Self-assembling cytotoxins.
Decanal and N-amino-N'-1-octylguanidine (AOG), combined at 28 microM each, mediated erythrocyte lysis within 80 minutes under physiological conditions. By contrast, no lysis was observed after 20 hours with either decanal (56 microM) or AOG (100 microM) alone. The pronounced synergism observed for these chemicals and similar reactive pairs of chemicals is due to the self-assembly of more cytotoxic hydrazones in situ. Decanal and AOG also exhibit synergistic activity against cultured human cells (HeLa) and bacteria (Escherichia coli J96). This synergism may be useful in the design of cytotoxins that would self-assemble selectively from nontoxic precursors within tumors, while sparing normal tissue.
D000447:Aldehydes / Q000378:metabolism* / Q000494:pharmacology; D003603:Cytotoxins / Q000378:metabolism* / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D004357:Drug Synergism; D004912:Erythrocytes / Q000187:drug effects; D004926:Escherichia coli / Q000187:drug effects; D006146:Guanidines / Q000378:metabolism* / Q000494:pharmacology*; D006367:HeLa Cells / Q000187:drug effects; D006801:Humans; D007700:Kinetics; D009369:Neoplasms / Q000188:drug therapy
D000447:Aldehydes; D003603:Cytotoxins; D006146:Guanidines; C049574:N-decylidenimino-N'-1-octylguanidine; C021170:decanaldehyde; C049575:N-amino-N'-1-octylguanidine