title: Components from the steamed leaves of Acanthopanax koreanum and their effects on PPAR activity in HepG2 cells.
abstract: Three ent-kaurane diterpenes (1-3), four lupane-triterpene glycosides (4-7), and an oleanane-triterpene glycoside (8) were isolated from the ethyl acetate and water extracts of the steamed leaves of Acanthopanax koreanum using a combination of various column chromatographies. The structures of the isolates were determined by 1H-, 13C-NMR spectroscopy and mass spectrometry. To investigate the biological effects of the eight compounds (1-8) on peroxisome proliferator-activated receptor gamma (PPARgamma), luciferase reporter assays were used. Among the tested compounds, ent-kaur-16-en-19-oic acid (1), 16alpha-hydroxy-ent-kauran-19-oic acid (2), and 17-hydroxy-ent-kaur-15-en-19-oic acid (3) showed considerable effects on PPARgamma activity, compared with the positive control, troglitazone. To evaluate specificity and sensitivity of the active compounds (1-3) in the regulation of transactivation of PPARs, Gal4-PPARs-LBD luciferase reporter assays were examined. In this study, the three ent-kaurane diterpenes (1-3) were found to up-regulate PPARbeta/delta and PPARgamma activities, whereas they did not activate PPARalpha activity.
authors.affiliation: College of Pharmacy, Chungnam National University, Daejeon 305-764, Korea.
authors.forename: Jeong Ah
authors.initials: JA
authors.lastname: Kim
authors.forename: Seek Bean
authors.initials: SB
authors.lastname: Song
authors.forename: Seo Young
authors.initials: SY
authors.lastname: Yang
authors.forename: Young Ho
authors.initials: YH
authors.lastname: Kim
mesh_terms: D004224:Diterpenes / Q000737:chemistry* / Q000494:pharmacology*; D045786:Diterpenes, Kaurane; D028001:Eleutherococcus / Q000737:chemistry*; D056945:Hep G2 Cells; D006801:Humans; D015394:Molecular Structure; D047492:Peroxisome Proliferator-Activated Receptors / Q000378:metabolism*; D018515:Plant Leaves / Q000737:chemistry*
chemical_list: D004224:Diterpenes; D045786:Diterpenes, Kaurane; D047492:Peroxisome Proliferator-Activated Receptors; C518478:ent-16alphaH,17-hydroxy-kauran-19-oic acid; C014341:argyrophilic acid; C008037:17-hydroxy-ent-kaur-15-en-19-oic acid