Cytotoxic Activity of N, N’-Bis (2-hydroxybenzyl) ethylenediamine Derivatives in Human Cancer Cell Lines

Abstract

Background: Compounds containing ethylenediamine (−NCH₂CH₂N-) moiety are known to exhibit antimicrobial, -fungal, -bacterial, -tuberculosis and -cancer activities. Materials and Methods: In the present study, we evaluated the in vitro cytotoxic activity of N,N’-bis(2-hydroxybenzyl)- (6), N,N’-bis(5-bromo-2-hydroxybenzyl)- (7) and N,N’-bis(5-chloro-2-hydroxybenzyl) (8)- ethylenediamine dihydrochlorides; and N,N’-bis(2-hydroxybenzyl)- (9), N,N’-bis(5-bromo-2-hydroxybenzyl)- (10) and N,N’-bis(5-chloro-2-hydroxybenzyl) (11)- ethylenediamine toward human lung (A549), breast (MDA-MB-231) and prostate (PC3) cancer cell lines after 24-h treatment using crystal violet dye binding assay. Effects on the cell cycle the using flow cytometry, and mitochondrial membrane potential using rhodamine-123 florescent dye were also evaluated. Results: Compounds 7 and 8 exhibit cytotoxic activity, causing cell arrest at different phases of the cell cycle and loss of mitochondrial membrane potential in the above cancer cell lines. Conclusion: These findings clearly demonstrate, to our knowledge for the first time, that ethylenediamine dihydrochloride salts–compounds 7 and 8–exhibit concentration-dependent cytotoxic activity towards A549, MDA-MB-231 and PC3 cancer cell lines, which may serve as a basis for future work on novel therapeutic agents.