title: Peroxisome proliferator-activated receptor transactivational effects in HepG2 cells of cembranoids from the soft coral Lobophytum crassum Von Marenzeller.
abstract: Peroxisome proliferator-activated receptors (PPARs) are ligand-activated transcription factors that regulate the expression of multiple genes involved in metabolic, anti-inflammatory, and developmental processes. This study evaluated the PPARs transactivational effects of thirteen cembranoid diterpenoids 1-13 from the soft coral Lobophytum crassum, using PPAR-responsive elements-luciferase reporter and GAL4-PPAR chimera assays. All isolated compounds activated the transcription of PPARs in a dose-dependent manner, with EC50 values ranging from 2.07 ± 1.73 to 130.20 ± 1.85 μM. Moreover, compounds 6-9 affected the transactivation of all three PPAR types, PPARα, γ, β(δ), in a dose-dependent manner, with EC50 values in a ranging from 11.92 ± 1.23 to 122.50 ± 2.12 μM. These results provide a scientific rationale for further studies on the soft coral L. crassum and its diterpenoid constituents to develop medicinal products against inflammatory and metabolic diseases.
authors.affiliation: Institute of Marine Biochemistry (IMBC), Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet, Nghiado, Caugiay, Hanoi, Vietnam.
authors.forename: Nguyen Phuong
authors.initials: NP
authors.lastname: Thao
authors.forename: Bui Thi Thuy
authors.initials: BT
authors.lastname: Luyen
authors.forename: Nguyen Thi Thanh
authors.initials: NT
authors.lastname: Ngan
authors.forename: Le Duc
authors.initials: le D
authors.lastname: Dat
authors.forename: Nguyen Xuan
authors.initials: NX
authors.lastname: Cuong
authors.forename: Nguyen Hoai
authors.initials: NH
authors.lastname: Nam
authors.forename: Phan Van
authors.initials: PV
authors.lastname: Kiem
authors.forename: Seok Bean
authors.initials: SB
authors.lastname: Song
authors.forename: Chau Van
authors.initials: CV
authors.lastname: Minh
authors.forename: Young Ho
authors.initials: YH
authors.lastname: Kim
mesh_terms: D000818:Animals; D037421:Anthozoa; D004224:Diterpenes / Q000302:isolation & purification* / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D056945:Hep G2 Cells; D006801:Humans; D047492:Peroxisome Proliferator-Activated Receptors / Q000235:genetics* / Q000378:metabolism*; D015533:Transcriptional Activation / Q000187:drug effects / Q000502:physiology*
chemical_list: D004224:Diterpenes; D047492:Peroxisome Proliferator-Activated Receptors