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Biocompatibility and bioactivity study of a cytostatic drug belonging to the group of alkylating agents of the triazine derivative class
Journal of Molecular Liquids ( IF 5.3 ) Pub Date : 2021-09-22 , DOI: 10.1016/j.molliq.2021.117630
Olga V. Mikolaichuk 1 , Vladimir V. Sharoyko 1, 2 , Elena A. Popova 2 , Alexandra V. Protas 2 , Alexander V. Fonin 3 , Lubov V. Vasina 2 , Yurii A. Anufrikov 1 , Mikhail D. Luttsev 2 , Iuliia A. Nashchekina 3 , Anna M. Malkova 1, 2 , Grigorii V. Tochilnikov 4 , Sergei V. Ageev 1, 2 , Konstantin N. Semenov 1, 2
Affiliation  

The article describes the study of biocompatibility and bioactivity of a cytostatic agent [5-[[4,6-bis(aziridin-1-yl)-1,3,5-triazin-2-yl]amino]-2,2-dimethyl-1,3-dioxan-5-yl]methanol (substance (a)). The compound was characterised by means of 1H and 13C NMR spectroscopy, IR spectroscopy, mass spectrometry. Biomedicinal investigations included haemocompatibility studies (spontaneous haemolysis, platelet aggregation, plasma-coagulation haemostasis, binding with human serum albumin and DNA); determination of antioxidant properties (reaction with 2,2-diphenyl-1-picrylhydrazyl, photo-induced haemolysis, photodynamic properties, NO-radical uptake); genotoxicity, as well as cytotoxicity using HEK-293, A549, PA-1, T98G, SK-HEP-1, PANC-1 cell lines. The article shows two possible mechanisms of the cytostatic action of the substance (a): due to its antioxidant activity and the possibility of the formation of adducts with DNA.



中文翻译:

属于三嗪衍生物类烷化剂组的细胞抑制药物的生物相容性和生物活性研究

文章描述了细胞抑制剂[5-[[4,6-(氮丙啶-1-基)-1,3,5-三嗪-2-基]氨基]-2,2-的生物相容性和生物活性的研究二甲基-1,3-二恶烷-5-基]甲醇(物质(a))。该化合物通过1 H 和13碳谱、红外光谱、质谱。生物医学研究包括血液相容性研究(自发性溶血、血小板聚集、血浆凝固止血、与人血清白蛋白和 DNA 的结合);抗氧化特性的测定(与 2,2-diphenyl-1-picrylhydrazyl 的反应、光致溶血、光动力特性、NO-自由基吸收);基因毒性,以及使用 HEK-293、A549、PA-1、T98G、SK-HEP-1、PANC-1 细胞系的细胞毒性。该文章显示了物质 (a) 的细胞抑制作用的两种可能机制:由于其抗氧化活性和与 DNA 形成加合物的可能性。

更新日期:2021-09-27
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