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.
Terpenes U 0200 Farnesoid X-Activated Receptor Antagonists from a Marine Sponge Spongia sp. -Compounds (I) show high antagonistic activity against the target receptor. -(NAM, S.-J.; KO, H.; SHIN, M.; HAM, J.; CHIN, J.; KIM, Y.; KIM, H.; SHIN, K.; CHOI, H.; KANG*, H.; Bioorg.
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