In vitro study of redox properties of azolyl-lactones in human serum

IF 1 4区 化学 Q4 CHEMISTRY, MULTIDISCIPLINARY
M. Simic, J. Kotur-Stevuljević, Predrag Jovanovic, Milos Petkovic, M. Jovanovic, G. Tasic, V. Savić
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引用次数: 0

Abstract

Disruption of the redox balance in the body causes oxidative stress that can initiate many diseases. While antioxidants reduce the level of oxidizing compounds in the medium, prooxidants promote the opposite process and were used in therapies in particular those of cancer diseases. In this study, a series of azolyl lactones, were tested in human serum as a biological matrix and the obtained values of their oxy scores (OS) were compared. The antioxidative properties of these compounds were also tested under conditions of induced oxidative stress using an external prooxidant, t-butylhydroperoxide. The results showed that the sulphur analogue 4-azolyl coumarin 5 has the best antioxidant properties (OS -2.2), while the halogenated derivatives of pyrazolylcoumarin 7 and 8 act as prooxidant, but successfully resist oxidative stress (OS 2.7 and 2.0). Related phthalides and isocoumarins showed prooxidative properties, but azolyl isocoumarins 10 and 11 show the strongest resistance to oxidative stress, reflected in their negative oxy score value (OS -2.1 and OS -1.1). The results demonstrated that combining two pharmacophores with known redox properties can produce potent compounds in both directions, with the antioxidative and the prooxidative characteristics.
人血清中偶氮酰内酯氧化还原特性的体外研究
体内氧化还原平衡的破坏会引起氧化应激,从而引发许多疾病。虽然抗氧化剂降低了介质中氧化性化合物的水平,但促氧化剂促进了相反的过程,并被用于治疗,特别是癌症疾病。本研究将一系列偶氮酰内酯作为生物基质,在人血清中进行了检测,并比较了它们的氧分数(OS)。这些化合物的抗氧化性能也被测试在诱导氧化应激条件下使用外部促氧化剂,t-丁基过氧化氢。结果表明,含硫类似物4-偶氮基香豆素5具有最佳的抗氧化性能(OS -2.2),而吡唑基香豆素7和8的卤代衍生物具有促氧化作用,但能成功抵抗氧化应激(OS 2.7和2.0)。相关邻苯二甲酸酯和异香豆素具有促氧化特性,但偶氮基异香豆素10和11抗氧化能力最强,体现在其负氧评分值(OS -2.1和OS -1.1)上。结果表明,两种已知氧化还原性质的药效团结合可以产生具有抗氧化和促氧化特性的双向强效化合物。
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来源期刊
CiteScore
1.80
自引率
0.00%
发文量
76
审稿时长
1 months
期刊介绍: The Journal of the Serbian Chemical Society -JSCS (formerly Glasnik Hemijskog društva Beograd) publishes articles original papers that have not been published previously, from the fields of fundamental and applied chemistry: Theoretical Chemistry, Organic Chemistry, Biochemistry and Biotechnology, Food Chemistry, Technology and Engineering, Inorganic Chemistry, Polymers, Analytical Chemistry, Physical Chemistry, Spectroscopy, Electrochemistry, Thermodynamics, Chemical Engineering, Textile Engineering, Materials, Ceramics, Metallurgy, Geochemistry, Environmental Chemistry, History of and Education in Chemistry.
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