Inhibition effects of some bioactive peroxovanadium complexes on the tyrosine phosphatase
- 生命科学－已发表论文 
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(O-2)(2)L](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 V-51 NMR, C-13 NMR, IR and elemental analysis. The complexes displayed remarkable inhibitory effects on the bovine heart tyrosine phosphatase. Their IC50 were 0.22, 0.36, 0.90 and 0.28 mu mol/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.