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  • Title: Inhibitory effect of aprotinin and gabexate mesilate on human plasma kallikrein.
    Author: Nakahara M.
    Journal: Arzneimittelforschung; 1983; 33(7):969-71. PubMed ID: 6194800.
    Abstract:
    Prekallikrein (PK) in human plasma was activated with kaolin in the presence of protease inhibitors aprotinin (Trasylol) and gabexate mesilate to investigate a difference in the inhibitory activity of plasma kallikrein (K) between these inhibitors. Benzoyl-prolyl-phenylalanyl arginine-p-nitroanilide (PPAN) cleavage of purified plasma K was markedly inhibited by aprotinin and gabexate mesilate, and acetyl-glycyl-l-lysine methyl ester hydrolysis of purified PK activator was slightly inhibited. PPAN cleavage of plasma K-alpha2 macroglobulin complex was hardly inhibited by aprotinin while PPAN cleavage of the complex was markedly inhibited by gabexate mesilate. The inhibitory activity of gabexate mesilate towards plasma K completely disappeared after 10 min incubation with plasma at 37 degrees C and also in 30 min on the experiment in which the time course of kaolin-induced PK activation was observed at 10 degrees C. On the other hand, the inhibitory activity of aprotinin towards plasma K never changed after 10 min incubation with plasma at 37 degrees C or 30 min incubation with plasma at 10 degrees C. From the results it is concluded that a predominant effect of aprotinin in human plasma is due to its stability in contrast to instability of gabexate mesilate.
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