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...

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Bibliographic Details
Published in:	Journal of natural products (Washington, D.C.) Vol. 68; no. 4; pp. 617 - 619
Main Authors:	Herath, Kithsiri, Jayasuriya, Hiranthi, Ondeyka, John G, Guan, Ziqiang, Borris, Robert P, Stijfhoorn, Eirik, Stevenson, Dennis, Wang, Jianhua, Sharma, Neelam, MacNaul, Karen, Menke, John G, Ali, Aisha, Schulman, Marvin J, Singh, Sheo B
Format:	Journal Article
Language:	English
Published:	Washington, DC American Chemical Society 01-04-2005 Glendale, AZ American Society of Pharmacognosy
Subjects:	benzophenone Benzophenones - chemistry Benzophenones - isolation & purification Benzophenones - pharmacology Biological and medical sciences chemical structure DNA-Binding Proteins - metabolism Garcinia Garcinia - chemistry Garcinia humilis General pharmacology guttiferones Inhibitory Concentration 50 Ligands Liver - metabolism liver X receptor Liver X Receptors Medical sciences Molecular Structure Orphan Nuclear Receptors Pharmacognosy. Homeopathy. Health food Pharmacology. Drug treatments Receptors, Cytoplasmic and Nuclear - metabolism spectral analysis stereochemistry Ligand binding Agonist Benzophenone derivatives Ligand Guttiferae Bark Cholesterol LDL Isoprenoid Biological activity Stem Screening Dicotyledones Chemical compound library Angiospermae Plant origin Liver X receptor Isolation Spermatophyta Structural analysis
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Summary:	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 IC50 value for this compound in the LXRα-SPA binding assay was 3.4 μM. Details of the isolation, structure elucidation, and ligand binding activity of 1 are described.
Bibliography:	istex:F4929B8E371BFF3C8EDDEE4A69E6B0FEEC835431 ark:/67375/TPS-JGVN74RF-C
ISSN:	0163-3864 1520-6025
DOI:	10.1021/np050045j