Anticancer Properties of Fluorinated Aminophenylhydrazines on A549 Lung Carcinoma Cell Line

Abstract

Background: Non-small cell lung cancer (NSCLC) is responsible for up to 85% of deaths associated with lung cancer. Chemotherapy is still an important treatment method on the treatment of inoperable cases. In this study, the anticancer properties of a series of Schiff bases were tested on the A549 cell line representing NSCLC. Methods: Fluorinated Schiff bases (compounds 1-6) were synthesized based on 2-amino phenylhydrazines and benzaldehydes containing fluorine were used. The cytotoxic effects of the compounds on the A549 cell line were determined by colorimetric MTT assay and the antiproliferative effects of the compounds on the A549 cell line by the CFSE method. To demonstrate the development of apoptosis, cleaved caspase-3 expression in cells was tested using the immunofluorescence method. Morphological changes indicating apoptosis in cells were determined by histopathological staining methods (H & E, giemza, PAP). Results: The strongest cytotoxic effect on A549 lung cancer cells was obtained with compound 6 (IC50: 0.64 μM) containing 5 fluorine atoms. The strongest antiproliferative effect on A549 cells was achieved with compound 5 (PI: 4.95) carrying 2 fluorine atoms. Apoptosis induction was effective in cell death. In addition to cleaved caspase-3 expression, chromatin condensation, marginalization, and apoptotic bodies were observed in the cells. Conclusion: Some of the compounds tested showed high cytotoxic and antiproliferative effects, indicating that these compounds could be potential chemotherapeutic agent candidates for lung cancer. The result of immunofluorescence and immunohistochemical analysis showing that the cytotoxic effects have been induced by apoptosis is an important advantage.

Keywords

• Schiff bases
• IC50
• A549
• Lung cancer
• Apoptosis