Study on the interaction of 4'-hydroxychalcones and their Mannich derivatives with calf thymus DNA by TLC and spectroscopic methods, a DNA cleavage study
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Data
2020
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Resumo
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.
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Palavras-chave
Chalcones, Hydroxychalcones, Mannich bases, DNA binding, UV-Vis spectroscopy, DNA cleavage
Citação
ROZMER, Zsuzsanna; BERNARDES, Aline; PÉREZ, Caridad N.; PERJÉSI, Pal. Study on the interaction of 4'-hydroxychalcones and their Mannich derivatives with calf thymus DNA by TLC and spectroscopic methods, a DNA cleavage study. The Open Medicinal Chemistry Journal, [s. l.], v. 14, p. 122-131, 2020. DOI: 10.2174/1874104502014010122. Disponível em: https://openmedicinalchemistryjournal.com/VOLUME/14/PAGE/122/. Acesso em: 24 ago. 2023.