60(P-31) 薬用ハーブに抗肥満作用成分を探る : Salacia,Artichoke,Sage(ポスター発表の部)

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Obesity is one of the most risk factor against many life-style diseases, such as diabetes mellitus, hyperlipidemia, and hypertension. Since anti-obesitic compounds are useful for prevention or treatment of these life-style diseases, we examined the effects of three herbal medicines, Salacia, Artichoke, and Sage, on in vivo anti-obesitic and hypolipidemic activities and in vitro lipase inhibitory activities, such as pancreatic lipase (PL), rat adipose tissue-derived lipoprotein lipase (LPL), and glycerophosphate dehydrogenase (GPDH) activity in rat adipose tissue, etc. 1. Salacia reticutala The roots and stems of S. reticulata (Hippocrateaceae) have been used for prevention or remedy of diabetes in Sri Lanka and India. Previously, we reported the characterization of two α-glucosidase inhibitors named salacinol and kotalanol were isolated from the methanolic extract of this natural medicine. As a continuing study of this natural medicine, we examined the anti-obesitic effects of the water extract using obese rat models, such as female Zucker fatty rats and male SD rats fed a high fat-diet. Body weights in both obese model rats tended to be suppressed by oral administration of the water extract for 27-30 days. To clarify the mode of action of anti-obestic activity for the water extract of S. reticulata, several in vitro assays were examined. Thus, the water extract of S. reticulata tended to enhance lipolysis in rat adipocytes and was found to inhibit lipase activities (PL, LPL) and GPDH activity. By bioassay-guided separation, the following phenolic compounds were isolated as the active constituents, 1) lipolysis activity: mangiferin (1),(-)4'-O-methylepigallocatechin (2); 2) PL inhibitory activity: (-)-epigallocatechin (4), (-)-epicatechin-(4β→8)-(-)-4'-O-methylepicatechin (5); 3) LPL inhibitory activity: (-)-epicatechin (3). 2. Cynara scolymus The leaves of C. scolymus (Compositae), which is commonly called "artichoke", have been used for the treatment of hepatitis and hyperlipidemia in European traditional medicine. The methanolic extract from the leaves of C. scolymus was found to show hypolipidemic activity in olive oil-loaded mice. By bioassay-guided separation, principal guaiane-type sesquiterpenes, such as cynaropicrin. aguerin B, and grosheimin, were isolated as the active constituents. As to the structural requirement of guaiane-type sesquiterpenes for hypolipidemic activity, it was suggested that the oxygen functional groups in the guaiane skeleton and exo-methylene moiety in the α-methylene-γ-butyrolactone ring were essential for the activity. Since the methanolic extract and active constituents also suppressed gastric emptying in olive oil-loaded mice, the inhibitory activity of gastric emptying was considered to be involved in the hypolipidemic activity. 3. Salvia officinalis The leaves of S. officinalis (Labiatae, common name "Sage") have been used for the treatment of inflammation for throat, dyspepsia, and disorders. The methanolic extract and diterpene constituents from the leaves of S. officinalis were found to show the potent PL inhibitory activity.
天然有機化合物討論会の論文
2002-09-01

60(P-31) 薬用ハーブに抗肥満作用成分を探る : Salacia,Artichoke,Sage(ポスター発表の部)

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