Pubblicazione:
On the Cholesterol Raising Effect of Coffee Diterpenes Cafestol and 16-O-Methylcafestol: Interaction with Farnesoid X Receptor
On the Cholesterol Raising Effect of Coffee Diterpenes Cafestol and 16-O-Methylcafestol: Interaction with Farnesoid X Receptor
Nessuna miniatura disponibile
Data
2024
Autori
Elena Guercia
Federico Berti
Rita DE ZORZI
Luciano Navarini
Silvano Geremia
Barbara Medagli
Marco De Conto
Alberto Cassetta
Cristina FORZATO
Titolo del Periodico
ISSN Periodico
Titolo volume
Editore
Progetti di ricerca
Strutture
Fascicolo Periodico
Abstract
The diterpene cafestol represents the most potent cholesterol-elevating compound known in the human diet, being responsible for more than 80% of the effect of coffee on serum lipids, with a mechanism still not fully clarified. In the present study, the interaction of cafestol and 16-O-methylcafestol with the stabilized ligand-binding domain (LBD) of the Farnesoid X Receptor was evaluated by fluorescence and circular dichroism. Fluorescence quenching was observed with both cafestol and 16-O-methylcafestol due to an interaction occurring in the close environment of the tryptophan W454 residue of the protein, as confirmed by docking and molecular dynamics. A conformational change of the protein was also observed by circular dichroism, particularly for cafestol. These results provide evidence at the molecular level of the interactions of FXR with the coffee diterpenes, confirming that cafestol can act as an agonist of FXR, causing an enhancement of the cholesterol level in blood serum.
Descrizione
Parole chiavi
16-O-methylcafestol,
FXR,
cafestol,
circular dichroism,
coffee,
fluorescence