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氯碘羟喹,一种专门干扰脑金属代谢的治疗阿尔茨海默病的药物:其二价锌和二价铜配合物的结构表征

Clioquinol, a drug for Alzheimer's disease specifically interfering with brain metal metabolism: structural characterization of its zinc(II) and copper(II) complexes.

作者信息

Di Vaira Massimo, Bazzicalupi Carla, Orioli Pierluigi, Messori Luigi, Bruni Bruno, Zatta Paolo

机构信息

Department of Chemistry, University of Florence, via della Lastruccia 3, Sesto Fiorentino, Florence, Italy.

出版信息

Inorg Chem. 2004 Jun 28;43(13):3795-7. doi: 10.1021/ic0494051.

Abstract

Clioquinol, a 8-hydroxyquinoline derivative, is producing very encouraging results in the treatment of Alzheimer's disease (AD). Its biological effects are most likely ascribed to complexation of specific metal ions, such as copper(II) and zinc(II), critically associated with protein aggregation and degeneration processes in the brain. We report here, for the first time, a structural characterization of the zinc(II) and copper(II) complexes of clioquinol. A ligand to metal stoichiometry of 2:1 is found in both cases, though in the presence of quite different coordination polyhedra. The present findings are discussed in the frame of modern approaches to AD treatment.

摘要

氯碘羟喹是一种8-羟基喹啉衍生物,在治疗阿尔茨海默病(AD)方面正产生非常令人鼓舞的结果。其生物学效应很可能归因于与大脑中蛋白质聚集和变性过程密切相关的特定金属离子(如铜(II)和锌(II))的络合。我们在此首次报告氯碘羟喹的锌(II)和铜(II)配合物的结构表征。在两种情况下都发现配体与金属的化学计量比为2:1,尽管存在相当不同的配位多面体。本文的研究结果在现代AD治疗方法的框架内进行了讨论。

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