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Mar. Drugs 2014, 12(4), 2066-2078; doi:10.3390/md12042066
Article

Phallusiasterols A and B: Two New Sulfated Sterols from the Mediterranean Tunicate Phallusia fumigata and Their Effects as Modulators of the PXR Receptor

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Received: 11 December 2013; in revised form: 27 February 2014 / Accepted: 27 February 2014 / Published: 3 April 2014
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Abstract: 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.
Keywords: sterols; ascidians; tunicates; Phallusia fumigata; NMR; PXR receptor sterols; ascidians; tunicates; Phallusia fumigata; NMR; PXR receptor
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

Imperatore, C.; D'Aniello, F.; Aiello, A.; Fiorucci, S.; D'Amore, C.; Sepe, V.; Menna, M. Phallusiasterols A and B: Two New Sulfated Sterols from the Mediterranean Tunicate Phallusia fumigata and Their Effects as Modulators of the PXR Receptor. Mar. Drugs 2014, 12, 2066-2078.

AMA Style

Imperatore C, D'Aniello F, Aiello A, Fiorucci S, D'Amore C, Sepe V, Menna M. Phallusiasterols A and B: Two New Sulfated Sterols from the Mediterranean Tunicate Phallusia fumigata and Their Effects as Modulators of the PXR Receptor. Marine Drugs. 2014; 12(4):2066-2078.

Chicago/Turabian Style

Imperatore, Concetta; D'Aniello, Filomena; Aiello, Anna; Fiorucci, Stefano; D'Amore, Claudio; Sepe, Valentina; Menna, Marialuisa. 2014. "Phallusiasterols A and B: Two New Sulfated Sterols from the Mediterranean Tunicate Phallusia fumigata and Their Effects as Modulators of the PXR Receptor." Mar. Drugs 12, no. 4: 2066-2078.



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