Midura-Nowaczek Krystyna, Purwin Maciej, Markowska Agnieszka, Drozdowska Danuta, Bruzgo Magdalena
Department of Organic Chemistry, Medical University of Białystok, Kiliński St. 1, 15-089 Białystok, Poland.
Acta Pol Pharm. 2013 May-Jun;70(3):431-4.
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.
研究了八种含赖氨酸和ε-氨基己酸（EACA）的短肽对延长凝血块溶解时间的影响以及溶血和抗菌活性。还测试了它们与质粒pBR322和pUC19的相互作用（使用溴化乙锭测定法）以及对拓扑异构酶I和II活性的影响。所检测的化合物抑制了纤溶酶的纤维蛋白溶解活性，其中五种比EACA更具活性。二肽酰胺是最具活性的抗纤维蛋白溶解剂（IC50 < 0.2 mM）。根据所得数据，纤溶酶纤维蛋白溶解活性的显著抑制与溶血作用无关。所检测的化合物未显示出抗菌活性（MIC > 512 mg/L）。使用溴化乙锭测定的DNA结合效应对于所有肽都很弱，且与EACA观察到的相似。六种化合物抑制拓扑异构酶II对超螺旋DNA的作用。
