Guttiferone I, a new prenylated benzophenone from Garcinia humilis as a liver X receptor ligand.
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.
Herath, K; Jayasuriya, H; Ondeyka, JG; Guan, Z; Borris, RP; Stijfhoorn, E; Stevenson, D; Wang, J; Sharma, N; Macnaul, K; Menke, JG; Ali, A; Schulman, MJ; Singh, SB
Volume / Issue
Start / End Page
International Standard Serial Number (ISSN)
Digital Object Identifier (DOI)