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

Hyukjae Choi, Hoosang Hwang, Jungwook Chin, Euno Kim, Jaehwan Lee, Sang Jip Nam, Byoung Chan Lee, Boon Jo Rho, Heonjoong Kang

Research output: Contribution to journalArticlepeer-review

56 Scopus citations

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.

Original languageEnglish
Pages (from-to)90-94
Number of pages5
JournalJournal of Natural Products
Volume74
Issue number1
DOIs
StatePublished - 28 Jan 2011

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