title: Identification of diacylglycerol acyltransferase inhibitors from Rosa centifolia petals.
abstract: Diacylglycerol acyltransferase (DGAT) catalyzes the final step of triacylglycerol (TAG) synthesis, and is considered as a potential target to control hypertriglyceridemia or other metabolic disorders. In this study, we found that the extract of rose petals suppressed TAG synthesis in cultured cells, and that the extract showed DGAT inhibitory action in a dose-dependent manner. Fractionation of the rose extract revealed that the DGAT inhibitory substances in the extract were ellagitannins; among them rugosin B, and D, and eusupinin A inhibited DGAT activity by 96, 82, and 84% respectively, at 10 μM. These substances did not inhibit the activities of other hepatic microsomal enzymes, glucose-6-phosphatase and HMG-CoA reductase, or pancreatic lipase, suggesting that ellagitannins inhibit DGAT preferentially. In an oral fat load test using mice, postprandial plasma TAG increase was suppressed by rose extract; TAG levels 2 h after the fat load were significantly lower in mice administered a fat emulsion containing rose extract than in control mice (446.3 ± 33.1 vs 345.3 ± 25.0 mg/dL, control vs rose extract group; P < 0.05). These results suggest that rose ellagitannins or rose extract could be beneficial in controlling lipid metabolism and used to improve metabolic disorders.
authors.affiliation: Biological Science Laboratories, Kao Corporation, 2606 Akabane, Ichikai-machi, Haga-gun, Tochigi, 321-3497, Japan. kondo.hidehiko@kao.co.jp
authors.forename: Hidehiko
authors.initials: H
authors.lastname: Kondo
authors.forename: Kohjiro
authors.initials: K
authors.lastname: Hashizume
authors.forename: Yusuke
authors.initials: Y
authors.lastname: Shibuya
authors.forename: Tadashi
authors.initials: T
authors.lastname: Hase
authors.forename: Takatoshi
authors.initials: T
authors.lastname: Murase
mesh_terms: D000818:Animals; D002460:Cell Line; D051048:Diacylglycerol O-Acyltransferase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D004041:Dietary Fats; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000378:metabolism*; D004847:Epithelial Cells / Q000166:cytology / Q000187:drug effects; D035264:Flowers / Q000737:chemistry*; D047348:Hydrolyzable Tannins / Q000737:chemistry / Q000378:metabolism; D015228:Hypertriglyceridemia / Q000378:metabolism; D007413:Intestinal Mucosa / Q000166:cytology; D050356:Lipid Metabolism / Q000187:drug effects*; D051379:Mice; D008810:Mice, Inbred C57BL; D015394:Molecular Structure; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D027826:Rosa / Q000033:anatomy & histology / Q000737:chemistry*; D014280:Triglycerides / Q000378:metabolism
chemical_list: D004041:Dietary Fats; D004791:Enzyme Inhibitors; D047348:Hydrolyzable Tannins; D010936:Plant Extracts; D014280:Triglycerides; D051048:Diacylglycerol O-Acyltransferase