Ninomiya Kiyofumi, Matsuda Hisashi, Kubo Mizuho, Morikawa Toshio, Nishida Norihisa, Yoshikawa Masayuki
Kyoto Pharmaceutical University, Misasagi, Yamashina-ku, Kyoto 607-8412, Japan.
Bioorg Med Chem Lett. 2007 Jun 1;17(11):3059-64. doi: 10.1016/j.bmcl.2007.03.051. Epub 2007 Mar 18.
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-O-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-O-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.
研究发现，犬蔷薇果实（50毫克/千克/天）和种子（12.5毫克/千克/天和25毫克/千克/天）的80%丙酮水提取物对小鼠体重增加和/或内脏脂肪重量有显著抑制作用，但果皮提取物无此作用，且给药后2周内不影响小鼠食物摄入量。关于活性成分，主要成分反式椴树苷（0.1 - 10毫克/千克/天）能有效抑制体重增加，尤其是内脏脂肪重量，并显著降低小鼠葡萄糖负荷（1克/千克，腹腔注射）后的血糖水平。另一方面，山奈酚和对香豆酸没有这种作用，山奈酚3 - O - β - D - 吡喃葡萄糖苷在剂量为10毫克/千克/天时倾向于降低体重和内脏脂肪重量，但不显著。这些结果表明山奈酚3 - O - β - D - 吡喃葡萄糖苷和对香豆酰部分对抗肥胖作用都很重要。此外，以10毫克/千克的剂量单次口服反式椴树苷可增加小鼠肝脏组织中PPAR - α mRNA的表达。
