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高异黄酮类化合物是有效的葡萄糖转运蛋白2(GLUT2)抑制剂:玉竹降血糖特性的一种潜在机制。

Homoisoflavonoids Are Potent Glucose Transporter 2 (GLUT2) Inhibitors: A Potential Mechanism for the Glucose-Lowering Properties of Polygonatum odoratum.

作者信息

Wang Huijun, Fowler Mark I, Messenger David J, Terry Leon A, Gu Xuelan, Zhou Luxian, Liu Ruimin, Su Juan, Shi Songshan, Ordaz-Ortiz Jose Juan, Lian Guoping, Berry Mark J, Wang Shunchun

机构信息

The MOE Key Laboratory for Standardization of Chinese Medicines and the SATCM Key Laboratory for New Resources and Quality Evaluation of Chinese Medicines, Institute of Chinese Materia Medica , Shanghai University of Traditional Chinese Medicine , 1200 Cailun Road , Shanghai 201203 , P. R. China.

Unilever R&D Colworth , Colworth Science Park , Sharnbrook, Bedford MK44 1LQ , United Kingdom.

出版信息

J Agric Food Chem. 2018 Mar 28;66(12):3137-3145. doi: 10.1021/acs.jafc.8b00107. Epub 2018 Mar 19.

DOI:10.1021/acs.jafc.8b00107
PMID:29533635
Abstract

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.

摘要

高碳水化合物含量的食物,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由两个部分组成:钠依赖性葡萄糖转运蛋白1(SGLT1)和葡萄糖转运蛋白2(GLUT2)。在此,五种山奈酚型(SAP)同型异黄酮被鉴定为新型强效GLUT2抑制剂,其中三种是从玉竹(Polygonatum odoratum (Mill.) Druce)的须根中分离得到的。在15μM浓度下,SAP同型异黄酮对25mM葡萄糖转运的抑制作用(EA - 1、EA - 2、EA - 3、MOA和MOB分别为41.6±2.5、50.5±7.6、47.5±1.9、42.6±2.4和45.7±4.1%)强于黄酮类化合物(芹菜素、木犀草素、槲皮素、柚皮素、橙皮素和染料木黄酮分别为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%)和根皮素(28.1±1.6%)。使用包含Caco - 2细胞的体外模型发现,SAP同型异黄酮和SGLT1抑制剂能协同抑制葡萄糖的摄取。玉竹这种新观察到的降血糖作用机制表明,SAP同型异黄酮及其与黄酮类单糖苷的组合有望作为天然功能性成分,用于控制餐后血糖水平的食品和饮料中。

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