Flavonoid derivative exerts an antidiabetic effect via AMPK activation in diet-induced obesity mice
Flavonoid derivative exerts an antidiabetic effect via AMPK activation in diet-induced obesity mice
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类黄酮衍生物通过 AMPK 激活在饮食诱导的肥胖小鼠中发挥抗糖尿病作用
DOI：
10.1080/14786419.2015.1101105
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发表时间：
2016-01-01
影响因子：
2.2
通讯作者：
Niu, Wen-Yan
中科院分区：
文献类型：
--
作者：
Chen, Ying;Zhang, Chang;Niu, Wen-Yan
在我们之前的研究中，铁力苷衍生物3-O-[(E)-4-（4-乙氧基苯基）-2-氧丁-3-烯-1-基]山奈酚（Fla-OEt）显著提高胰岛素抵抗HepG2细胞的葡萄糖消耗。本文研究了黄酮黄酮对饮食性肥胖（DIO）小鼠的降血糖和降血脂作用。每日给予Fla-OEt可显著降低口服葡萄糖耐量试验、腹腔胰岛素耐量试验和血脂。与高脂饮食（HFD）组相比，高胰岛素-正糖钳位和高密度脂蛋白/低密度脂蛋白比值升高，脂质代谢得到改善。组织病理学检查显示，黄酮可恢复DIO小鼠脂肪组织和肝脏的损伤。此外，与HFD组相比，Fla-OEt处理显著增加了脂肪组织、肝脏和肌肉中AMPK和ACC的磷酸化。其作用机制可能是激活AMPK通路。Fla-OEt作为一种潜在的抗糖尿病药物的先导化合物值得进一步研究。
In our previous study, a derivative of tiliroside, 3-O-[(E)-4-(4-ethoxyphenyl)-2-oxobut-3-en-1-yl]kaempferol (Fla-OEt) significantly enhanced glucose consumption in insulin resistant HepG2 cells. This article deals with the antihyperglycemic and antihyperlipidemic effects of Fla-OEt in diet-induced obesity (DIO) mice. Daily administration of Fla-OEt significantly decreased oral glucose tolerance test, intraperitoneal insulin tolerance test and serum lipids. Hyperinsulinemic-euglycemic clamp and the ratio of high-density-lipoprotein/low-density-lipoprotein with Fla-OEt treatment were increased comparing with high-fat diet (HFD) group, so lipid metabolism was improved. Histopathology examination showed that the Fla-OEt restored the damage of adipose tissues and liver in DIO mice. Moreover, compared with HFD group, Fla-OEt treatment significantly increased the phosphorylation of AMPK and ACC in adiposity tissues, liver, and muscles. The mechanism of its action might be the activation of AMPK pathway. It appears that Fla-OEt is worth further study for development as a lead compound for a potential antidiabetic agent.[GRAPHICS].