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| Festa, Carmen; D'Amore, Claudio; Renga, Barbara; Lauro, Gianluigi; De Marino, Simona; D'Auria, Maria Valeria; Bifulco, Giuseppe; Zampella, Angela; Fiorucci, Stefano. |
| 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 (H-1 and C-13, 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. |
| Tipo: Text |
Palavras-chave: Marine sponge; Plakinastrella mamillaris; Oxygenated polyketide; Nuclear receptors; Pregnane-X-receptor; Anti-inflammatory activity. |
| Ano: 2013 |
URL: https://archimer.ifremer.fr/doc/00217/32781/31238.pdf |
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