Tuberatolides, Potent FXR Antagonists from the Korean Marine Tunicate Botryllus tuberatus

Title
Tuberatolides, Potent FXR Antagonists from the Korean Marine Tunicate Botryllus tuberatus
Author(s)
최혁재Hoosang Hwang[Hoosang Hwang]Jungwook Chin[Jungwook Chin]Euno Kim[Euno Kim]Jaehwan Lee[Jaehwan Lee]Sang-Jip Nam[Sang-Jip Nam]Byoung Chan Lee[Byoung Chan Lee]Boon Jo Rho [Boon Jo Rho ]Heonjoong Kang[Heonjoong Kang]
Keywords
FARNESOID-X-RECEPTOR; NUCLEAR RECEPTOR; ABSOLUTE-CONFIGURATION; NATURAL-PRODUCT; BILE-ACIDS; IDENTIFICATION; LIGAND; ATHEROSCLEROSIS; PLASTOQUINONES; CHOLESTEROL
Issue Date
201101
Publisher
AMER CHEMICAL SOC
Citation
JOURNAL OF NATURAL PRODUCTS, v.74, no.1, pp.90 - 94
Abstract
One isoprenoid, tuberatolide A (1), meroterpenoids tuberatolide B (2) and 2'-epi-tuberatolide B (3), and the known meroterpenoids yezoquinolide (4), (R)-sargachromenol (5), and (S)-sargachromenol (6) were isolated from the Korean marine tunicate Botryllus tuberatus. The structures of these compounds were elucidated by NMR, MS, and CD spectroscopic analyses. These terpenoids antagonized the chenodeoxycholic acid (CDCA)-activated human farnesoid X receptor (hFXR) in a cell-based co-transfection assay with IC(50) values as low as 1.5 mu M without significant effect on steroid receptors. Furthermore, they released the co-activator peptide from the CDCA-bound hFXR ligand binding domain in cell-free surface plasmon resonance experiments.
URI
http://hdl.handle.net/YU.REPOSITORY/25738http://dx.doi.org/10.1021/np100489u
ISSN
0163-3864
Appears in Collections:
약학대학 > 약학부 > Articles
Files in This Item:
There are no files associated with this item.
Export
RIS (EndNote)
XLS (Excel)
XML


qrcode

Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.

BROWSE