Guttiferone I, a new prenylated benzophenone from Garcinia humilis as a liver X receptor ligand

被引：51

作者：

Herath, K

Jayasuriya, H

Ondeyka, JG

Guan, ZQ

Borris, RP

Stijfhoorn, E

Stevenson, D

Wang, JH

Sharma, N

MacNaul, K

Menke, JG

Ali, A

Schulman, MJ

Singh, SB

机构：

[1] Merck Res Labs, Rahway, NJ 07065 USA

[2] New York Bot Garden, Inst Econ Bot, Bronx, NY 10458 USA

来源：

JOURNAL OF NATURAL PRODUCTS | 2005年 / 68卷 / 04期

关键词：

D O I：

10.1021/np050045j

中图分类号：

Q94 [植物学];

学科分类号：

071001 ;

摘要：

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 1 (1). The IC50 value for this compound in the LXR alpha-SPA binding assay was 3.4 mu M. Details of the isolation, structure elucidation, and ligand binding activity of 1 are described.

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页码：617 / 619

页数：3

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