| Registro completo |
| Provedor de dados: |
ArchiMer
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| País: |
France
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| Título: |
Oxygenated Polyketides from Plakinastrella mamillaris as a New Chemotype of PXR Agonists
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| Autores: |
Festa, Carmen
D'Amore, Claudio
Renga, Barbara
Lauro, Gianluigi
De Marino, Simona
D'Auria, Maria Valeria
Bifulco, Giuseppe
Zampella, Angela
Fiorucci, Stefano
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| Data: |
2013-07
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| Ano: |
2013
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| Palavras-chave: |
Marine sponge
Plakinastrella mamillaris
Oxygenated polyketide
Nuclear receptors
Pregnane-X-receptor
Anti-inflammatory activity
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| Resumo: |
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.
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| Tipo: |
Text
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| Idioma: |
Inglês
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| Identificador: |
https://archimer.ifremer.fr/doc/00217/32781/31238.pdf
DOI:10.3390/md11072314
https://archimer.ifremer.fr/doc/00217/32781/
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| Editor: |
Mdpi Ag
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| Formato: |
application/pdf
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| Fonte: |
Marine Drugs (1660-3397) (Mdpi Ag), 2013-07 , Vol. 11 , N. 7 , P. 2314-2327
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| Direitos: |
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.
info:eu-repo/semantics/openAccess
restricted use
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