Title | Fatty acid synthase inhibitory activity of acylphloroglucinols isolated from Dryopteris crassirhizoma |
Authors | Min Kyun Na; JunPil Jang; B S Min; S J Lee; M S Lee; Bo Yeon Kim; Won Keun Oh; Jong Seog Ahn |
Publisher | Elsevier |
Issue Date | 2006 |
Citation | Bioorganic & Medicinal Chemistry Letters, vol. 16, no. 18, pp. 4738-4742 |
Keywords | acylphloroglucinols; dryopteridaceae; dryopteris crassirhizoma; FAS inhibitors; fatty acid synthase (FAS); fatty acid synthase inhibitor; filixic acid; flavaspidic acid; norflavaspidic acid; antineoplastic activity |
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 μM. The results of the present study indicate that the acylphloroglucinol derivatives could be considered to be a promising class of FAS inhibitors. |
ISSN | 0960-894X |
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Registered Date |
2017-04-19 |