Investigation of Selective Cytotoxicity and Determination of Ligand Induced Apoptosis of a New Acenaphtho[1,2-b]quinoxaline Derivative

Abstract

Several new acenaphtho[1,2-b] quinoxaline derivatives were prepared by the reaction of o-phenylenediamines with acenaphthenequinones. The response of different carcinoid cell lines to these compounds were evaluated by MTT (3-(4,5-dimethylthiazol-2-yl)2,5-diphenyl tetrazolium bromide) assay and trypan blue exclusion tests. The cytotoxicity of 3,4-dinitroacenaphtho[1,2-b]quinoxaline (III_d) on the tested cell lines was confirmed by both tests. Furthermore, the MTT test showed a significant difference (p < 0.05) between the cytotoxicity of this compound on malignant cell lines of Caco-2, HT-29, T47D and non malignant mouse fibroblast cell line of NIH-3T3. An apoptosis inducing effect of compound III_d on K562 cells was detected by flow cytometry using Annexin-V-fluorescein isothiocyanate (AnV-FITC) and propi-dium iodide (PI) staining. The apoptosis induction (PI−/AnV+) in treated K562 cells was significantly (p < 0.01) more at 0.5 µg/ml concentration of compound III_d in comparison to all other concentrations of this compound and also doxorubicin (CAS 25316-40-9) (250 nM).

Key words

Acenaphtho[1,2-b]quinoxaline, apoptosis induction, selective cytototoxicity - Anticancer agents

• References

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