Author/Authors :
Rozmer, Zsuzsanna Institute of Pharmaceutical Chemistry - University of Pécs, Rókus str. 2., Hungary , Bernardes, Aline Institute of Chemistry - Federal University of Goiás, 74690-900 Goiánia-GO, Brazil , Pérez, Caridad N. Institute of Chemistry - Federal University of Goiás, 74690-900 Goiánia-GO, Brazil , Perjési, Pál Institute of Pharmaceutical Chemistry - University of Pécs, Rókus str. 2., Hungary
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
