title: Bioassay-guided isolation of fatty acid synthase inhibitory diterpenoids from the roots of Salvia miltiorrhiza Bunge.
abstract: Fatty acid synthase (FAS) is considered as a novel drug target for the development of anticancer and anti-obesity agents. Bioassay-guided fractionation of a n-hexane-soluble extract prepared from the roots of Salvia miltiorrhiza Bunge (Labiatae), using an in vitro enzyme assay, led to the isolation of five abietane diterpenoids: 15,16-dihydrotanshinone I (1), cryptotanshinone (2), tanshinone I (3), tanshinone IIA (4), and dansenspiroketallactone (5). Compounds 1-5 were tested for their in vitro FAS inhibitory activity and, except for compound 5 (IC(50) > 100 μM), compounds 1-4 inhibited the enzyme activity with IC(50) values ranging from 12.0 to 30.3 μM. Our findings may be partially related to the anticancer activity of abietane diterpenoids from the plant, suggesting a further study on the anticancer potential of tanshinone derivatives.
authors.affiliation: College of Medicine, CHA University, Seoul 135-080, Korea.
authors.forename: Tae-Su
authors.initials: TS
authors.lastname: Jang
authors.forename: HaiYan
authors.initials: H
authors.lastname: Zhang
authors.forename: GeumJin
authors.initials: G
authors.lastname: Kim
authors.forename: Dong Woo
authors.initials: DW
authors.lastname: Kim
authors.forename: Byung-Sun
authors.initials: BS
authors.lastname: Min
authors.forename: Wonku
authors.initials: W
authors.lastname: Kang
authors.forename: Kun Ho
authors.initials: KH
authors.lastname: Son
authors.forename: MinKyun
authors.initials: M
authors.lastname: Na
authors.forename: Seung Ho
authors.initials: SH
authors.lastname: Lee
mesh_terms: D045784:Abietanes / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000302:isolation & purification* / Q000494:pharmacology*; D001681:Biological Assay; D049109:Cell Proliferation / Q000187:drug effects; D005591:Chemical Fractionation / Q000379:methods*; D002851:Chromatography, High Pressure Liquid; D004305:Dose-Response Relationship, Drug; D064429:Fatty Acid Synthases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D054872:Fatty Acid Synthesis Inhibitors / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D018922:HL-60 Cells; D006586:Hexanes / Q000737:chemistry; D006801:Humans; D020128:Inhibitory Concentration 50; D009682:Magnetic Resonance Spectroscopy; D018517:Plant Roots; D051381:Rats; D027561:Salvia miltiorrhiza / Q000737:chemistry*; D012997:Solvents / Q000737:chemistry; D013056:Spectrophotometry, Ultraviolet
chemical_list: D045784:Abietanes; D000972:Antineoplastic Agents, Phytogenic; D054872:Fatty Acid Synthesis Inhibitors; D006586:Hexanes; D012997:Solvents; D064429:Fatty Acid Synthases