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帕拉朵类似物的酰基链长度与其口服后的抗肥胖活性之间的关系。

Relationship between the acyl chain length of paradol analogues and their antiobesity activity following oral ingestion.

作者信息

Haratake Akinori, Watase Daisuke, Setoguchi Shuichi, Terada Kazuki, Matsunaga Kazuhisa, Takata Jiro

机构信息

Laboratory of Drug Design and Drug Delivery, Faculty of Pharmaceutical Sciences, Fukuoka University, 8-19-1 Nanakuma, Jonan-ku, Fukuoka 814-0180, Japan.

出版信息

J Agric Food Chem. 2014 Jul 2;62(26):6166-74. doi: 10.1021/jf500873a. Epub 2014 Jun 18.

DOI:10.1021/jf500873a
PMID:24909840
Abstract

6-Paradol is known to activate thermogenesis in brown adipose tissue (BAT), and paradol analogues with different acyl chain lengths possess different pungency thresholds. In this study, the influence of the acyl chain length on the antiobesity activity of the paradol analogues was investigated. The antiobesity activity of 6-paradol in mice fed a high-fat diet for 8 weeks was greater than that of dihydrocapsiate. A comparison of the antiobesity activities of zingerone and 6-paradol showed that the length of the acyl chain in the paradol analogue was important for strong activity. Furthermore, the antiobesity activities of 6-, 8-, and 12-paradol appeared to decrease in an acyl chain length-dependent manner. The mechanism of the antiobesity activity of 6-paradol was enhanced by increasing levels of energy metabolism in the BAT, as well as an increase in the expression of uncoupling proteins 1 via the activation of sympathetic nerve activity.

摘要

已知6-姜酚可激活棕色脂肪组织(BAT)中的产热作用,且不同酰基链长度的姜酚类似物具有不同的辛辣阈值。在本研究中,研究了酰基链长度对姜酚类似物抗肥胖活性的影响。在高脂饮食喂养8周的小鼠中,6-姜酚的抗肥胖活性大于二氢辣椒素。姜酮和6-姜酚抗肥胖活性的比较表明,姜酚类似物中酰基链的长度对强活性很重要。此外,6-、8-和12-姜酚的抗肥胖活性似乎以酰基链长度依赖性方式降低。6-姜酚抗肥胖活性的机制是通过增加BAT中的能量代谢水平,以及通过激活交感神经活动增加解偶联蛋白1的表达来增强的。

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