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二吡啶甲酮异烟酰腙铜(II)配合物的合成:结构、抗癌活性及抗癌机制

Synthesis of Dipyridyl Ketone Isonicotinoyl Hydrazone Copper(II) Complex: Structure, Anticancer Activity and Anticancer Mechanism.

作者信息

Deng JunGang, Chen Wei, Deng Hang

机构信息

Affiliated Hospital, Guilin Medical College, 109 Huancheng North Road, Guilin, Guangxi, 541004, China.

出版信息

J Fluoresc. 2016 Nov;26(6):1987-1996. doi: 10.1007/s10895-016-1892-2. Epub 2016 Aug 3.

Abstract

In an effort to better understand the biological efficacy of the tridentate aroyl hydrazone Cu(II) complexes, the Cu(II) complex of di-2-pyridyl ketone isonicotinoyl hydrazone ligand (HL), {[Cu(L)(HO)]·HO·NO} (C1) was synthesized and characterized. Single crystal X-ray study reveals that complex C1 forms 1D zigzag chains in solid state. In water, the hydrolysis of the 1D zigzag chains was observed, and finally formation of monomeric species. In vitro studies revealed that complex C1 showed significantly more anticancer activity than the ligand alone. Investigation of the anticancer mechanisms of C1, confirmed that the Cu(II) complex exhibit a strong capacity to promote productions of reactive oxygen species (ROS), leading to caspase-dependent apoptotic cell death.

摘要

为了更好地理解三齿芳酰腙铜(II)配合物的生物学功效,合成并表征了二-2-吡啶基酮异烟酰腙配体(HL)的铜(II)配合物{[Cu(L)(HO)]·HO·NO}(C1)。单晶X射线研究表明,配合物C1在固态下形成一维之字形链。在水中,观察到一维之字形链的水解,最终形成单体物种。体外研究表明,配合物C1显示出比单独的配体显著更强的抗癌活性。对C1抗癌机制的研究证实,铜(II)配合物具有很强的促进活性氧(ROS)产生的能力,导致半胱天冬酶依赖性凋亡细胞死亡。

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