Sterols from a soft coral, Dendronephthya gigantea as farnesoid X-activated receptor antagonists

Abstract

Three new steroids 3-oxocholest-1,22-dien-12 beta-ol (1), 3-oxocholest-1,4-dien-20 beta-ol (2), 3-oxocholest-1,4-dien-12 beta-ol (3), and three known steroids (20S)-20-Hydroxyergosta-1,4,24(28)-trien-3-one (4)[7a], 5 alpha,8 alpha-Epidioxycholesta-6,22-dien-3 beta-ol (5) [10] and 5-cholestene-3 beta,12 beta-diol (6) 1111 were isolated from a soft coral Dendronephthya gigantea. Their chemical structures and relative stereochemistry were elucidated by the analysis of HRMS and 2-D NMR spectroscopic data. The steroids 1 and 2 showed notable inhibitory activity against farnesoid X-activated receptor (FXR) with IC50's 14 and 15 mu M. (C) 2012 Elsevier Inc. All rights reserved.