Fibrinolytic and Fibrinogenolytic Effects of Acyl Urokinase and Urokinase Combinations In Vitro
L. I. Mukhametova, R. B. Aisina,# and S. D. Varfolomeev
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Faculty of Chemistry, Moscow State University, Vorob'evy gory, Moscow, 119899 Russia
Received July 19, 2005; in final form, September 27, 2005
Abstract: The in vitro thrombolytic and side effects of double-strand urokinase-type plasminogen activator (tcu-PA), p-guanidinobenzoyltcu-PA (GB-tcu-PA), and their combinations were compared. The reversible blocking of the active site stabilizes GB-tcu-PA in human plasma and results in longer thrombolysis and lesser side effects than those of tcu-PA. However, the acylated activator displays a marked lag period of thrombolytic action. GB-tcu-PA and tcu-PA combinations (molar ratios 4 : 1 and 1 : 1) induce a prolonged and effective thrombolysis without the initial lag period at a low level of plasminogen, fibrinogen, and α2-antiplasmin depletion in the plasma surrounding the clot.
Key words: agent combination, p-guanidinobenzoylurokinase, side effects, stability in plasma, thrombolysis, urokinase
Russian Journal of Bioorganic Chemistry 2006, 32 (4):345-351