Fatty acid synthase inhibitory activity of acylphloroglucinols isolated from Dryopteris crassirhizoma

Bioorg Med Chem Lett. 2006 Sep 15;16(18):4738-42. doi: 10.1016/j.bmcl.2006.07.018. Epub 2006 Jul 25.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acylation
  • Dryopteris / chemistry*
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / isolation & purification
  • Enzyme Inhibitors / pharmacology*
  • Fatty Acid Synthases / antagonists & inhibitors*
  • Fatty Acid Synthases / metabolism*
  • Inhibitory Concentration 50
  • Molecular Structure
  • Phloroglucinol / chemistry*
  • Phloroglucinol / isolation & purification
  • Phloroglucinol / pharmacology*

Substances

  • Enzyme Inhibitors
  • Phloroglucinol
  • Fatty Acid Synthases