A Metallo Pro‐Drug to Target CuII in the Context of Alzheimer's Disease,Chemistry - A European Journal

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A Metallo Pro‐Drug to Target CuII in the Context of Alzheimer's Disease
Chemistry - A European Journal ( IF 3.9 ) Pub Date : 2018-02-16 , DOI: 10.1002/chem.201706049
Amandine Conte-Daban _{1,

2} , Vinita Ambike ₃ , Régis Guillot ₃ , Nicolas Delsuc ₄ , Clotilde Policar ₄ , Christelle Hureau _{1,

2}

Affiliation

Alzheimer's disease and oxidative stress are connected. In the present communication, we report the use of a Mn^II‐based superoxide dismutase (SOD) mimic ([Mn^II(L)]⁺, 1⁺) as a pro‐drug candidate to target Cu^II‐associated events, namely, Cu^II‐induced formation of reactive oxygen species (ROS) and modulation of the amyloid‐β (Aβ) peptide aggregation. Complex 1⁺ is able to remove Cu^II from Aβ, stop ROS and prevent alteration of Aβ aggregation as would do the corresponding free ligand LH. Using 1⁺ instead of LH in further biological applications would have the double advantage to avoid the cell toxicity of LH and to benefit from its proved SOD‐like activity.

中文翻译：

一种在阿尔茨海默病中靶向 CuII 的金属前药

阿尔茨海默病和氧化应激密切相关。在本通讯中，我们报告了使用基于 Mn ^II的超氧化物歧化酶 (SOD) 模拟物 ([Mn ^II (L)] ⁺ , 1 ⁺ ) 作为前药候选物来靶向 Cu ^II相关事件，即Cu ^II诱导活性氧 (ROS) 的形成和淀粉样蛋白-β (Aβ) 肽聚集的调节。复合物1 ⁺能够从 Aβ 中去除 Cu ^II ，阻止 ROS 并防止 Aβ 聚集的改变，就像相应的游离配体 LH 一样。在进一步的生物学应用中使用1 ⁺代替 LH 将具有双重优势，既可以避免 LH 的细胞毒性，又可以从其经过验证的 SOD 样活性中受益。

更新日期：2018-02-16

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