Kotowska Dorota, El-Houri Rime B, Borkowski Kamil, Petersen Rasmus K, Fretté Xavier C, Wolber Gerhard, Grevsen Kai, Christensen Kathrine B, Christensen Lars P, Kristiansen Karsten
Department of Biology, University of Copenhagen, Copenhagen, Denmark.
Department of Chemical Engineering, Biotechnology and Environmental Technology, University of Southern Denmark, Odense, Denmark.
Planta Med. 2014 Dec;80(18):1712-20. doi: 10.1055/s-0034-1383252. Epub 2014 Nov 5.
Echinacea purpurea has been used in traditional medicine as a remedy for the treatment and prevention of upper respiratory tract infections and the common cold. Recent investigations have indicated that E. purpurea also has an effect on insulin resistance. A dichloromethane extract of E. purpurea roots was found to enhance glucose uptake in adipocytes and to activate peroxisome proliferator-activated receptor γ. The purpose of the present study was to identify the bioactive compounds responsible for the potential antidiabetic effect of the dichloromethane extract using a bioassay-guided fractionation approach. Basal and insulin-dependent glucose uptake in 3T3-L1 adipocytes were used to assess the bioactivity of extract, fractions and isolated metabolites. A peroxisome proliferator-activated receptor γ transactivation assay was used to determine the peroxisome proliferator-activated receptor γ activating properties of the extract, active fractions and isolated metabolites. Two novel isomeric dodeca-2E,4E,8Z,10E/Z-tetraenoic acid 2-methylbutylamides together with two known C12-alkamides and α-linolenic acid were isolated from the active fractions. The isomeric C12-alkamides were found to activate peroxisome proliferator-activated receptor γ, to increase basal and insulin-dependent glucose uptake in adipocytes in a dose-dependent manner, and to exhibit characteristics of a peroxisome proliferator-activated receptor γ partial agonist.
紫锥菊在传统医学中一直被用作治疗和预防上呼吸道感染及普通感冒的药物。最近的研究表明，紫锥菊对胰岛素抵抗也有影响。紫锥菊根的二氯甲烷提取物被发现可增强脂肪细胞对葡萄糖的摄取，并激活过氧化物酶体增殖物激活受体γ。本研究的目的是使用生物测定导向的分级分离方法，鉴定负责二氯甲烷提取物潜在抗糖尿病作用的生物活性化合物。利用3T3-L1脂肪细胞中的基础和胰岛素依赖性葡萄糖摄取来评估提取物、馏分和分离代谢物的生物活性。使用过氧化物酶体增殖物激活受体γ反式激活测定法来确定提取物、活性馏分和分离代谢物的过氧化物酶体增殖物激活受体γ激活特性。从活性馏分中分离出两种新型的异构体十二碳-2E,4E,8Z,10E/Z-四烯酸2-甲基丁酰胺，以及两种已知的C12-链烷酰胺和α-亚麻酸。发现异构体C12-链烷酰胺可激活过氧化物酶体增殖物激活受体γ，以剂量依赖性方式增加脂肪细胞中基础和胰岛素依赖性葡萄糖摄取，并表现出过氧化物酶体增殖物激活受体γ部分激动剂的特征。
