College of Veterinary Medicine , Hunan Agricultural University , Changsha 410128 , China.
Hunan Province University Key Laboratory for Agricultural Biochemistry and Biotransformation , Hunan Agricultural University , Changsha 410128 , China.
J Agric Food Chem. 2018 Aug 29;66(34):8983-8990. doi: 10.1021/acs.jafc.8b02696. Epub 2018 Aug 20.
Previous investigations have shown molecular cross-talk among activated adenosine monophosphate-activated protein kinase (AMPK), proprotein convertase subtilisin/kexin type 9 (PCSK9), sterol regulatory element-binding proteins (SREBPs), and low-density lipoprotein receptor (LDLR) and that it may be an innovative pharmacologic objective for treating obesity. We scrutinized the beneficial effect of naringin, a flavanone-7- O-glycoside, on obesity and the mechanisms in the present study. We arbitrarily divided 50 mice into five groups ( n = 10): 25 or 50 or 100 mg/kg/day naringin-treated obese mice (gavage for 8 weeks), untreated obese mice, and C57BL/6J control. After 8 weeks, body weight was 51.8 ± 4.4 in the untreated obese mice group, while the weights were 41.4 ± 4.1, 34.6 ± 2.2, and 28.0 ± 2.3 in 25, 50,100 mg/kg naringin groups, respectively. Moreover, naringin treatment significantly decreased plasma 8-isoprostane (an indicator of the oxidative stress) level, fat weight, liver weight, hepatic total cholesterol concentration, hepatic triglyceride concentration, plasma leptin level, plasma insulin content, plasma low-density lipoprotein cholesterol level, and plasma PCSK9 production concomitantly with down-regulated expression of SREBP-2, PCSK9, and SREBP-1, and up-regulated expression of p-AMPKα and LDLR. The present results suggest that naringin activates AMPK resulting in altered expression of SREBPs, PCSK9, and LDLR to reduce the body weight of obese C57BL/6J mice.
先前的研究表明,腺苷单磷酸激活蛋白激酶(AMPK)、脯氨酸内切酶枯草杆菌蛋白酶/凝血酶原 kexin 型 9(PCSK9)、固醇调节元件结合蛋白(SREBPs)和低密度脂蛋白受体(LDLR)之间存在分子串扰,这可能是治疗肥胖的创新药物靶点。本研究旨在探讨柚皮苷(一种黄烷酮-7-O-糖苷)对肥胖的有益作用及其机制。我们将 50 只小鼠任意分为 5 组(n=10):柚皮苷治疗肥胖组(灌胃 8 周,25、50 或 100mg/kg/d)、未治疗肥胖组和 C57BL/6J 对照组。8 周后,未治疗肥胖组小鼠体重为 51.8±4.4g,而 25、50、100mg/kg 柚皮苷组小鼠体重分别为 41.4±4.1、34.6±2.2 和 28.0±2.3g。此外,柚皮苷治疗可显著降低血浆 8-异前列腺素(氧化应激标志物)水平、脂肪重量、肝脏重量、肝总胆固醇浓度、肝甘油三酯浓度、血浆瘦素水平、血浆胰岛素含量、血浆低密度脂蛋白胆固醇水平和血浆 PCSK9 生成量,同时下调 SREBP-2、PCSK9 和 SREBP-1 的表达,并上调 p-AMPKα和 LDLR 的表达。本研究结果表明,柚皮苷激活 AMPK,改变 SREBPs、PCSK9 和 LDLR 的表达,从而降低肥胖 C57BL/6J 小鼠的体重。