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Tuberatolides, potent FXR antagonists from the korean marine tunicate Botryllus tuberatus

Title
Tuberatolides, potent FXR antagonists from the korean marine tunicate Botryllus tuberatus
Authors
Choi H.Hwang H.Chin J.Kim E.Lee J.Nam S.J.Lee B.C.Rho B.J.Kang H.
Ewha Authors
노분조
SCOPUS Author ID
노분조scopusscopus
Issue Date
2011
Journal Title
Journal of Natural Products
ISSN
0163-3864JCR Link
Citation
Journal of Natural Products vol. 74, no. 1, pp. 90 - 94
Indexed
SCI; SCIE; SCOPUS WOS scopus
Document Type
Article
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 IC50 values as low as 1.5 μM 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. © 2011 American Chemical Society and American Society of Pharmacognosy.
DOI
10.1021/np100489u
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자연과학대학 > 생명과학전공 > Journal papers
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