title: Scalarane sesterterpenes from a marine sponge of the genus Spongia and their FXR antagonistic activity.
abstract: Three new scalarane-based sesterterpenes, 1- 3, were isolated from a marine sponge of the genus Spongia, and their chemical structures were elucidated by analysis of HRMS and 2-D NMR spectra. The isolated compounds 1 and 3 showed inhibition against the farnesoid X-activated receptor (FXR) with IC50 values of 2.4 and 24 microM, respectively. In particular, compound 3 directly inhibited the interaction between FXR and a coactivator peptide (SRC-1) as determined by surface plasmon resonance (SPR) spectroscopy.
authors.affiliation: Center for Marine Natural Products and Drug Discovery, School of Earth and Environmental Sciences, Seoul National University, NS-80, Seoul, 151-747, Korea.
authors.forename: Sang-Jip
authors.initials: SJ
authors.lastname: Nam
authors.forename: Hyunsil
authors.initials: H
authors.lastname: Ko
authors.forename: Moon Kyeong
authors.initials: MK
authors.lastname: Ju
authors.forename: Hoosang
authors.initials: H
authors.lastname: Hwang
authors.forename: Jungwook
authors.initials: J
authors.lastname: Chin
authors.forename: Jungyeob
authors.initials: J
authors.lastname: Ham
authors.forename: Byoungchan
authors.initials: B
authors.lastname: Lee
authors.forename: Jaehwan
authors.initials: J
authors.lastname: Lee
authors.forename: Dong Hwan
authors.initials: DH
authors.lastname: Won
authors.forename: Hyukjae
authors.initials: H
authors.lastname: Choi
authors.forename: Jaeyoung
authors.initials: J
authors.lastname: Ko
authors.forename: Kyoungjin
authors.initials: K
authors.lastname: Shin
authors.forename: Taekyung
authors.initials: T
authors.lastname: Oh
authors.forename: Seokho
authors.initials: S
authors.lastname: Kim
authors.forename: Jung-Rae
authors.initials: JR
authors.lastname: Rho
authors.forename: Heonjoong
authors.initials: H
authors.lastname: Kang
mesh_terms: D000818:Animals; D004268:DNA-Binding Proteins / Q000037:antagonists & inhibitors*; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D019906:Nuclear Magnetic Resonance, Biomolecular; D011161:Porifera / Q000737:chemistry*; D018160:Receptors, Cytoplasmic and Nuclear / Q000037:antagonists & inhibitors*; D054830:Sesterterpenes / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D014157:Transcription Factors / Q000037:antagonists & inhibitors*; D000099150:Receptor, Farnesoid X-Activated
chemical_list: D004268:DNA-Binding Proteins; D018160:Receptors, Cytoplasmic and Nuclear; D054830:Sesterterpenes; D014157:Transcription Factors; D000099150:Receptor, Farnesoid X-Activated