Journal
JOURNAL OF NATURAL PRODUCTS
Volume 74, Issue 1, Pages 90-94Publisher
AMER CHEMICAL SOC
DOI: 10.1021/np100489u
Keywords
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Funding
- Ministry of Education, Science and Technology, Korea
- Ministry of Land, Transport and Maritime Affairs of Korea
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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 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.
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