The influence of some promising fused azaisocytosine-containing congeners on zebrafish (Danio rerio) embryos/larvae and their antihaemolytic, antitumour and antiviral activities

European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences
Małgorzata SztankeMałgorzata Polz-Dacewicz

Abstract

The present study was aimed at broadening the profile of toxicity and biological activity of promising fused azaisocytosine-containing congeners (I-VI) possessing medical applicability and important pharmacokinetic properties. For this purpose, the in vivo zebrafish test was applied for evaluating embryotoxic effects of test compounds, whereas the ex vivo model of oxidatively-stressed rat erythrocytes was developed for assessing their antihaemolytic activities. Additionally, the MTT-based assays suitable for assessing cytotoxic and antiviral activities of I-VI were employed. The influence of compounds I-VI on zebrafish embryos/larvae was carefully investigated in relation to lack or presence of various substituents at the phenyl moiety. The least embryotoxic proved to be the parent compound (I) and its para-methyl (II) and ortho-chloro (III) derivatives. Simultaneously, they revealed the minimum embryotoxic concentrations higher than that of aciclovir, what makes them safer than this pharmaceutic. Moreover, most of test compounds showed protective effects (better or comparable to that of ascorbic acid) on oxidatively-stressed erythrocytes. All the investigated compounds were effective at inhibiting the growth of human solid tum...Continue Reading

Citations

Jan 26, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Małgorzata JanickaKrzysztof Sztanke
Oct 5, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·František ZálešákJakub Stýskala
Jan 5, 2021·Journal of Enzyme Inhibition and Medicinal Chemistry·Małgorzata SztankeKrzysztof Sztanke

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