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Hypoglycemic effect and mechanism of isoquercitrin as an inhibitor of dipeptidyl peptidase-4 in type 2 diabetic mice
RSC Advances ( IF 3.9 ) Pub Date : 2018-04-19 00:00:00 , DOI: 10.1039/c8ra00675j Lei Zhang 1, 2 , Shi-Tao Zhang 1 , Yan-Chun Yin 1 , Shu Xing 1 , Wan-Nan Li 1 , Xue-Qi Fu 1
RSC Advances ( IF 3.9 ) Pub Date : 2018-04-19 00:00:00 , DOI: 10.1039/c8ra00675j Lei Zhang 1, 2 , Shi-Tao Zhang 1 , Yan-Chun Yin 1 , Shu Xing 1 , Wan-Nan Li 1 , Xue-Qi Fu 1
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Glucagon-like peptide (GLP)-1 is a potent glucose-dependent insulinotropic gut hormone released from intestinal L cells. The aim of this study was to investigate isoquercitrin as an inhibitor of dipeptidyl peptidase IV (DPP-IV) and determine whether it affects GLP-1 release in normal mice and NCI-H716 cells. In vitro, we used chromogenic substrate method detection methods to measure DPP-IV. We found that isoquercitrin was a competitive inhibitor, with IC50 and Ki values of 96.8 and 236 μM, respectively. Isoquercitrin and sitagliptin also stimulated GLP-1 release in NCI-H716 cells. In vivo, a type 2 diabetic mouse model was established, and oral treatment with different concentration of isoquercitrin and sitagliptin for 8 weeks significantly decreased the fasting blood glucose level. The weight and the levels of serum GLP-1 and insulin of the mice in the isoquercitrin group were higher than those in the model group (P < 0.001). An oral glucose tolerance test showed that the isoquercitrin significantly inhibited postprandial blood glucose changes in a dose-dependent manner. These findings demonstrated the hypoglycemic effects of isoquercitrin and indicated that isoquercitrin improved insulin sensitivity by targeting DPP-IV.
中文翻译：
异槲皮苷作为二肽基肽酶4抑制剂对2型糖尿病小鼠的降血糖作用及机制
胰高血糖素样肽 (GLP)-1 是一种从肠道 L 细胞释放的有效的葡萄糖依赖性促胰岛素肠道激素。本研究的目的是研究异槲皮苷作为二肽基肽酶 IV (DPP-IV) 的抑制剂，并确定它是否影响正常小鼠和 NCI-H716 细胞中 GLP-1 的释放。在体外，我们采用显色底物法检测方法测定DPP-IV。我们发现异槲皮苷是一种竞争性抑制剂，IC 50和K i值分别为 96.8 和 236 μM。异槲皮苷和西格列汀也刺激 NCI-H716 细胞中 GLP-1 的释放。体内等，建立了2型糖尿病小鼠模型，口服不同浓度的异槲皮素和西格列汀8周后，空腹血糖水平显着降低。异槲皮苷组小鼠体重、血清GLP-1、胰岛素水平高于模型组（P < 0.001）。口服葡萄糖耐量试验表明，异槲皮苷以剂量依赖性方式显着抑制餐后血糖变化。这些发现证明了异槲皮苷的降血糖作用，并表明异槲皮苷通过靶向 DPP-IV 提高了胰岛素敏感性。
更新日期：2018-04-19
中文翻译：
异槲皮苷作为二肽基肽酶4抑制剂对2型糖尿病小鼠的降血糖作用及机制
胰高血糖素样肽 (GLP)-1 是一种从肠道 L 细胞释放的有效的葡萄糖依赖性促胰岛素肠道激素。本研究的目的是研究异槲皮苷作为二肽基肽酶 IV (DPP-IV) 的抑制剂，并确定它是否影响正常小鼠和 NCI-H716 细胞中 GLP-1 的释放。在体外，我们采用显色底物法检测方法测定DPP-IV。我们发现异槲皮苷是一种竞争性抑制剂，IC 50和K i值分别为 96.8 和 236 μM。异槲皮苷和西格列汀也刺激 NCI-H716 细胞中 GLP-1 的释放。体内等，建立了2型糖尿病小鼠模型，口服不同浓度的异槲皮素和西格列汀8周后，空腹血糖水平显着降低。异槲皮苷组小鼠体重、血清GLP-1、胰岛素水平高于模型组（P < 0.001）。口服葡萄糖耐量试验表明，异槲皮苷以剂量依赖性方式显着抑制餐后血糖变化。这些发现证明了异槲皮苷的降血糖作用，并表明异槲皮苷通过靶向 DPP-IV 提高了胰岛素敏感性。
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