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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Alkyl and Aryl Transferases / antagonists & inhibitors
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Alnus*
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Animals
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Curcuma*
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Diarylheptanoids / administration & dosage
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Diarylheptanoids / pharmacology*
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Diarylheptanoids / therapeutic use
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Fruit
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Inhibitory Concentration 50
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Organophosphonates / administration & dosage
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Organophosphonates / pharmacology*
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Organophosphonates / therapeutic use
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Phytotherapy*
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Plant Extracts / administration & dosage
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Plant Extracts / pharmacology*
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Plant Extracts / therapeutic use
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Plant Roots
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Rats
Substances
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2-(2-oxo-2-((3,7,11-trimethyl-2,6,10-dodecatrienyl)oxy)aminoethyl)phosphonic acid, (2,2-dimethyl-1-oxopropoxy)methyl ester sodium
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Diarylheptanoids
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Organophosphonates
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Plant Extracts
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Alkyl and Aryl Transferases
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p21(ras) farnesyl-protein transferase