超氧自由基的微分子抑制剂

L. Andronache, V. Pantea, A. Gulea, Inna Svet, Vasilii Graur, Valerii Matcovschi, M. Gamaniuc, V. Gudumac
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引用次数: 0

摘要

背景:目前,人们对新的铜(Cu2+)杂环配位化合物(CC),异硫杂环叠氮化物衍生物越来越感兴趣,它们表现出多种有益的性质,但它们对与自由基(如超氧自由基)反应的影响尚未研究。材料与方法:采用分光光度法测定了氯化铜(Cu2+)和溴化铜与n-(丙-2-烯-1-基)-2-(吡啶-2-基亚甲基)肼-碳酰亚胺基硫代甲酯的新型微分子配合物对超氧自由基的捕获活性。结果:发现氯化铜和溴化物与n-(丙-2-烯-1-基)-2-(吡啶-2-基亚甲基)肼-碳酰亚胺基硫代甲酯的微分子配合物在与超氧化物自由基相互作用时具有较强的超氧化物自由度抑制剂性能。除此之外,所研究化合物的IC50取决于配合物内部酸性配体的性质,并按以下顺序增加:Cl-–Br-。结论:上述化合物的既定性质是新的,因为到目前为止,它们作为超氧化物自由基的小分子抑制剂的用途还没有描述。合成的CC扩大了具有高生物活性的超氧化物自由基抑制剂的库。讨论了它们对开发与超氧化物自由基过量产生相关的疾病的新治疗策略的可能意义。
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Micromolecular inhibitors of superoxide radicals
Background: Currently, there is a growing interest in new copper (Cu2+) heterocyclic coordination compounds (CC), isothiosemicarbazide derivates, which demonstrated multiple beneficial properties, but their effect on reactions with free radicals such as the superoxide radical has not been investigated. Material and methods: The action of new micromolecular complexes of copper (Cu2+) chloride and bromide with methyl n- (prop-2-en-1-yl) -2- (pyridin2-ylmethylidene) hydrazine carbimidothioate on capturing activity of the superoxide radical was determined by the spectrophotometric method in vitro experiments. Results: It was established that the micromolecular complexes of copper (II) chloride and bromide with methyl n-(prop-2-en-1-yl)-2-(pyridin-2- ylmethylidene) hydrazine carbimidothioate have been found to possess strong superoxide radical inhibitor properties when interacting with a superoxide radical. In addition to this, the IC50 of the studied compounds depends on the nature of the acid-ligand in the internal sphere of the complex and increases in the following sequence: Cl- –Br- . Conclusions: The established property of mentioned compounds is new, because their use as micromolecular inhibitors of superoxide radicals has not been described so far. The synthesized CC expand the arsenal of superoxide radical inhibitors with high biological activity. Their possible significance for the development of new treatment strategies for diseases associated with the overproduction of superoxide radicals is discussed.
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