氨基酸羟胺钒配合物的合成、表征及对PTP1B酶的抑制活性

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20 μg/mL时对PTP1B酶的抑制率达到90.51%.

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

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).