title: Inhibitory activity of diarylheptanoids on farnesyl protein transferase.
abstract: Diarylheptanoids [curcumin (1), demethoxycurcumin (2), bisdemethoxycurcumin (3), bisdimethoxymethylcurcumin (4), and 1,2-dihydrobis(de-O-methyl)curcumin (5)] were isolated from the methanolic extract of Curcuma longa L. and a new cyclic diarylheptanoid (6) and a known Compound 7 were isolated from fruits of Alnus japonica Steud. Diarylheptanoids (1-3) inhibited farnesyl protein transferase (FPTase) with an IC50 of 29-50 microM. The other compounds very mildly inhibited FPTase, therefore, the inhibitory activity on FPTase very much depends on the structure of diarylheptanoids.
authors.affiliation: Korea Research Institute of Bioscience and Biotechnology, 52 Uendong, Yusung, Taejon 305-600, Republic of Korea.
authors.forename: Hyun-Mi
authors.initials: HM
authors.lastname: Kang
authors.forename: Kwang-Hee
authors.initials: KH
authors.lastname: Son
authors.forename: Deok Cho
authors.initials: DC
authors.lastname: Yang
authors.forename: Dong-Cho
authors.initials: DC
authors.lastname: Han
authors.forename: Jong Han
authors.initials: JH
authors.lastname: Kim
authors.forename: Nam-In
authors.initials: NI
authors.lastname: Baek
authors.forename: Byoung-Mog
authors.initials: BM
authors.lastname: Kwon
mesh_terms: D019883:Alkyl and Aryl Transferases / Q000037:antagonists & inhibitors; D029661:Alnus; D000818:Animals; D030024:Curcuma; D036381:Diarylheptanoids / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D005638:Fruit; D020128:Inhibitory Concentration 50; D063065:Organophosphonates / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D008517:Phytotherapy; D010936:Plant Extracts / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D018517:Plant Roots; D051381:Rats
chemical_list: C436083:2-(2-oxo-2-((3,7,11-trimethyl-2,6,10-dodecatrienyl)oxy)aminoethyl)phosphonic acid, (2,2-dimethyl-1-oxopropoxy)methyl ester sodium; D036381:Diarylheptanoids; D063065:Organophosphonates; D010936:Plant Extracts; D019883:Alkyl and Aryl Transferases; C064911:p21(ras) farnesyl-protein transferase