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
Phenolic Mannich bases derived from hydroxychalcones show remarkable cytotoxic potencies towards cancer cell lines. However, the exact mechanism of action is still partially uncleared.
Interaction of two hydroxychalcones and their Mannich derivatives with calf thymus DNA (ctDNA) has been investigated.
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.
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.
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.
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* Address correspondence to this author at the Institute of Pharmaceutical Chemistry, University of Pécs, Rókus str. 2., H-7624Pécs, Hungary; E-mail: email@example.com