| Autor: |
Magklaras AC; Laboratory of Biological Inorganic Chemistry, Department of Chemistry, University of Ioannina, 45110 Ioannina, Greece., Banti CN; Laboratory of Biological Inorganic Chemistry, Department of Chemistry, University of Ioannina, 45110 Ioannina, Greece., Hadjikakou SK; Laboratory of Biological Inorganic Chemistry, Department of Chemistry, University of Ioannina, 45110 Ioannina, Greece. |
| Jazyk: |
angličtina |
| Zdroj: |
International journal of molecular sciences [Int J Mol Sci] 2023 Jan 29; Vol. 24 (3). Date of Electronic Publication: 2023 Jan 29. |
| DOI: |
10.3390/ijms24032563 |
| Abstrakt: |
The antiproliferative activity of three antibiotics clinically use, was studied through DNA inhibition mechanisms, ex vivo, in silico and in vitro. The ex vivo interaction of DNA with ciprofloxacin hydrochloride ( CIP·HCl ), penicillin G sodium salt ( PEN·Na ), and tetracycline hydrochloride ( TC·HCl ) was determined by UV-Vis spectra and viscosity measurements. Furthermore, their binding constants ( K b ) toward CT-DNA were calculated ( K b = (2.8 ± 0.6) × 10 4 ( CIP·HCl ), (0.4 ± 0.1) × 10 4 ( PEN·Na ) and (6.9 ± 0.3) × 10 4 ( TC·HCl ) Μ -1 ). Docking studies on the binding interactions of antibiotics with DNA were performed to rationalize the ex vivo results. The in vitro antiproliferative activity of the antibiotics was evaluated against human breast adenocarcinoma (MCF-7) cells (IC 50 values: 417.4 ± 28.2 ( CIP·HCl ), >2000 ( PEN·Na ) and 443.1 ± 17.2 ( TC·HCl ) μΜ). Cell cycle arrest studies confirmed the apoptotic type of MCF-7 cells. The toxicity of the studied agents was in vitro tested against human fetal lung fibroblast cells (MRC-5). The results are compared with the corresponding one for doxorubicin ( DOX ). Despite their low binding affinity to DNA ( K b ) or their different mode of interaction, TC·HCl (anthracycline) or CIP·HCl (quinolones), exhibit notable antiproliferative activity and low toxicity. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
|
|
Nepřihlášeným uživatelům se plný text nezobrazuje |
K zobrazení výsledku je třeba se přihlásit.
|
