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新型含硫和硒的吩嗪酸钾类似物对HO诱导的肿瘤细胞细胞毒性的抗氧化活性

Antioxidant Activity of New Sulphur- and Selenium-Containing Analogues of Potassium Phenosan against HO-Induced Cytotoxicity in Tumour Cells.

作者信息

Klyushova Lyubov S, Kandalintseva Natalya V, Grishanova Alevtina Y

机构信息

Institute of Molecular Biology and Biophysics, Federal Research Center of Fundamental and Translational Medicine, 2/12 Timakova Str., 630060 Novosibirsk, Russia.

Department of Chemistry, Novosibirsk State Pedagogical University, 28 Vilyuyskaya Str., 630126 Novosibirsk, Russia.

出版信息

Curr Issues Mol Biol. 2022 Jul 7;44(7):3131-3145. doi: 10.3390/cimb44070216.

Abstract

Among known phenolic antioxidants, the overwhelming majority of compounds have lipophilic properties and the number of known water-soluble compounds is very small. The list of hydrophilic phenolic antioxidants can be expanded via the synthesis of a structurally related series of polyfunctional compounds for further research on their biological activity in vitro. New sulphur- and selenium-containing analogues of antioxidant potassium phenosan were synthesised. In vitro cytotoxicity and cytostaticity as well as antioxidant activity against HO-induced cytotoxicity to human cell lines (HepG2, Hep-2 and MCF-7) were investigated by high-content analysis. A selenium-containing analogue showed higher biological activity than did a sulphur-containing one. As compared to the activity of potassium phenosan, the selenium-containing analogue had a cell line-dependent antioxidant effect against HO-induced cytotoxicity: comparable in HepG2 cells and greater in Hep-2 cells. The selenium-containing analogue significantly increased the death of MCF-7 cells at concentrations above 50 µM. The sulphur-containing analogue has lower biological activity as compared to potassium phenosan and the selenium-containing analogue.

摘要

在已知的酚类抗氧化剂中,绝大多数化合物具有亲脂性,而已知的水溶性化合物数量很少。通过合成一系列结构相关的多官能化合物,可以扩充亲水性酚类抗氧化剂的清单,以便进一步研究它们在体外的生物活性。合成了抗氧化剂苯氧山酸钾的新型含硫和含硒类似物。通过高内涵分析研究了它们的体外细胞毒性和细胞生长抑制作用,以及对羟基自由基(HO)诱导的对人细胞系(HepG2、Hep-2和MCF-7)细胞毒性的抗氧化活性。一种含硒类似物显示出比含硫类似物更高的生物活性。与苯氧山酸钾的活性相比,含硒类似物对HO诱导的细胞毒性具有细胞系依赖性的抗氧化作用:在HepG2细胞中相当,在Hep-2细胞中更强。含硒类似物在浓度高于50μM时显著增加了MCF-7细胞的死亡。与苯氧山酸钾和含硒类似物相比,含硫类似物具有较低的生物活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e8db/9317250/ec5c680733fc/cimb-44-00216-g001.jpg

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