The effect of ε-aminocaproyl-S-benzyl-L-cysteine on the t-PA activity of human saliva.
OBJECTIVE
The aim of this work was to study the effect of the synthetic antifibrinolytics: ε-aminocaproic acid (EACA), tranexamic acid (AMCHA) and ε-aminocaproyl-S-benzyl-L-cysteine (H-EACA-S-Bzl-L-Cys-OH) on the fibrinolytic activity of saliva in order to obtain new data on the activity of saliva tissue plasminogen activator (t-PA).


METHODS
Saliva samples were obtained from healthy volunteers. Saliva, precipitate and supernatant were tested 1hr, 4 hrs and 6hrs after collection. The effect of the synthetic antifibrinolytics was examined with the use of the clot lysis time determination.


RESULTS
All examined compounds inhibited the fibrinolytic activity of saliva 1hr after collection. H-EACA-S-Bzl-L-Cys-OH was the most active inhibitor. After 6 hours in room temperature only this compound showed a certain possibility to prolong the clot lysis time.


CONCLUSIONS
The obtained results may indicate the possibility of the difference in specificity between the activities of t-PA of saliva and recombinant tissue plasminogen activator activities. It may explain the unexpected high inhibitory activity of H-EACA-S-Bzl-L-Cys-OH in our study.
Department of Organic Chemistry, Medical University of Bialystok, Bialystok, Poland. krystyna.midura-nowaczek@umwb.edu.pl
K
K
Midura-Nowaczek
J
J
Kaczyńska
I
I
Bruzgo
A
A
Markowska
D
D
Drozdowska
D000614:Aminocaproates; D015119:Aminocaproic Acid / Q000494:pharmacology; D000818:Animals; D000933:Antifibrinolytic Agents / Q000494:pharmacology; D001777:Blood Coagulation; D002417:Cattle; D003545:Cysteine / Q000031:analogs & derivatives* / Q000494:pharmacology; D005340:Fibrinogen / Q000378:metabolism; D005342:Fibrinolysis; D006470:Hemorrhage; D006801:Humans; D008954:Models, Biological; D010455:Peptides / Q000737:chemistry; D012463:Saliva / Q000187:drug effects* / Q000378:metabolism; D013997:Time Factors; D010959:Tissue Plasminogen Activator / Q000037:antagonists & inhibitors / Q000378:metabolism*; D014148:Tranexamic Acid / Q000494:pharmacology
D000614:Aminocaproates; D000933:Antifibrinolytic Agents; D010455:Peptides; C539166:epsilon-aminocaproyl-S-benzylcysteine; D014148:Tranexamic Acid; D005340:Fibrinogen; D010959:Tissue Plasminogen Activator; D003545:Cysteine; D015119:Aminocaproic Acid