Department of Food Science and Nutrition, Hallym University, Chuncheon 200-702, Republic of Korea.
Biomed Res Int. 2013;2013:727143. doi: 10.1155/2013/727143. Epub 2013 Mar 17.
Aldose reductase (AR) inhibitors have a considerable therapeutic potential against diabetes complications and do not increase the risk of hypoglycemia. Through bioassay-guided fractionation of an EtOH extract of the kernel from purple corn (Zea mays L.), 7 nonanthocyanin phenolic compounds (compound 1-7) and 5 anthocyanins (compound 8-12) were isolated. These compounds were investigated by rat lens aldose reductase (RLAR) inhibitory assays. Kinetic analyses of recombinant human aldose reductase (rhAR) were performed, and intracellular galactitol levels were measured. Hirsutrin, one of 12 isolated compounds, showed the most potent RLAR inhibitory activity (IC(50), 4.78 μ M). In the kinetic analyses using Lineweaver-Burk plots of 1/velocity and 1/substrate concentration, hirsutrin showed competitive inhibition against rhAR. Furthermore, hirsutrin inhibited galactitol formation in rat lens and erythrocytes sample incubated with a high concentration of galactose; this finding indicates that hirsutrin may effectively prevent osmotic stress in hyperglycemia. Therefore, hirsutrin derived from Zea mays L. may be a potential therapeutic agent against diabetes complications.
醛糖还原酶(AR)抑制剂在治疗糖尿病并发症方面具有很大的潜力,并且不会增加低血糖的风险。通过对紫玉米(Zea mays L.)果仁的乙醇提取物进行生物活性导向分离,分离得到了 7 种非花青素类酚类化合物(化合物 1-7)和 5 种花青素类化合物(化合物 8-12)。这些化合物通过大鼠晶状体醛糖还原酶(RLAR)抑制试验进行了研究。对重组人醛糖还原酶(rhAR)进行了动力学分析,并测量了细胞内半乳糖醇水平。12 种分离得到的化合物之一,毛蕊花糖苷,表现出最强的 RLAR 抑制活性(IC50,4.78 μM)。在使用 Lineweaver-Burk 图的 1/速度和 1/底物浓度的动力学分析中,毛蕊花糖苷对 rhAR 表现出竞争性抑制。此外,毛蕊花糖苷抑制了高浓度半乳糖孵育的大鼠晶状体和红细胞样本中半乳糖醇的形成;这一发现表明,毛蕊花糖苷可能有效预防高血糖引起的渗透应激。因此,来源于 Zea mays L.的毛蕊花糖苷可能是一种治疗糖尿病并发症的潜在治疗剂。