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  • Research PaperImmunobiological efficacy and immunotoxicity of novel synthetically prepared fluoroquinolone ethyl 6-fluoro-8-nitro-4-oxo-1,4-dihydroquinoline-3-carboxylate

  • Add time:09/09/2019    Source:sciencedirect.com

    The present study examined the cytotoxicity, anti-cancer reactivity, and immunomodulatory properties of new synthetically prepared fluoroquinolone derivative 6-fluoro-8-nitro-4-oxo-1,4-dihydroquinoline-3-carboxylate (6FN) in vitro. The cytotoxicity/toxicity studies (concentrations in the range 1–100 μM) are focused on the cervical cancer cells HeLa, murine melanoma cancer cells B16, non-cancer fibroblast NIH-3T3 cells and reconstructed human epidermis tissues EpiDerm™. The significant growth inhibition of cancer cells HeLa and B16 was detected. The cytotoxicity was mediated via apoptosis-associated with activation of caspase-9 and -3. After 72 h of treatment, the two highest 6FN concentrations (100 and 50 μM) induced toxic effect on epidermis tissue EpiDerm™, even the structural changes in tissue were observed with concentration of 100 μM. The effective induction of RAW 264.7 macrophages cell-release of pro- and anti-inflammatory TH1, TH2 and TH17 cytokines, with anti-cancer and/or anti-infection activities, respectively, has been revealed even following low-dose exposition.

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    Prev:Polyfunctional 4-quinolinones. Synthesis of 2-substituted 3-hydroxy-4-oxo-1,4-dihydroquinolines
    Next:New approach to [a]-fused fluoroquinolones: the synthesis of 5-oxo-1,2,3,3a,4,5-hexahydropyrrolo[1,2-a]quinolines)

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