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Scalarane sesterterpenes from a marine sponge of the genus Spongia and their FXR antagonistic activity

  • Sang Jip Nam
  • , Hyunsil Ko
  • , Kyeong Ju Moon
  • , Hoosang Hwang
  • , Jungwook Chin
  • , Jungyeob Ham
  • , Byoungchan Lee
  • , Jaehwan Lee
  • , Hwan Won Dong
  • , Hyukjae Choi
  • , Jaeyoung Ko
  • , Kyoungjin Shin
  • , Taekyung Oh
  • , Seokho Kim
  • , Jung Rae Rho
  • , Heonjoong Kang
  • Seoul National University
  • Korea Institute of Science and Technology
  • Kunsan National University

Research output: Contribution to journalArticlepeer-review

Abstract

Three new scalarane-based sesterterpenes, 1-3, were isolated from a marine sponge of the genus Spongia, and their chemical structures were elucidated by analysis of HRMS and 2-D NMR spectra. The isolated compounds 1 and 3 showed inhibition against the farnesoid X-activated receptor (FXR) with IC 50 values of 2.4 and 24 μM, respectively. In particular, compound 3 directly inhibited the interaction between FXR and a coactivator peptide (SRC-1) as determined by surface plasmon resonance (SPR) spectroscopy.

Original languageEnglish
Pages (from-to)1691-1695
Number of pages5
JournalJournal of Natural Products
Volume70
Issue number11
DOIs
StatePublished - Nov 2007
Externally publishedYes

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