title: Guttiferone I, a new prenylated benzophenone from Garcinia humilis as a liver X receptor ligand.
abstract: Liver X receptors (LXR) have been implicated in cholesterol homeostasis. Agonists of LXR are expected to increase cholesterol efflux, lower LDL, and raise HDL levels. Screening of a natural product library of plant extracts using a LXR-SPA binding assay and bioassay-guided fractionation of the bark and stem extract of Garcinia humilis led to the discovery of a new polyisoprenylated benzophenone named guttiferone I (1). The IC(50) value for this compound in the LXRalpha-SPA binding assay was 3.4 muM. Details of the isolation, structure elucidation, and ligand binding activity of 1 are described.
authors.affiliation: Merck Research Laboratories, P.O. Box 2000, Rahway, New Jersey 07065, USA.
authors.forename: Kithsiri
authors.initials: K
authors.lastname: Herath
authors.forename: Hiranthi
authors.initials: H
authors.lastname: Jayasuriya
authors.forename: John G
authors.initials: JG
authors.lastname: Ondeyka
authors.forename: Ziqiang
authors.initials: Z
authors.lastname: Guan
authors.forename: Robert P
authors.initials: RP
authors.lastname: Borris
authors.forename: Eirik
authors.initials: E
authors.lastname: Stijfhoorn
authors.forename: Dennis
authors.initials: D
authors.lastname: Stevenson
authors.forename: Jianhua
authors.initials: J
authors.lastname: Wang
authors.forename: Neelam
authors.initials: N
authors.lastname: Sharma
authors.forename: Karen
authors.initials: K
authors.lastname: Macnaul
authors.forename: John G
authors.initials: JG
authors.lastname: Menke
authors.forename: Aisha
authors.initials: A
authors.lastname: Ali
authors.forename: Marvin J
authors.initials: MJ
authors.lastname: Schulman
authors.forename: Sheo B
authors.initials: SB
authors.lastname: Singh
mesh_terms: D001577:Benzophenones / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D004268:DNA-Binding Proteins / Q000378:metabolism*; D029760:Garcinia / Q000737:chemistry*; D020128:Inhibitory Concentration 50; D008024:Ligands; D008099:Liver / Q000378:metabolism; D000071518:Liver X Receptors; D015394:Molecular Structure; D057093:Orphan Nuclear Receptors; D018160:Receptors, Cytoplasmic and Nuclear / Q000378:metabolism*
chemical_list: D001577:Benzophenones; D004268:DNA-Binding Proteins; D008024:Ligands; D000071518:Liver X Receptors; D057093:Orphan Nuclear Receptors; D018160:Receptors, Cytoplasmic and Nuclear; C501151:guttiferone I