2. Academic Validation
  3. Scalarane sesterterpenes from a marine sponge of the genus Spongia and their FXR antagonistic activity

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

Affiliation

  • 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.

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