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 µM. The other compounds very mildly inhibited FPTase, therefore, the inhibitory activity on FPTase very much depends on the structure of diarylheptanoids.

Keywords:

• Alnus japonica
• Curcuma longa
• Farnesyl protein transferase
• Diarylheptanoids

Acknowledgments

This research was financially supported by a grant (code: PF002107-00) from Plant Diversity Research Center of 21st Century Frontier Research Program and by a grant of Biogreen 21 Program of the Rural Development Administration.