Data/hora: 13/06/2024 08:23:06

Provedor de dados: | 5
País: | France
Título: | Oxygenated Polyketides from Plakinastrella mamillaris as a New Chemotype of PXR Agonists
Autores: | Festa, Carmen; D'Amore, Claudio; Renga, Barbara; Lauro, Gianluigi; De Marino, Simona; D'Auria, Maria Valeria; Bifulco, Giuseppe; Zampella, Angela; Fiorucci, Stefano.
Data: | 2013-07
Ano: | 2013
Palavras-chave: | Marine sponge; Plakinastrella mamillaris; Oxygenated polyketide; Nuclear receptors; Pregnane-X-receptor; Anti-inflammatory activity.
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.
Tipo: | Text
Idioma: | Inglês

Identificador:

https://archimer.ifremer.fr/doc/00217/32781/31238.pdf

DOI:10.3390/md11072314

https://archimer.ifremer.fr/doc/00217/32781/

Editor: | Mdpi Ag
Formato: | application/pdf
Fonte: | Marine Drugs (1660-3397) (Mdpi Ag), 2013-07 , Vol. 11 , N. 7 , P. 2314-2327

Fonte:

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