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

  • J Nat Prod. 2007 Nov;70(11):1691-5. doi: 10.1021/np070024k.
Sang-Jip Nam  1 ,  Hyunsil Ko ,  Moon Kyeong Ju ,  Hoosang Hwang ,  Jungwook Chin ,  Jungyeob Ham ,  Byoungchan Lee ,  Jaehwan Lee ,  Dong Hwan Won ,  Hyukjae Choi ,  Jaeyoung Ko ,  Kyoungjin Shin ,  Taekyung Oh ,  Seokho Kim ,  Jung-Rae Rho ,  Heonjoong Kang
Affiliations
  • 1. Center for Marine Natural Products and Drug Discovery, School of Earth and Environmental Sciences, Seoul National University, NS-80, Seoul, 151-747, Korea.
PMID: 17988093 DOI: 10.1021/np070024k
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 IC50 values of 2.4 and 24 microM, 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.