Fatty acid synthase inhibitory activity of acylphloroglucinols isolated from Dryopteris crassirhizoma.

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Na M, Jang J, Min BS, Lee SJ, Lee MS, Kim BY, Oh WK, Ahn JS

Fatty acid synthase inhibitory activity of acylphloroglucinols isolated from Dryopteris crassirhizoma.

Bioorg Med Chem Lett. 2006 Sep 15;16(18):4738-42. Epub 2006 Jul 25.

PubMed ID
16870425 [ View in PubMed
]
Abstract

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 microM. The results of the present study indicate that the acylphloroglucinol derivatives could be considered to be a promising class of FAS inhibitors.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
CeruleninFatty acid synthaseIC 50 (nM)13000N/AN/ADetails