مطالعه اثر سيتوتوكسيك بعضي از مشتقات جديد نورفلوكساسين بر رشد و تكثير رده هاي سلول سرطان انساني در محيط كشت

In Vitro study of cytotoxic effects of new Norfloxacin derivatives on human cancer cell lines

Objectives: In this in vitro study a series of new norfloxacin derivatives with an oxime or a substituted oxime attached to the piperazine ring at C-7 position were evaluated for their cytotoxicity on Human Cancer Cell Lines Materials and Methods: The growth inhibitory activity of these compounds was determined for human cancer cell lines including bladder carcinoma (EJ138), renal adenocarcinoma (ACHN), breast adenocarcinoma (MCF-7), hepatocyte carcinoma (HEPG2), lung carcinoma (A549) and rat-Adrenal fibroblast-pheochromocytoma (PC-12) using colorimetric MTT assay. Results: The results showed that the norfloxacin derivatives tested in this study showed significant inhibitory activity for cancer cell lines. Some of the compounds such as Cl, C9, C10 and C11 exhibited the most inhibitory activity against MCF-7 and PC-12 with 1C50 value of 9 µM (p<0.05). Among the cell lines tested, PC-12 was very sensitive to these compounds. The known cytotoxic drug, Etoposide, demonstrated the most significant activities against all the cell lines tested with 1C50 value less than 1.7 µM (p<0.001). Conclusion: The results indicated that the synthesized norfloxacin derivatives tested in this study, although they act mostly as antibacterial agents, they can also affect the function of the type 2 DNA topoisomerase in eukaryotic cells. Further studies are needed to elucidate the mechanisms by which these derivatives act.