Inhibition of in vitro clot growth by r-hirudin is more effective and longer sustained than by an analogous peptide
Research article published in Thrombosis and haemostasis (1994)
Abstract
The specific thrombin inhibitors r-hirudin and a synthetic peptide (I) D-FPRP(G)4-NGDFEEIPEEYL were compared in in vitro tests. r-hirudin proved to be the superior compound with respect to inhibition of amidolytic small substrate turnover that is catalysed by soluble and immobilised thrombin as well as to inhibition of fibrinogen activation. In an in vitro clot model significantly higher molar concentrations of peptide I are needed to achieve fibrin bound thrombin inhibition equivalent to that of r-hirudin. Stable complexes consisting of thrombin and hirudin oppose labile complexes containing the synthetic peptide. The latter leads to a regaining of thrombin activity with subsequent additional fibrin accretion. Analyses of the mixtures of thrombin and peptide I display a time dependent release of amino-terminal D-FPR peptide (III) exhibiting, similar to the residual fragment (peptide II), only weak inhibitory activity. Peptide I and the carboxy-terminal fragment induce, within a certain concentration range, an increase in thrombin activity and clot growth.
Abstract sourced from PubMed (NCBI) for the cited record. See the original publication for the authoritative version.
Резюме
Inhibition of in vitro clot growth by r-hirudin is more effective and longer sustained than by an analogous peptide.
Почему это важно для гирудотерапии
This study compared the specific thrombin inhibitors r-hirudin and a synthetic peptide (D-FPRP(G)4-NGDFEEIPEEYL) in in vitro tests of amidolytic substrate turnover, fibrinogen activation, and an in vitro clot model. r-Hirudin was the superior compound, forming stable thrombin–hirudin complexes, whereas the synthetic peptide formed labile complexes that allowed thrombin activity to resume and, within certain concentration ranges, even increased thrombin activity and clot growth. The findings highlight differences in complex stability and durability, but the abstract describes only 'in vitro tests' without specifying the blood source and does not involve live leeches or clinical outcomes; the relevance to hirudotherapy is limited to characterizing recombinant hirudin's properties.
Цитирование
Связанный клинический контекст
Узнайте, как это исследование связано с клинической практикой
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