In vitro detection of breast and cervical cancer cells using a novel fluorescent choline derivative

Introduction Cervical and breast cancers can be easily preventable but they still represent the main causes of cancer-related deaths of women worldwide. Detecting cancer at its early stages is key since treatment of pre-invasive lesions is more efficient than treating an invasive disease. However, there no screening method that is highly sensitive and specific, as well as affordable and practical is currently available. Therefore, the identification of markers complementing traditional cyto/histopathological assessments is needed. Alterations in choline metabolism represents a hallmark of many malignancies, including cervical and breast cancers. Choline radiotracers are widely used for several imaging purposes for the detection of tumours, even though there are many risks associated with the use of radioactivity. Therefore, the aim of this work was to synthesize and characterize a choline tracer based on fluorinated acridine scaffold (CFA) for the in vitro detection of cervical and breast cancer cells. Methods CFA was synthesized, fully characterized and tested for cytotoxicity on breast (MCF-7) and cervical (HeLa) cancer cell lines. CFA’s uptake by cancer cells was investigated by confocal microscopy and its intracellular intensity was studied by fluorescence means; a comparative uptake between living normal and cancer cells was also conducted. Results An enhanced intensity of CFA was recorded in breast cancer cells compared to cervical cancer cells in both confocal and fluorescence microscope analysis ( p ≤ 0.001). Weak signal intensity of CFA was recorded in normal cells ( p ≤ 0.0001). CFA was toxic at much higher concentrations (HeLa IC ₅₀ = 200 ±18 µM and MCF-7 IC ₅₀ =105 ±3 µM) than the one needed for its detection in cancer cells (5 µM). Conclusions Results showed that CFA preferentially accumulated in cancer cells rather than in normal ones. This suggests that CFA may be a potential diagnostic probe in discriminating healthy tissues from malignant ones, due to its specific and highly sensitive features; CFA may also represent a useful tool for in vitro investigations of choline metabolism in cervical and breast cancers.