title: Cytotoxic and PPARs transcriptional activities of sterols from the Vietnamese soft coral Lobophytum laevigatum.
abstract: A new unusual sterol, named lobophytosterol (1), and five known metabolites (2-6) were isolated from the methanol extract of the soft coral Lobophytum laevigatum. Their chemical structures were elucidated by extensive spectroscopic analysis and comparison with those reported in the literature. The absolute stereochemistry of 1 was determined using a modified Mosher's method. Compounds 1-3 showed cytotoxic activity against HCT-116 cells with IC(50) values of 3.2, 6.9 and 18.1 μM, respectively. Compound 1 additionally displayed cytotoxic effects on A549 and HL-60 cells with IC(50) values of 4.5 and 5.6 μM, respectively. Treatment of these cells with compound 1 resulted in an induction of apoptosis evident by chromatin condensation in treated cells. Besides, compounds 2, 4, and 6 significantly upregulated PPARs transcriptional activity dose-dependently in Hep-G2 cells. Taken together, these data suggest that compound 1 might inhibit the growth of the cancer cells by the induction of apoptosis, and compounds 2, 4, and 6 might act as specific agonists for PPARα, PPARδ, and PPARγ and may therefore regulate cellular glucose, lipid, and cholesterol metabolism.
authors.affiliation: College of Pharmacy, Chungnam National University, Daejeon 305-764, Republic of Korea.
authors.forename: Tran Hong
authors.initials: TH
authors.lastname: Quang
authors.forename: Tran Thu
authors.initials: TT
authors.lastname: Ha
authors.forename: Chau Van
authors.initials: CV
authors.lastname: Minh
authors.forename: Phan Van
authors.initials: PV
authors.lastname: Kiem
authors.forename: Hoang Thanh
authors.initials: HT
authors.lastname: Huong
authors.forename: Nguyen Thi Thanh
authors.initials: NT
authors.lastname: Ngan
authors.forename: Nguyen Xuan
authors.initials: NX
authors.lastname: Nhiem
authors.forename: Nguyen Huu
authors.initials: NH
authors.lastname: Tung
authors.forename: Nguyen Phuong
authors.initials: NP
authors.lastname: Thao
authors.forename: Dinh Thi Thu
authors.initials: DT
authors.lastname: Thuy
authors.forename: Seok Bean
authors.initials: SB
authors.lastname: Song
authors.forename: Hye-Jin
authors.initials: HJ
authors.lastname: Boo
authors.forename: Hee-Kyoung
authors.initials: HK
authors.lastname: Kang
authors.forename: Young Ho
authors.initials: YH
authors.lastname: Kim
mesh_terms: D000818:Animals; D037421:Anthozoa / Q000737:chemistry*; D049109:Cell Proliferation / Q000187:drug effects; D005786:Gene Expression Regulation / Q000187:drug effects; D045325:HCT116 Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D009682:Magnetic Resonance Spectroscopy; D000432:Methanol / Q000737:chemistry; D008958:Models, Molecular; D015394:Molecular Structure; D047492:Peroxisome Proliferator-Activated Receptors / Q000378:metabolism*; D013261:Sterols / Q000032:analysis / Q000633:toxicity*
chemical_list: D047492:Peroxisome Proliferator-Activated Receptors; D013261:Sterols; D000432:Methanol