活性过氧钒配合物对酪氨酸磷酸酶的抑制作用  

Inhibition Effects of Some Bioactive Peroxovanadium Complexes on the Tyrosine Phosphatase

作　　者：周兴旺[1] 陈忠[1] 陈清西 叶剑良[1] 黄培强[1] 吴钦义 

机构地区：[1]厦门大学化学系,厦门361005

出　　处：《生物化学与生物物理学报》2000年第2期133-138,共6页

基　　金：国家自然科学基金!重点项目资助!No .2 983 2 0 2 0;国家自然科学基金资助项目!No .196 0 5 0 0 4&&

摘　　要：为研究过氧钒配合物降血糖作用的构效关系规律和构效关系的分子机制 ,从牛心分离纯化了电泳纯的低分子量牛心酪氨酸磷酸酶 (BHPTPase)。合成并用51VNMR和13CNMR以及IR等谱学表征了 4种具有很强生物活性的过氧钒配合物K3[VO(O2 ) 2 (ox) ]·2H2 O、Na[VO(O2 ) 2 (bipy) ]·5H2 O、K[VO(O2 ) 2 ( phen) ]·3H2 O和K2 [VO(O2 ) 2 ( pic) ]·2H2 O。4种配合物对BHPTPase都有极显著的抑制作用 ,抑制强度的IC50 分别为 0 .2 2、0 .3 6、0 .90和0 .2 8μmol/L ,并根据实验结果讨论了过氧钒配合物的氧化能力和有机配体的空间位阻对构效关系的影响。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) 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 51 V NMR, 13 C NMR, IR and elemental analysis. The complexes displayed remarkable inhibitory effects on the bovine heart tyrosine phosphatase. Their IC 50 were 0.22, 0.36, 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.

关 键 词：过氧钒配合物 酪氨酸磷酸酶 抑制作用 构效关系 

分 类 号：Q55[生物学—生物化学]