Journal
MARINE DRUGS
Volume 12, Issue 4, Pages 2066-2078Publisher
MDPI AG
DOI: 10.3390/md12042066
Keywords
sterols; ascidians; tunicates; Phallusia fumigata; NMR; PXR receptor
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Funding
- European Commission [229893 (NatPharma), 311848 (BlueGenics)]
- Italian Ministero dell'Universita e della Ricerca (MIUR)
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Purification of the apolar extracts of the marine ascidian Phallusia fumigata, afforded two new sulfated sterols, phallusiasterols A (1) and B (2). The structures of the new compounds have been elucidated using mass spectrometry and NMR experiments. The effects of phallusiasterols A and B as modulators of pregnane-X-receptor (PXR) have been investigated. These studies revealed that phallusiasterol A induces PXR transactivation in HepG2 cells and stimulates the expression of the PXR target genes CYP3A4 and MDR1 in the same cell line. Molecular docking calculations suggested the theoretical binding mode of phallusiasterol A with hPXR and revealed that phallusiasterol A fitted well in the LBD of PXR.
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