Abstract：
:In recent years many sterols with unusual structures and promising biological profiles have been identified from marine sources. Here we report the isolation of a series of 24-alkylated-hydroxysteroids from the soft coral Sinularia kavarattiensis, acting as pregnane X receptor (PXR) modulators. Starting from this scaffold a number of derivatives were prepared and evaluated for their ability to activate the PXR by assessing transactivation and quantifying gene expression. Our study reveals that ergost-5-en-3β-ol (4) induces PXR transactivation in HepG2 cells and stimulates the expression of the PXR target gene CYP3A4. To shed light on the molecular basis of the interaction between these ligands and PXR, we investigated, through docking simulations, the binding mechanism of the most potent compound of the series, 4, to the PXR. Our findings provide useful functional and structural information to guide further investigations and drug design.
journal_name
Mar Drugsjournal_title
Marine drugsauthors
Sepe V,Di Leva FS,D'Amore C,Festa C,De Marino S,Renga B,D'Auria MV,Novellino E,Limongelli V,D'Souza L,Majik M,Zampella A,Fiorucci Sdoi
10.3390/md12063091subject
Has Abstractpub_date
2014-05-27 00:00:00pages
3091-115issue
6issn
1660-3397pii
md12063091journal_volume
12pub_type
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