Potent anti-obese principle from Rosa canina:: Structural requirements and mode of action of trans-tiliroside
Potent anti-obese principle from Rosa canina:: Structural requirements and mode of action of trans-tiliroside
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DOI：
10.1016/j.bmcl.2007.03.051
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发表时间：
2007-06-01
影响因子：
2.7
通讯作者：
Yoshikawa, Masayuki
中科院分区：
文献类型：
--
作者：
Ninomiya, Kiyofumi;Matsuda, Hisashi;Yoshikawa, Masayuki
研究发现，来自犬蔷薇果实（50 mg/kg/d）和种子（12.5 和 25 mg/kg/d）而非果皮的 80% 丙酮水提取物，在给予提取物后 2 周内，对小鼠体重和/或内脏脂肪重量的增加显示出显着的抑制作用，而不影响食物摄入。就其活性成分而言，主要成分反式替洛甙（0.1-10 mg/kg/d）可有效抑制小鼠体重增加，特别是内脏脂肪重量，并显着降低小鼠葡萄糖负荷（1 g/kg，腹膜内注射）后的血糖水平。另一方面，山奈酚和对香豆酸缺乏这种作用，而山奈酚3-0-β-D-吡喃葡萄糖苷在10mg/kg/d的剂量下倾向于降低体重和内脏脂肪重量的增加，但不显着。这些结果表明山奈酚 3-0-β-D-吡喃葡萄糖苷和对香豆酰基部分对于抗肥胖作用的重要性。此外，单次口服10 mg/kg剂量的反式-tiliroside可增加小鼠肝组织中PPAR-α mRNA的表达。 (C) 2007 Elsevier Ltd. 保留所有权利。
The 80% aqueous acetone extracts from the fruit (50 mg/kg/d) and seeds (12.5 and 25 mg/kg/d) of Rosa canina L., but not from the pericarps, were found to show substantial inhibitory effect on the gain of body weight and/or weight of visceral fat without affecting food intake in mice for 2 weeks after administration of the extracts. With regard to the active constituents, the principal constituent, trans-tiliroside (0.1-10 mg/kg/d), potently inhibited the gain of body weight, especially visceral fat weight, and significantly reduced blood glucose levels after glucose loading (1 g/kg, ip) in mice. On the other hand, kaempferol and p-coumaric acid lacked such effect and kaempferol 3-0-beta-D-glucopyranoside tended to reduce the gain of body weight and visceral fat weight, but not significantly, at a dose of 10 mg/kg/d. These results indicate the importance of both kaempferol 3-0-beta-D-glucopyranoside and p-coumaroyl moieties for anti-obese effects. Furthermore, a single oral administration of trans-tiliroside at a dose of 10 mg/kg increased the expression of PPAR-alpha mRNA of liver tissue in mice. (C) 2007 Elsevier Ltd. All rights reserved.