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首页> 外文期刊>Journal of biological inorganic chemistry: JBIC: a publication of the Society of Biological Inorganic Chemistry >Ternary oxovanadium(IV) complexes of ONO-donor Schiff base and polypyridyl derivatives as protein tyrosine phosphatase inhibitors: synthesis, characterization, and biological activities
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Ternary oxovanadium(IV) complexes of ONO-donor Schiff base and polypyridyl derivatives as protein tyrosine phosphatase inhibitors: synthesis, characterization, and biological activities

机译：作为蛋白质酪氨酸磷酸酶抑制剂的ONO供体Schiff碱和聚吡啶基衍生物的三价氧钒（IV）配合物：合成，表征和生物学活性

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摘要

A series of oxovanadium complexes with mixed ligands, a tridentate ONO-donor Schiff base ligand [viz., salicylidene anthranilic acid (SAA)], and a bidentate NN ligand [viz., 2,2'-bipyridine (bpy), 1,10-phenanthroline (phen), dipyrido[3,2-d:2',3'-f]quinoxaline (dpq), dipyrido[3,2-a:2',3'-c]phenazine (dppz), or 7-methyldipyrido[3,2-a:2',3'-c]phenazine (dppm)], have been synthesized and characterized by elemental analysis, electrospray ionization mass spectrometry, UV-vis spectroscopy, Fourier transform IR spectroscopy, EPR spectroscopy, and X-ray crystallography. Crystal structures of both complexes, [(VO)-O-IV(SAA)(bpy)]center dot 0.25bpy and [(VO)-O-IV(SAA)(phen)]center dot 0.33H(2)O, reveal that oxovanadium(IV) is coordinated with one nitrogen and two oxygen atoms from the Schiff base and two nitrogen atoms from the bidentate planar ligands, in a distorted octahedral geometry (VO3N3). The oxidation state of V(IV) with d (1) configuration was confirmed by EPR spectroscopy. The speciation of VO-SAA-bpy in aqueous solution was investigated by potentiomtreic pH titrations, and the results revealed that the main species are two ternary complexes at a pH range of 7.0-7.4, and one is the isolated crystalline complex. The complexes have been found to be potent inhibitors against human protein tyrosine phosphatase 1B (PTP1B) (IC50 approximately 30-61 nM), T-cell protein tyrosine phosphatase (TCPTP), and Src homology phosphatase 1 (SHP-1) in vitro. Interestingly, the [(VO)-O-IV(SAA)(bpy)] complex selectively inhibits PTP1B over the other two phosphatases (approximate ninefold selectivity against SHP-1 and about twofold selectivity against TCPTP). Kinetics assays suggest that the complexes inhibit PTP1B in a competitive and reversible manner. These suggest that the complexes may be promising candidates as novel antidiabetic agents.
机译：具有混合配体，三齿ONO供体席夫碱配体[即水杨基邻氨基苯甲酸（SAA）]和双齿NN配体[2,2'-联吡啶（bpy），1， 10-菲咯啉（phen），二吡ido并[3,2-d：2'，3'-f]喹喔啉（dpq），二吡ido并[3,2-a：2'，3'-c]吩嗪（dppz）或合成并通过元素分析，电喷雾电离质谱，紫外可见光谱，傅里叶变换红外光谱，EPR光谱合成了7-甲基二吡啶并[3,2-a：2'，3'-c]吩嗪（dppm）和X射线晶体学。 [（VO）-O-IV（SAA）（bpy）]中心点0.25bpy和[（VO）-O-IV（SAA）（phen）]中心点0.33H（2）O的两种配合物的晶体结构揭示氧杂钒（IV）在一个八面体几何形状（VO3N3）中与席夫碱的一个氮和两个氧原子以及二齿平面配体的两个氮原子配位。通过EPR光谱证实了d（1）构型的V（IV）的氧化态。通过电位滴定pH滴定法研究了水溶液中VO-SAA-bpy的形态，结果表明，主要种类是pH范围为7.0-7.4的两种三元络合物，一种是分离的结晶络合物。已发现该复合物是有效的抗人蛋白酪氨酸磷酸酶1B（PTP1B）（IC50约30-61 nM），T细胞蛋白酪氨酸磷酸酶（TCPTP）和Src同源磷酸酶1（SHP-1）的抑制剂。有趣的是，[（VO）-O-IV（SAA）（bpy）]复合物相对于其他两种磷酸酶选择性抑制PTP1B（对SHP-1的选择性约为9倍，对TCPTP的选择性约为2倍）。动力学测定表明，该复合物以竞争和可逆的方式抑制PTP1B。这些表明，该复合物可能是有希望的候选物，作为新型抗糖尿病药。

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