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

► Three new steroids 1–3 were isolated from a marine organism Dendronephthya gigantea. ► Relative stereochemistry was elucidated by the analysis of HRMS and 2-D NMR. ► New steroids 1 and 2 showed potent inhibitory activity against FXR. Three new steroids 3-oxocholest-1,22-dien-12β-ol (1), 3-oxochole...

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Published in:Steroids 2012-04, Vol.77 (5), p.355-359
Main Authors: Shin, Kyoungjin, Chin, Jungwook, Hahn, Dongyup, Lee, Jaehwan, Hwang, Hoosang, Won, Dong Hwan, Ham, Jungyeob, Choi, Hyukjae, Kang, Eunsoo, Kim, Hiyoung, Ju, Moon Kyeong, Nam, Sang-Jip, Kang, Heonjoong
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Language:English
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Summary:► Three new steroids 1–3 were isolated from a marine organism Dendronephthya gigantea. ► Relative stereochemistry was elucidated by the analysis of HRMS and 2-D NMR. ► New steroids 1 and 2 showed potent inhibitory activity against FXR. Three new steroids 3-oxocholest-1,22-dien-12β-ol (1), 3-oxocholest-1,4-dien-20β-ol (2), 3-oxocholest-1,4-dien-12β-ol (3), and three known steroids (20S)-20-Hydroxyergosta-1,4,24(28)-trien-3-one (4) [7a], 5α,8α-Epidioxycholesta-6,22-dien-3β-ol (5) [10] and 5-cholestene-3β,12β-diol (6) [11] 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 15μM.
ISSN:0039-128X
1878-5867
DOI:10.1016/j.steroids.2011.12.027