Fatty acid synthase inhibitory activity of acylphloroglucinols isolated from Dryopteris crassirhizoma

Fatty acid synthase (FAS) is emerging as a potential therapeutic target to treat cancer and obesity. Bioassay-guided fractionation of a MeOH extract of the rhizomes of Dryopteris crassirhizoma (Dryopteridaceae), using an in vitro FAS inhibitory assay, resulted in the isolation of a series of acylphloroglucinols, as the active principles. The isolates 1–10 inhibited FAS with IC50 values ranging from 23.1 ± 1.4 to 71.7 ± 3.9 μM. The results of the present study indicate that the acylphloroglucinol derivatives could be considered to be a promising class of FAS inhibitors.

Graphical abstractBioassay-guided fractionation of a MeOH extract of the rhizomes of Dryopteris crassirhizoma led to the isolation of a series of acylphloroglucinols, as the active principles.Figure optionsDownload full-size imageDownload as PowerPoint slide