Inhibition Effects of
Some Bioactive Peroxovanadium Complexes on the Tyrosine Phosphatase
ZHOU Xing-Wang1,2, CHEN Zhong1, CHEN
Qing-Xi2, YE Jian-Liang1, HUANG Pei-Qiang1, WU
Qin-Yi1
( 1Department of Chemistry, 2Department of
Biology, Laboratory of Analytical Science for Material and Life Chemistry,
Xiamen University, Xiamen 361005, China )
Abstract In order to
study the structure-activity relationship and molecular mechanism of
insulin-mimetic peroxovanadium complexes, the low-molecular-weight BHPTPase
from bovine heart has been purified mainly by chromatography of DEAE-cellulose
and Sephadex G-75, which was showed homogenicity on SDS-PAGE. Four bioactive
peroxovanadium(pV) complexes bpV(ox), bpV(bipy), bpV(phen) and bpV(pic), [VO(O2)2L]n-,
where L = oxalic acid dianion(ox), bipyridine(bipy), 1,10-phenanthroline(phen),
pyridine-2-carboxylic acid(pic) have been synthesized； the bonding properties of
center metal and its ligand were characterized by 51V NMR, 13C
NMR, IR and elemental analysis. The complexes displayed remarkable inhibitory
effects on the bovine heart tyrosine phosphatase. Their IC50 were
0.22, 0.36 and 0.90 and 0.28 μmol/L, respectively. The structure-activity
relationship of the complexes were discussed by their oxidizing ability and
through the steric space hindrance of the organic ligands.
Key words peroxovanadium complexes； tyrosine phosphatase； inhibition； structure-activity
relationship
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