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Synthesis and characterization of mononuclear oxovanadium(IV) complexes and their enzyme inhibition studies with a carbohydrate metabolic enzyme phosphodiesterase I

机译:碳水化合物代谢酶磷酸二酯酶I的单核氧钒(IV)配合物的合成,表征及其酶抑制研究

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摘要

The increasing interest in vanadium coordination chemistry is based on its well-established chemical and biological functions. A beta-diketonato complex of oxovanadium(IV) is known to be having numerous catalytic applications and also exhibits promising insulin mimetic properties. In continuation of our structure activity relationship studies of metal complexes, we report herein the synthesis and characterization of the vanadium complexes of beta-diketonato ligand system with systematic variations of electronic and steric factors. Two complexes, VO(tmh)(2) (tmh = 2,2,6,6,-tetramethyl-3,5-heptanedione), and VO(hd)(2) (hd = 3,5-heptanedione) were synthesized and characterized by using different spectroscopic techniques. Elemental and mass spectral analysis supports the presence of two beta-diketonato ligands per VO(2+) unit. UV-Vis spectra in different solvents indicate coordination of coordinating solvent molecules at sixth position resulting in red shift of the band I transition. NMR and IR spectra reveal binding of coordinating solvent molecule at vacant sixth position trans to oxo group without releasing beta-diketonato ligands. Enzyme inhibition studies of these and other related oxovanadium(IV) complexes with beta-diketonato ligand system are conducted with snake venom phosphodiesterase I (SPVDE). All of these complexes showed significant inhibitory potential and were found to be non-competitive inhibitors against this enzyme.
机译:对钒配位化学的日益增长的兴趣是基于其完善的化学和生物学功能。已知氧钒(IV)的β-二酮基络合物具有多种催化应用,并且还显示出有希望的胰岛素模拟特性。在继续我们对金属配合物的结构活性关系研究的过程中,我们在此报告了β-二酮基配体系统中钒配合物的合成和表征,其中电子和位阻因素具有系统性变化。合成了两个配合物VO(tmh)(2)(tmh = 2,2,6,6,-四甲基-3,5-庚二酮)和VO(hd)(2)(hd = 3,5-庚二酮)并通过使用不同的光谱技术进行表征。元素和质谱分析支持每个VO(2+)单元存在两个β-二酮体配体。不同溶剂中的UV-Vis光谱表明配位溶剂分子在第六位置的配位导致带I跃迁的红移。 NMR和IR光谱揭示了在空位第六位的配位溶剂分子与氧代基团的结合,而没有释放β-二酮基配体。用蛇毒磷酸二酯酶I(SPVDE)对这些和其他相关的含钒-IV配体的氧钒(IV)复合物进行酶抑制研究。所有这些复合物均显示出显着的抑制潜能,并且被发现是对该酶的非竞争性抑制剂。

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