氨基酸羟胺钒配合物的合成、表征及对PTP1B酶的抑制活性

doi:10.3969/j.issn.0251-0790.2012.02.006

摘要/Abstract

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20 μg/mL时对PTP1B酶的抑制率达到90.51%.

关键词: 氨基酸羟胺氧钒配合物, 晶体结构, PTP1B酶抑制活性

Abstract: Two vanadium-amino acid-hydroxylamido complexes,[VO(NH₂O)₂(C₅H₁₀O₂N] (1) and K[VO(NH₂O)₂(C₆H₁₂NO₂N]₂Cl·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).

Key words: Vanadium-amino acid-hydroxylamido complex, Crystal structure, PTP1B inhibitory activity

中图分类号:

O614.5

TrendMD:

张恒强, 张其颖, 李佳, 刘东, 吴小芳, 单永奎. 氨基酸羟胺钒配合物的合成、表征及对PTP1B酶的抑制活性. 高等学校化学学报, 2012, 33(02): 243.

ZHANG Heng-Qiang, ZHANG Qi-Ying, LI Jia, LIU Dong, WU Xiao-Fang, SHAN Yong-Kui. Synthesis, Characterization and PTP1B Inhibitory Activity of the Vanadium Complexes with Amino-acids. Chem. J. Chinese Universities, 2012, 33(02): 243.

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