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Study of the potential biological role of natural product derivatives as antioxidant and anticancer agents (Bachelor thesis)

Παπαδόπουλος, Γεώργιος/ Papadopoulos, Georgios

Introduction: Quinolones and fluoroquinolones are compounds of interest due to their use as antibiotics, as well as their potential antioxidant, anti-inflammatory, and anticancer activity. The chemical modification of the quinolone core increases research interest, as structural changes appear to affect their biological activity in conditions associated with oxidative stress or carcinogenesis. Aim: The aim of the present study is to investigate quinolone derivatives for potential antioxidant, anti-inflammatory, and anticancer activity. Methodology: To evaluate the biological activity of the compounds, the protocols of inhibition of the 2,2-diphenyl-1-picrylhydrazyl radical (DPPH), inhibition of lipid peroxidation by AAPH (2,2′-azobis-(2-amidinopropane)-dihydrochloride), inhibition of lipoxygenase (LOX), and determination of cell viability using the MTT method were applied. Results: In the DPPH assay, most compounds exhibited low to moderate activity, with ADER763 and ADKX462 being representative. In the AAPH assay, high inhibition was characteristically observed for ADMAK899, ADMAK895, and ADGM850, while in the LOX assay for ADGM850, ADKX466, ADMAK895, and ADER763. In the MTT assay, most compounds exhibited low cytotoxicity against HaCaT cells, while in A549 and A375 cells the activity was mainly moderate, with ADMAK896, ADMAK688, and ADMAK690 being representative. Conclusion: The compounds presented different activity profiles depending on their structure, concentration, and evaluation method. ADGM850, ADMAK895, and ADER763 are of particular interest regarding potential antioxidant and anti-inflammatory activity, as well as ADMAK896, ADMAK688, and ADMAK690 regarding potential anticancer activity.