title: Oleanane-type triterpenoids of Aceriphyllum rossii and their diacylglycerol acyltransferase-inhibitory activity.
abstract: Six known triterpenoid compounds, 3-oxoolean-12-en-27-oic acid (1), gypsogenic acid (2), 3α-hydroxyolean-12-en-27-oic acid (3), 3β-hydroxyolean-12-en-27-oic acid (4), aceriphyllic acid A (5), and oleanolic acid (6), were isolated from the roots of Aceriphyllum rossii. Their chemical structures were determined by comparison with available (1)H-NMR and (13)C-NMR data on known compounds. All the isolated compounds were evaluated for inhibitory activity against human diacylglycerol acyltransferases 1 and 2. Most of the isolates exhibited a better inhibitory activity against diacylglycerol acyltransferase 2 (IC50: 11.6-44.2 µM) than against diacylglycerol acyltransferase 1 (IC50: 22.7-119.5 µM). In particular, compounds 1 and 5 showed strong inhibition efficacy towards diacylglycerol acyltransferases 1 and 2, and appeared to act competitively against oleoyl-CoA in vitro. The results also indicated that both compounds reduced newly synthesized triacylglycerol in HuTu80 and HepG2 cells. Oral administration of compound 1 significantly reduced postprandial triacylglycerol in mice following an oral lipid challenge. In conclusion, the current study indicates that compound 1 suppresses both de novo triacylglycerol biosynthesis and resynthesis through the inhibition of diacylglycerol acyltransferase activity, and therefore may be a useful agent for treating diseases associated with a high triacylglycerol level.
authors: Natural Medicines Research Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB), Ochang-eup, Cheongju, Korea.
authors: Jee-Hee
authors: JH
authors: Seo
authors: Natural Medicines Research Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB), Ochang-eup, Cheongju, Korea.
authors: Mun-Ock
authors: MO
authors: Kim
authors: Natural Medicines Research Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB), Ochang-eup, Cheongju, Korea.
authors: Ah-Reum
authors: AR
authors: Han
authors: Natural Medicines Research Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB), Ochang-eup, Cheongju, Korea.
authors: Eun-Bin
authors: EB
authors: Kwon
authors: Natural Medicines Research Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB), Ochang-eup, Cheongju, Korea.
authors: Myung Ji
authors: MJ
authors: Kang
authors: Incurable Diseases Therapeutics Research Center, KRIBB, Cheongju, Korea.
authors: Sungchan
authors: S
authors: Cho
authors: Department of Biology Education, Daegu University, Gyungsan, Gyeongbuk, Korea.
authors: Dong-Oh
authors: DO
authors: Moon
authors: Laboratory Animal Center, KRIBB, Yuseong-gu, Daejeon, Korea.
authors: Jung-Ran
authors: JR
authors: Noh
authors: Laboratory Animal Center, KRIBB, Yuseong-gu, Daejeon, Korea.
authors: Chul-Ho
authors: CH
authors: Lee
authors: Department of Pharmacology, Chungbuk National University, Cheongju, Korea.
authors: Young-Soo
authors: YS
authors: Kim
authors: Natural Medicines Research Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB), Ochang-eup, Cheongju, Korea.
authors: Hyun-Sun
authors: HS
authors: Lee
mesh_terms: D000214:Acyl Coenzyme A / Q000378:metabolism; D000818:Animals; D051048:Diacylglycerol O-Acyltransferase / Q000097:blood*; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D056945:Hep G2 Cells; D006801:Humans; D051379:Mice; D015394:Molecular Structure; D009828:Oleanolic Acid / Q000031:analogs & derivatives / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology*; D018517:Plant Roots; D031995:Saxifragaceae / Q000737:chemistry*; D014280:Triglycerides / Q000097:blood*
chemical_list: D000214:Acyl Coenzyme A; D004791:Enzyme Inhibitors; D010936:Plant Extracts; D014280:Triglycerides; C413246:oleanane; C017585:oleoyl-coenzyme A; D009828:Oleanolic Acid; D051048:Diacylglycerol O-Acyltransferase