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.

Journal of natural products (2007-11-09)

Sang-Jip Nam, 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

PMID17988093

ZUSAMMENFASSUNG

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.