RESEARCH ARTICLE


Study on the Interaction of 4'-Hydroxychalcones and their Mannich Derivatives with Calf Thymus DNA by TLC and Spectroscopic Methods, a DNA Cleavage Study



Zsuzsanna Rozmer1, Aline Bernardes2, 3, Caridad N. Pérez3, Pál Perjési1, *
1 Institute of Pharmaceutical Chemistry, University of Pécs, Rókus str. 2., H-7624 Pécs, Hungary
2 Department of Education, Research and Extension, Federal Institute of Education, Science and Technology of Mato Grosso, 78050-560, Cuiabá-MT, Brazil
3 Institute of Chemistry, Federal University of Goiás, 74690-900 Goiánia-GO, Brazil


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Creative Commons License
© 2020 Rozmer et al.

open-access license: This is an open access article distributed under the terms of the Creative Commons Attribution 4.0 International Public License (CC-BY 4.0), a copy of which is available at: (https://creativecommons.org/licenses/by/4.0/legalcode). This license permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

* Address correspondence to this author at the Institute of Pharmaceutical Chemistry, University of Pécs, Rókus str. 2., H-7624Pécs, Hungary; E-mail: pal.perjesi@gytk.pte.hu


Abstract

Background:

Phenolic Mannich bases derived from hydroxychalcones show remarkable cytotoxic potencies towards cancer cell lines. However, the exact mechanism of action is still partially uncleared.

Objective:

Interaction of two hydroxychalcones and their Mannich derivatives with calf thymus DNA (ctDNA) has been investigated.

Methods:

Thin-layer chromatography and UV-Vis spectroscopic method were used for studying the interaction. The binding constant has been determined by UV-Vis spectrophotometric titration. The DNA cleavage activity of the compounds was studied by agarose gel electrophoresis.

Results:

Interaction of the compounds with ctDNA exhibited relatively high intrinsic binding constant (4-5x104 M-1). The results indicate existence of weak, non-covalent interactions between the investigated derivatives with ctDNA. Some compounds showed a slight DNA cleavage activity with pBR322.

Conclusion:

The obtained results provide additional knowledge on the previously documented cytotoxicity against tumor cell lines of the hydroxychalcones and their Mannich-derivatives.

Keywords: Chalcones, Hydroxychalcones, Mannich bases, DNA binding, UV-Vis spectroscopy, DNA cleavage.