Assessment of Immunomodulatory Activities and in vitro Toxicity of New Quinolone 7-ethyl 9-ethyl-6-oxo-6,9-dihydro[1,2,5]selenadiazolo[3,4-h]quinoline-7-carboxylate

ABSTRACT

Our previous studies on leukemia cells L1210 and cervical cancer HeLa cells revealed cytotoxic effects of the 7-ethyl 9-ethyl-6-oxo-6,9-dihydro[1,2,5]selenadiazolo[3,4-h]quinoline-7-carboxylate (E2h), a new synthetically prepared quinolone derivative, toward selected cancer cell lines. The aim of the present study was to examine the cytotoxicity of E2h toward next cell lines and tissues; that is, human cancer HL-60 and A549 cells, human non-cancer fibroblast BHNF-1 cells, and reconstructed human epidermis tissues. Further we investigated the immunomodulatory activity of E2h on murine macrophage RAW 264.7 cells. Selenadiazoloquinolone E2h induced specific antiproliferative/cytotoxic activity against leukemia HL-60 cells and is the potent inducer of apoptotic cell death. Quinolone derivative demonstrated the immunomodulatory activities on RAW 264.7 cell line murine macrophages. The immunobiological studies revealed time- and concentration-dependent effective immunomodulation of pro- and anti-inflammatory cytokines’ release and antiproliferative/cytotoxic effect following exposure of RAW 264.7 cells to E2h.

Abbreviations: DMEM, Dulbecco’s modified eagle medium; DMSO, Dimethylsulfoxide; EtBr, Ethidium bromide; PI, Propidium iodide; E2h, 7-ethyl 9-ethyl-6-oxo-6,9-dihydro[1,2,5]selenadiazolo[3,4-h]quinoline-7-carboxylate.

KEYWORDS:

• Anticancer
• apoptosis
• cytokines
• cytotoxicity
• HL-60
• immunomodulation
• proliferation
• quinolones

Funding

This work was supported by the Slovak Research and Development Agency under the contracts No. APVV-0038-11 and by the Scientific Grant Agency of the Slovak Republic (Projects VEGA/1/0041/15).

This contribution is the result of the project implementation: Infrastructure for biomedical research, ITMS 26230120008, supported by the Research & Development Operational Program funded by the ERDF.

Conflicts of interest

The authors declare that they have no competing interests.

Additional information

Funding

This work was supported by the Slovak Research and Development Agency under the contracts No. APVV-0038-11 and by the Scientific Grant Agency of the Slovak Republic (Projects VEGA/1/0041/15). This contribution is the result of the project implementation: Infrastructure for biomedical research, ITMS 26230120008, supported by the Research & Development Operational Program funded by the ERDF.