Homoisoflavonoids Are Potent Glucose Transporter 2 (GLUT2) Inhibitors: A Potential Mechanism for the Glucose-Lowering Properties of Polygonatum odoratum,Journal of Agricultural and Food Chemistry

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Homoisoflavonoids Are Potent Glucose Transporter 2 (GLUT2) Inhibitors: A Potential Mechanism for the Glucose-Lowering Properties of Polygonatum odoratum
Journal of Agricultural and Food Chemistry ( IF 5.7 ) Pub Date : 2018-03-13 00:00:00 , DOI: 10.1021/acs.jafc.8b00107
Huijun Wang _{1,

2,

3} , Mark I. Fowler ₂ , David J. Messenger ₂ , Leon A. Terry ₄ , Xuelan Gu ₅ , Luxian Zhou ₅ , Ruimin Liu ₁ , Juan Su ₁ , Songshan Shi ₁ , Jose Juan Ordaz-Ortiz ₆ , Guoping Lian ₂ , Mark J. Berry ₂ , Shunchun Wang ₁

Affiliation

Foods of high carbohydrate content such as sucrose or starch increase postprandial blood glucose concentrations. The glucose absorption system in the intestine comprises two components: sodium-dependent glucose transporter-1 (SGLT1) and glucose transporter 2 (GLUT2). Here five sappanin-type (SAP) homoisoflavonoids were identified as novel potent GLUT2 inhibitors, with three of them isolated from the fibrous roots of Polygonatum odoratum (Mill.) Druce. SAP homoisolflavonoids had a stronger inhibitory effect on 25 mM glucose transport (41.6 ± 2.5, 50.5 ± 7.6, 47.5 ± 1.9, 42.6 ± 2.4, and 45.7 ± 4.1% for EA-1, EA-2, EA-3, MOA, and MOB) than flavonoids (19.3 ± 2.2, 11.5 ± 3.7, 16.4 ± 2.4, 5.3 ± 1.0, 3.7 ± 2.2, and 18.1 ± 2.4% for apigenin, luteolin, quercetin, naringenin, hesperetin, and genistein) and phloretin (28.1 ± 1.6%) at 15 μM. SAP homoisoflavonoids and SGLT1 inhibitors were found to synergistically inhibit the uptake of glucose using an in vitro model comprising Caco-2 cells. This observed new mechanism of the glucose-lowering action of P. odoratum suggests that SAP homoisoflavonoids and their combination with flavonoid monoglucosides show promise as naturally functional ingredients for inclusion in foods and drinks designed to control postprandial glucose levels.

中文翻译：

同型类黄酮是有效的葡萄糖转运蛋白2（GLUT2）抑制剂：玉竹降糖特性的潜在机制

碳水化合物含量高的食物（例如蔗糖或淀粉）会增加餐后血糖浓度。肠道中的葡萄糖吸收系统包括两个组件：钠依赖性葡萄糖转运蛋白1（SGLT1）和葡萄糖转运蛋白2（GLUT2）。在这里，确定了五种sappanin型（SAP）同型异黄酮类化合物是新型有效的GLUT2抑制剂，其中三种是从玉竹的纤维根中分离出来的。（米尔）SAP同型异黄酮类化合物对25 mM葡萄糖转运具有更强的抑制作用（EA-1，EA-2，EA-3，MOA和EA-1分别为41.6±2.5、50.5±7.6、47.5±1.9、42.6±2.4和45.7±4.1％）芹菜素，木犀草素，槲皮素，柚皮素，橙皮素和染料木黄酮的类黄酮（19.3±2.2、11.5±3.7、16.4±2.4、5.3±1.0、3.7±2.2和18.1±2.4％）和促黄体素（28.1±1.6）％）在15μM下。使用包含Caco-2细胞的体外模型，发现SAP同型异黄酮和SGLT1抑制剂可协同抑制葡萄糖的摄取。这观察到了香雪茄降糖作用的新机制。提示SAP异黄酮类化合物及其与类黄酮单糖苷的组合显示出有望作为天然功能成分包含在旨在控制餐后血糖水平的食品和饮料中。

更新日期：2018-03-13

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