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Open AccessArticle

Oxygenated Polyketides from Plakinastrella mamillaris as a New Chemotype of PXR Agonists

1
Department of Pharmacy, University of Naples "Federico II", via D. Montesano 49, Naples 80131, Italy
2
Department of Clinical and Experimental Medicine, Faculty of Medicine, University of Perugia, via Gerardo Dottori 1, S. Andrea Delle Fratte, Perugia 06132, Italy
3
Department of Pharmacy, University of Salerno, via Ponte don Melillo, Fisciano (SA) 84084, Italy
*
Author to whom correspondence should be addressed.
Mar. Drugs 2013, 11(7), 2314-2327; https://doi.org/10.3390/md11072314
Received: 24 April 2013 / Revised: 27 May 2013 / Accepted: 28 May 2013 / Published: 2 July 2013
(This article belongs to the Special Issue Marine Compounds and Inflammation)
Further purification of the apolar extracts of the sponge Plakinastrella mamillaris, afforded a new oxygenated polyketide named gracilioether K, together with the previously isolated gracilioethers E–G and gracilioethers I and J. The structure of the new compound has been elucidated by extensive NMR (1H and 13C, COSY, HSQC, HMBC, and ROESY) and ESI-MS analysis. With the exception of gracilioether F, all compounds are endowed with potent pregnane-X-receptor (PXR) agonistic activity and therefore represent a new chemotype of potential anti-inflammatory leads. Docking calculations suggested theoretical binding modes of the identified compounds, compatible with an agonistic activity on hPXR, and clarified the molecular basis of their biological activities. View Full-Text
Keywords: marine sponge; Plakinastrella mamillaris; oxygenated polyketide; nuclear receptors; pregnane-X-receptor; anti-inflammatory activity marine sponge; Plakinastrella mamillaris; oxygenated polyketide; nuclear receptors; pregnane-X-receptor; anti-inflammatory activity
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Festa, C.; D'Amore, C.; Renga, B.; Lauro, G.; Marino, S.D.; D'Auria, M.V.; Bifulco, G.; Zampella, A.; Fiorucci, S. Oxygenated Polyketides from Plakinastrella mamillaris as a New Chemotype of PXR Agonists. Mar. Drugs 2013, 11, 2314-2327.

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