Özet:

Bioactive molecules with higher activation power are now needed instead of organic compounds that are widely used against drug resistance that threatens human health. The development of Schiff base (SB) compounds supported by the unique properties of the fluorine atom may increase the chances of curing of drug-resistant lung cancer and bacterial infections. A series of fluorinated salicylaldimine SB ligands (C1-10) were synthesized. Their anticancer effects on the A549 human lung carcinoma cell line and antibacterial effects on Escherichia coli, Staphylococcus aureus and Pseudomonas aeruginosa were tested by MTT (3-(4,5-dimethylthi azol-2-yl)-2, 5-diphenyltetrazolium bromide) assay. CFSE (5(6)-Carboxyfluoresceindiacetate N-succinimidyl ester) method was used to determine the proliferative indexes (PI) of the compounds on A549 cells. The apoptosis-induce capabilities of the compounds were determined by active caspase-3 analysis and mitochondrial membrane potential analysis using rhodamine123. Morphological changes indicating apoptosis in the cells were determined by standard Hematoxylin and eosin, Giemsa and Papanicolaou staining protocols. Three fluorine-bearing (F2,4,5-SAL) SB ligands (C7) showed stronger cytotoxic activity than DOX on A549 cells (1.4 to 1.9 µM, respectively). The antiproliferative effects of the compounds were weaker than DOX. Mitochondrial membrane potential, active caspase analysis together with cell morphology analyses proved that cell death occurred by induction of apoptosis. No significant antibacterial effects of the compounds were found on the bacterial strains.

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