Potent anti-obese principle from Rosa canina: structural requirements and mode of action of trans-tiliroside.
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.
Ninomiya
Kiyofumi
K
Kyoto Pharmaceutical University, Misasagi, Yamashina-ku, Kyoto 607-8412, Japan.
Matsuda
Hisashi
H
Kubo
Mizuho
M
Morikawa
Toshio
T
Nishida
Norihisa
N
Yoshikawa
Masayuki
M
D000096:Acetone / Q000737:chemistry; D000818:Animals; D019440:Anti-Obesity Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D001578:Benzopyrans / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D001835:Body Weight / Q000187:drug effects*; D003373:Coumaric Acids / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D005419:Flavonoids; D050152:Intra-Abdominal Fat / Q000187:drug effects; D044949:Kaempferols / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D008099:Liver / Q000378:metabolism; D051379:Mice; D047493:PPAR alpha / Q000235:genetics / Q000378:metabolism*; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology; D011422:Propionates; D012333:RNA, Messenger / Q000378:metabolism; D027826:Rosa / Q000737:chemistry*; D013329:Structure-Activity Relationship; D014867:Water / Q000737:chemistry; D015430:Weight Gain / Q000187:drug effects
D019440:Anti-Obesity Agents; D001578:Benzopyrans; D003373:Coumaric Acids; D005419:Flavonoids; D044949:Kaempferols; D047493:PPAR alpha; D010936:Plant Extracts; D011422:Propionates; D012333:RNA, Messenger; D014867:Water; D000096:Acetone; C052083:tiliroside; C006552:kaempferol; C495469:p-coumaric acid