The extract of leaves of Acer truncatum Bunge: A natural inhibitor of fatty acid synthase with antitumor activity

Abstract

Fatty acid synthase (FAS) has been identified as a potential antitumor target. The extract from the leaves of Acer truncatum Bunge (Extr) was prepared to assay its inhibitory activity against FAS, which was isolated from duck liver, and the correlated antitumor bioactivity. Its inhibition of FAS is composed of reversible fast-binding inhibition, IC₅₀ = 0.7 μg/ml, and irreversible slow-binding inhibition following saturation kinetics with a dissociation constant of 0.68 μg/ml and a limiting rate constant of 0.0288 min^{− 1}. The Extr exhibited different type of inhibitions against the three substrates in the FAS overall reaction. Compared with EGCG in inhibition constant and IC₅₀ value, the Extr appeared to be a more efficient inhibitor, and exhibited a considerable inhibition against the growth of four kinds of cancer cells (patent application number 200510068054.2). It was infered that the inhibitory activity is likely attributable to the co-operative effect of the components.

Keywords::

• Fatty acid synthase
• enzyme inhibition
• antitumor
• Acer truncatum Bunge
• kinetics

Keywords::

• EGCG
• (-)-epigallocatechin gallate
• ECG
• (-)-epicatechin gallate
• GCG
• (-)gallocatechin gallate
• FAS
• fatty acid synthase
• Extr
• Extract of leaves of Acer truncatum Bunge
• DTT
• dithiothreitol
• EtOAc
• ethyl acetate

Acknowledgements

The present investigation was supported by the Scientific Research Common Program of Beijing Municipal Commission of Education No. KM200410025013, China.