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首页> 外文期刊>Life sciences >Induction of adiponectin by natural and synthetic phenolamides in mouse and human preadipocytes and its enhancement by docosahexaenoic acid
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Induction of adiponectin by natural and synthetic phenolamides in mouse and human preadipocytes and its enhancement by docosahexaenoic acid

机译：天然和合成酚酰胺在小鼠和人类前脂肪细胞中诱导脂联素的作用及其二十二碳六烯酸的增强作用

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Adiponectin, the adipose-derived cytokine, plays an important role in preventing metabolic syndromes. To develop new adiponectin inducers, eight species of ferulic esters and amides, and five related compounds were synthesized and tested on the stimulation of adiponectin production in mouse 3T3-L1 and normal human preadipocytes. The ferulamides with an aromatic ring in the N-substituent are very active in inducing adiponectin as compared with the known active compounds, curcumin, [6]-gingerol, and capsaicin, and furthermore the activities of these ferulamides are remarkably stronger than those of the corresponding esters or the straight chain octylamide. The most active compound, N-(2-phenylethyl)ferulamide (7), was found to activate the PPAR (peroxisome proliferator-activated receptor) gamma-RXR (retinoid X receptor) alpha heterodimeric complex in the PPRE (PPAR-responsive element)-driven luciferase reporter assay. The adiponectin production by 7 is synergistically enhanced by coaddition of a PPAR-gamma-specific agonist, pioglitazone (PGZ), or another PPAR gamma agonist, docosahexaenoic acid (DRA), in cultured preadipocytes. The compound 7 alone did not show a statistically significant effect on the plasma adiponectin level in KK-A(y)/Ta mice, while 1% 7 in the diets significantly lowered the blood glucose and triglyceride levels and 0.3% 7 mixed with DHA oil in the diets significantly increased the adiponectin level as compared with the control. These results suggest that the present ferulamides would be useful lead compounds in developing more potent agents for treatment of metabolic syndromes through promoting the endogenous adiponectin production, and that such an activity is possibly enhanced by the coadministration with DHA. (C) 2007 Elsevier Inc. All rights reserved.
机译：脂联素是脂肪细胞因子，在预防代谢综合征中起着重要作用。为了开发新的脂联素诱导剂，合成了八种阿魏酸酯和酰胺以及五种相关化合物，并测试了其对小鼠3T3-L1和正常人前脂肪细胞中脂联素产生的刺激作用。与已知的活性化合物姜黄素，[6]-姜油醇和辣椒素相比，在N取代基中带有芳香环的阿魏酰胺对脂联素的诱导非常有效，而且这些阿魏酰胺的活性明显强于相应的酯或直链辛酰胺。发现活性最高的化合物N-（2-苯乙基）阿魏酰胺（7）可以激活PPRE（PPAR响应元件）中的PPAR（过氧化物酶体增殖物激活受体）γ-RXR（类维生素X受体）α异二聚体复合物。驱动的荧光素酶报告基因分析。通过在培养的前脂肪细胞中共添加PPAR-γ特异性激动剂吡格列酮（PGZ）或另一种PPARγ激动剂二十二碳六烯酸（DRA）可以协同提高脂联素的产量。单独的化合物7对KK-A（y）/ Ta小鼠的血浆脂联素水平没有统计学上的显着影响，而饮食中的1％7显着降低了血糖和甘油三酸酯水平，而与DHA油混合则降低了0.3％7与对照组相比，日粮中的脂联素水平显着增加。这些结果表明，本发明的阿魏酰胺在通过促进内源性脂联素产生而开发用于治疗代谢综合症的更有效的药物中将是有用的先导化合物，并且这种活性可能通过与DHA共同施用而增强。 （C）2007 Elsevier Inc.保留所有权利。

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