Biocompatibility and bioactivity study of a cytostatic drug belonging to the group of alkylating agents of the triazine derivative class
•Bioactivity and biocompatibility of a cytostatic drug belonging to a triazine derivative class were investigated.•The calculated value of a binding constant (Ka = 3.44⋅107 M−1) indicates the formation of covalent adducts with DNA.•High haemocompatibility and dose-dependent cytostatic activity towar...
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Veröffentlicht in: | Journal of molecular liquids 2021-12, Vol.343, p.117630, Article 117630 |
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Hauptverfasser: | , , , , , , , , , , , , |
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Sprache: | eng |
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Zusammenfassung: | •Bioactivity and biocompatibility of a cytostatic drug belonging to a triazine derivative class were investigated.•The calculated value of a binding constant (Ka = 3.44⋅107 M−1) indicates the formation of covalent adducts with DNA.•High haemocompatibility and dose-dependent cytostatic activity towards tumour cell lines were observed.
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. |
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ISSN: | 0167-7322 1873-3166 |
DOI: | 10.1016/j.molliq.2021.117630 |