XXII. BIOCHEMICKÝ ZJAZD - Jesseniova lekárska fakulta

Posters
110.
INTEraCTION of PLaSMID DNA aND MITOCHONDria WITH CYCLIC
CHaLCONE anaLOGUES
Miroslava Štefanišinová 1 , Mária Kožurková 2 , Vladimíra Tomečková 1 and
Mária Mareková 1
1
Department of Medical Chemistry, Biochemistry and Clinical Biochemistry,
UPJŠ - Faculty of Medicine, Tr. SNP 1, 040 01 Košice, Slovak Republic,
2
Department of Biochemistry, Institute of Chemistry, UPJŠ - Faculty of Science,
Moyzesova 11, 040 66 Košice, Slovak Republic
The binding of small molecules to DNA has been of great interest due to the understanding
of the drug-DNA interaction. Substituted chalcone (1) and its cyclic chalcone analogues:
indanone (2), tetralone (3), benzosuberone (4) with dimethylamino substituent in 2, 4
position are interesting as drugs with antitumor activity. The purpose of this study was
to investigate the interaction of DNA with new ligands (1 – 4) using by spectroscopy
methods. Ligand - DNA binding affinities and constants (K) of the DNA-drug complexes
were determined by UV-Vis and fluorescence spectrophotometric titration and CD spectroscopy.
Generally, these compounds bound to DNA and show significant decrease of
fluorescence and bathochromic shift of excitation and emission maxima compared to the
spectral characteristics of the free form of ligands in solution phase. The strong hypochromism,
extensive broadening, red-shifting and increased stability of DNA double helix
were observed when these derivatives where bound to DNA. The compounds have no
circular dichroism spectrum when are free in the solution but they induced CD spectrum
when they are in the complex with DNA. The helical band at 246 nm corresponding to
the DNA unwound extent exhibited decrease for all the compounds in the same order
as that of the binding affinity. This phenomenon could be due to the stabilization of the
right-handed B-form of DNA by intercalation.
Acknowledgments: This work was supported by grant project VEGA 1/0402/10
XXII. Biochemistry Congress, Martin
235