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金(I)配合物中的聚集与生物活性:一个未被探索的概念

Aggregation versus Biological Activity in Gold(I) Complexes. An Unexplored Concept.

作者信息

Pinto Andrea, Roma-Rodrigues Catarina, Ward Jas S, Puttreddy Rakesh, Rissanen Kari, Baptista Pedro V, Fernandes Alexandra R, Lima João Carlos, Rodríguez Laura

机构信息

Departament de Química Inorgànica i Orgànica, Secció de Química Inorgànica, Universitat de Barcelona, Martí i Franquès 1-11, E-08028 Barcelona, Spain.

Institut de Nanociència i Nanotecnologia (IN2UB). Universitat de Barcelona, 08028 Barcelona, Spain.

出版信息

Inorg Chem. 2021 Dec 20;60(24):18753-18763. doi: 10.1021/acs.inorgchem.1c02359. Epub 2021 Nov 1.

DOI:10.1021/acs.inorgchem.1c02359
PMID:34719915
Abstract

The aggregation process of a series of mono- and dinuclear gold(I) complexes containing a 4-ethynylaniline ligand and a phosphane at the second coordination position (PR-Au-C≡CCH-NH, complexes -, and (diphos)(Au-C≡CCH-NH), complexes -), whose biological activity was previously studied by us, has been carefully analyzed through absorption, emission, and NMR spectroscopy, together with dynamic light scattering and small-angle X-ray scattering. These experiments allow us to retrieve information about how the compounds enter the cells. It was observed that all compounds present aggregation in fresh solutions, before biological treatment, and thus they must be entering the cells as aggregates. Inductively coupled plasma atomic emission spectrometry measurements showed that mononuclear complexes are mainly found in the cytosolic fraction; the dinuclear complexes are mainly found in a subsequent fraction composed of nuclei and cytoskeleton. Additionally, dinuclear complex affects the actin aggregation to a larger extent, suggesting a cooperative effect of dinuclear compounds.

摘要

我们之前对一系列在第二配位位置含有4-乙炔基苯胺配体和膦的单核和双核金(I)配合物(PR-Au-C≡CCH-NH,配合物 - ,以及(diphos)(Au-C≡CCH-NH),配合物 - )的生物活性进行了研究,通过吸收光谱、发射光谱、核磁共振光谱以及动态光散射和小角X射线散射对其聚集过程进行了仔细分析。这些实验使我们能够获取有关化合物如何进入细胞的信息。观察到所有化合物在生物处理之前的新鲜溶液中都会发生聚集,因此它们必定是以聚集体的形式进入细胞。电感耦合等离子体原子发射光谱测量表明,单核配合物主要存在于胞质部分;双核配合物主要存在于随后由细胞核和细胞骨架组成的部分中。此外,双核配合物 对肌动蛋白聚集的影响更大,表明双核化合物具有协同作用。

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