title: Effect of short peptides containing lysine and epsilon-aminocaproic acid on fibrinolytic activity of plasmin and topoisomerase II action on supercoiled DNA.
abstract: Effects of eight short peptides containing lysine and epsilon-aminocaproic acid (EACA) on prolongation of the clot lysis time, as well as hemolytic and antibacterial activities were investigated. Interaction with plasmids pBR322 and pUC19 with the use of ethidium bromide assay and determination of influence on the activity of topoisomerase I and II were also tested. Examined compounds inhibited fibrinolytic activity of plasmin and five of them were more active than EACA. Amides of dipeptides were most active antifibrinolytics (IC50 < 0.2 mM). According to the obtained data, the significant inhibition of fibrinolytic activity of plasmin was not associated with hemolytic effects. Examined compounds did not show antibacterial activity (MIC > 512 mg/L). DNA binding effects determined with the use of ethidium bromide were weak for all peptides and similar to those observed with EACA. Six compounds inhibited topoisomerase II action on supercoiled DNA.
authors.affiliation: Department of Organic Chemistry, Medical University of Białystok, Kiliński St. 1, 15-089 Białystok, Poland. krystyna.midura-nowaczek@umb.edu.pl
authors.forename: Krystyna
authors.initials: K
authors.lastname: Midura-Nowaczek
authors.forename: Maciej
authors.initials: M
authors.lastname: Purwin
authors.forename: Agnieszka
authors.initials: A
authors.lastname: Markowska
authors.forename: Danuta
authors.initials: D
authors.lastname: Drozdowska
authors.forename: Magdalena
authors.initials: M
authors.lastname: Bruzgo
mesh_terms: D015119:Aminocaproic Acid / Q000494:pharmacology*; D000900:Anti-Bacterial Agents / Q000494:pharmacology; D000933:Antifibrinolytic Agents / Q000494:pharmacology*; D004278:DNA, Superhelical / Q000378:metabolism*; D005341:Fibrinolysin / Q000037:antagonists & inhibitors*; D006461:Hemolysis / Q000187:drug effects; D008239:Lysine / Q000494:pharmacology*; D010455:Peptides / Q000494:pharmacology*; D059005:Topoisomerase II Inhibitors / Q000494:pharmacology*
chemical_list: D000900:Anti-Bacterial Agents; D000933:Antifibrinolytic Agents; D004278:DNA, Superhelical; D010455:Peptides; D059005:Topoisomerase II Inhibitors; D005341:Fibrinolysin; D008239:Lysine; D015119:Aminocaproic Acid