒性低。在这项工作中，分析了 13 种类黄酮的结构方面，以研究它们对亚马逊利什曼原虫（Leishmania）（Leishmania）精氨酸酶的抑制作用。漆黄素对精氨酸酶的抑制作用更强，其抑制活性分别是槲皮素和木樨草素的四倍和十倍。这些数据表明，位置 3 的羟基基团对精氨酸酶的抑制活性有很大贡献，而位置 5 的羟基基团则没有。芹菜素中儿茶酚基团的缺失大大降低了精氨酸酶的抑制作用。此外，化合物的对接表明，抑制剂与催化部位 Mn(+2)-Mn(+2)金属桥形成中涉及的氨基酸相互作用。由于这些类黄酮的 IC50 值较低，它们可能被用作治疗利什曼病的食品补充剂。
