The extract of leaves of Acer truncatum Bunge: A natural inhibitor of fatty acid synthase with antitumor activity.
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 microg/ml, and irreversible slow-binding inhibition following saturation kinetics with a dissociation constant of 0.68 microg/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.
Zhao
Wen-Hua
WH
Department of Chemical Biology, Capital University of Medical Sciences, Beijing 100069, China.
Zhang
Jin-Feng
JF
Zhe-Wang
Zhang
Ying-Xia
YX
Tian
Wei-Xi
WX
D031002:Acer / Q000737:chemistry*; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D001688:Biological Products / Q000737:chemistry / Q000494:pharmacology*; D002392:Catechin / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D064429:Fatty Acid Synthases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D007700:Kinetics; D015394:Molecular Structure; D009369:Neoplasms / Q000201:enzymology / Q000473:pathology; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology; D018515:Plant Leaves / Q000737:chemistry; D011485:Protein Binding; D013997:Time Factors
D000970:Antineoplastic Agents; D001688:Biological Products; D004791:Enzyme Inhibitors; D010936:Plant Extracts; D002392:Catechin; D064429:Fatty Acid Synthases