氨基酸羟胺钒配合物的合成、表征及对PTP1B酶的抑制活性  

Synthesis,Characterization and PTP1B Inhibitory Activity of the Vanadium Complexes with Amino-acids

作　　者：张恒强[1] 张其颖[1] 李佳[2] 刘东[1] 吴小芳[1] 单永奎[1] 

机构地区：[1]华东师范大学化学系,上海200062 [2]国家新药筛选中心,上海201203

出　　处：《高等学校化学学报》2012年第2期243-250,共8页Chemical Journal of Chinese Universities

基　　金：上海市科学技术委员会基础研究重点项目(批准号:11JC1403400;08JC1408600)资助

摘　　要：合成了2种羟胺氧钒配合物——缬(亮)氨酸羟胺氧钒,并通过元素分析、红外光谱、紫外光谱、热重分析及X射线单晶衍射对其结构进行了表征.采用PTP1B酶筛选模型评价了它们及相关配合物的PTP1B酶抑制活性.实验结果表明,这2种配合物同属于三斜晶系,P1空间群,中心钒原子与7个配位的氮氧原子形成扭曲的五角双锥构型,进而通过氢键作用形成三维晶体结构.这2种配合物对PTP1B酶都表现出抑制活性,亮氨酸羟胺氧钒在浓度为20μg/mL时对PTP1B酶的抑制率达到90.51%.Two vanadium-amino acid-hydroxylamido complexes,（1） and K2Cl·H2O（2） were synthesized.Their structures and components were characterized by elemental analysis,IR spectrometry,UV-Vis spectrometry,thermal analysis and X-ray single crystal diffraction and their PTP1B inhibitory activities were also explored.Complexes 1 and 2 both crystallize in triclinic system with space group P1.The central vanadium and seven coordinated atoms form a distorted pentagonal bipyramidal.Two O atoms and three N atoms from hydroxylamine and amino-acids define an equatorial plane approximately perpendicular to V-O.The N of hydroxylamine is cis to N of amino-acids and the O of amino-acids is trans to V-O.Complex 2 displays a good inhibitory activity against PTP1B（inhibition rate is 90.51% at 20 μg/mL）.

关 键 词：氨基酸羟胺氧钒配合物 晶体结构 PTP1B酶抑制活性 

分 类 号：O614.5[理学—无机化学]