Inhibitory activity of diarylheptanoids on farnesyl protein transferase.
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.
Kang
Hyun-Mi
HM
Korea Research Institute of Bioscience and Biotechnology, 52 Uendong, Yusung, Taejon 305-600, Republic of Korea.
Son
Kwang-Hee
KH
Yang
Deok Cho
DC
Han
Dong-Cho
DC
Kim
Jong Han
JH
Baek
Nam-In
NI
Kwon
Byoung-Mog
BM
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
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