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

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• 作者：Hyukjae Choi ; Hoosang Hwang ; Jungwook Chin ; Euno Kim ; Jaehwan Lee ; Sang-Jip Nam ; Byoung Chan Lee ; Boon Jo Rho ; Heonjoong Kang
• 刊名：Journal of Natural Products
• 出版年：2011
• 出版时间：January 28, 2011
• 年：2011
• 卷：74
• 期：1
• 页码：90-94
• 全文大小：207K
• 年卷期：v.74,no.1(January 28, 2011)
• ISSN：1520-6025

文摘

One isoprenoid, tuberatolide A (1), meroterpenoids tuberatolide B (2) and 2鈥?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 渭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.