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 microM. The results of the present study indicate that the acylphloroglucinol derivatives could be considered to be a promising class of FAS inhibitors.
Na
MinKyun
M
Korea Research Institute of Bioscience and Biotechnology, 52 Eoun-dong, Yuseong-gu, Daejeon 305-333, Republic of Korea.
Jang
JunPil
J
Min
Byung Sun
BS
Lee
Sang Jun
SJ
Lee
Myung Sun
MS
Kim
Bo Yeon
BY
Oh
Won Keun
WK
Ahn
Jong Seog
JS
D000215:Acylation; D032492:Dryopteris / Q000737:chemistry*; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology*; D064429:Fatty Acid Synthases / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D010696:Phloroglucinol / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology*
D004791:Enzyme Inhibitors; D010696:Phloroglucinol; D064429:Fatty Acid Synthases