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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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DNA-Binding Proteins / antagonists & inhibitors*
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Inhibitory Concentration 50
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Molecular Structure
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Nuclear Magnetic Resonance, Biomolecular
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Porifera / chemistry*
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Receptors, Cytoplasmic and Nuclear / antagonists & inhibitors*
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Sesterterpenes* / chemistry
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Sesterterpenes* / isolation & purification
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Sesterterpenes* / pharmacology
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Transcription Factors / antagonists & inhibitors*
Substances
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DNA-Binding Proteins
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Receptors, Cytoplasmic and Nuclear
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Sesterterpenes
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Transcription Factors
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farnesoid X-activated receptor