Spermine antagonizes the binding of adriamycin to the inner membrane of heart mitochondria.
The biologically active polyamine, spermine, has been found to function as a cationic antagonist of adriamycin binding to ox heart submitochondrial particles. This effect is specifically shown by spermine since other cations tested in the same conditions, can antagonize the binding only to a very low extent. Analysis of the adriamycin binding data in the presence of spermine indicate that the polyamine can greatly reduce the total number of binding sites for the anthracycline in submitochondrial particles and it can increase the apparent dissociation constant, whilst it leaves unchanged the degree of cooperativity of the binding. These results provide evidence on previously unexplored effects of spermine, suggesting that this polyamine might be examined as a possible in vivo antagonist of the adriamycin binding to mitochondria.
Solaini
G
G
Scuola Superiore di Studi Universitari, Sezione di Medicina, Pisa, Italy.
D000818:Animals; D001665:Binding Sites / Q000187:drug effects; D001667:Binding, Competitive; D002417:Cattle; D004317:Doxorubicin / Q000378:metabolism* / Q000494:pharmacology; D007425:Intracellular Membranes / Q000187:drug effects* / Q000378:metabolism; D007700:Kinetics; D046911:Macromolecular Substances; D008929:Mitochondria, Heart / Q000187:drug effects* / Q000378:metabolism; D013096:Spermine / Q000494:pharmacology*; D013367:Submitochondrial Particles / Q000187:drug effects / Q000378:metabolism
D046911:Macromolecular Substances; D013096:Spermine; D004317:Doxorubicin