Aliskiren Copper(II) Complex. Synthesis and Antioxidant Activity

IF 1.1 4区化学 Q3 CHEMISTRY, MULTIDISCIPLINARY

Journal of the Mexican Chemical Society Pub Date : 2024-02-01 DOI:10.29356/jmcs.v68i2.1981

Nadir Jori, M. S. Islas, E. Ferrer, Patricia Ana María Williams

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引用次数: 0

Abstract

Abstract. Aliskiren (Alk) is a highly selective competitive inhibitor of renin used for the treatment of hypertension and related cardiovascular diseases. With the aim of improving its biological properties by the strategy of the induction of favorable conformational changes, we designed a metal-based drug. In this work we report the synthesis of a solid copper(II) complex with aliskiren, CuAlk, and its characterization in solution and solid-state. Moreover, and based on the association of hypertension with elevated levels of reactive oxygen species (ROS), the antioxidant properties of CuAlk were studied measuring the activities against 2,2-diphenyl-1-picrilhidrazil (DPPH·), hydroxyl (OH·) and peroxyl (ROO·) radicals, in addition to its superoxide dismutase (SOD) simil activity. Both the ligand and the complex were able to scavenge hydroxyl radicals, but upon complexation, the SOD mimetic activity of the ligand is enhanced. Resumen. El Aliskiren (Alk) es un inhibidor por competencia altamente selectivo de la renina que se utiliza en el tratamiento de la hipertensión y enfermedades cardiovasculares relacionadas. Se diseñó un metalofármaco con la idea de mejorar las propiedades biológicas mediante la inducción de cambios conformacionales favorables. En este trabajo se reporta la síntesis de un complejo sólido de cobre(II) con aliskiren, CuAlk, junto con su caracterización en fase sólida y en solución. Además, de acuerdo con la relación que existe entre la hipertensión y los niveles elevados de especies reactivas de oxígeno (ROS), se estudian las propiedades antioxidantes del CuAlk frente a los radicales 2,2-difenil-1-picrilhidracilo (DPPH·), hidroxilo (OH·) y peroxilo (ROO·), además de la actividad superóxido dismutasa símil (SOD). Tanto el ligando, como el complejo fueron capaces de secuestrar radicales hidroxilos, pero, luego de la complejación, se mejoró la actividad SOD símil del ligando.

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阿利吉仑铜（II）复合物。合成与抗氧化活性

摘要阿利吉仑（Alk）是一种高选择性竞争性肾素抑制剂，用于治疗高血压和相关心血管疾病。为了通过诱导有利构象变化的策略改善其生物特性，我们设计了一种金属基药物。在这项工作中，我们报告了与阿利吉仑的固体铜（II）配合物 CuAlk 的合成及其在溶液和固体状态下的表征。此外，基于高血压与活性氧（ROS）水平升高的关系，我们还研究了 CuAlk 的抗氧化特性，测量了其对 2,2-二苯基-1-苦基肼（DPPH-）、羟基（OH-）和过氧自由基（ROO-）的活性，以及其类似超氧化物歧化酶（SOD）的活性。配体和络合物都能清除羟自由基，但络合后，配体的 SOD 模拟活性增强。小结阿利吉仑（Alk）是一种高选择性竞争性肾素抑制剂，用于治疗高血压和相关心血管疾病。设计金属药物的目的是通过诱导有利的构象变化来改善其生物特性。在这项研究中，报告了一种与阿利吉仑的固态铜（II）配合物 CuAlk 的合成及其在固相和溶液中的表征。此外，根据高血压与活性氧（ROS）水平升高之间的关系，研究了 CuAlk 对 2,2-二苯基-1-苦基肼（DPPH-）、羟基（OH-）和过氧自由基（ROO-）的抗氧化特性以及超氧化物歧化酶模拟酶（SOD）的活性。配体和络合物都能清除羟自由基，但络合后，配体的模拟 SOD 活性增强。

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来源期刊

Journal of the Mexican Chemical Society 化学-化学综合

CiteScore

2.00

自引率

0.00%

发文量

审稿时长

6-12 weeks

期刊介绍： The Journal of the Mexican Chemical Society (J. Mex. Chem. Soc.) is a scientific, blind, peer reviewed, and open access, free of charge publication that covers all areas of chemistry and its sub-disciplines (i.e. medicinal chemistry, natural products, electrochemistry, material science, computational chemistry, organic chemistry, bionirganic chemistry, etc). It is devoted to facilitating the worldwide advancement of our understanding of chemistry. It will primarily publish original contributions of research in all branches of the theory and practice of chemistry in its broadest context as well as critical reviews in active areas of chemical research where the author has published significant contribution. The J. Mex. Chem. Soc. is a quarterly publication which language of submission and publication is English. To be suitable for publication in J. Mex. Chem. Soc., manuscripts must describe novel aspects of chemistry, high quality of results and discussion an excellent bibliographic support, and contribute to the development of the field. Routine or incremental work are not suitable for publication in J. Mex. Chem. Soc. Authors are encouraged to send contributions in electronic form. Our online submission system guides you stepwise through the process of entering your article details and uploading your files.