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.
Resumen
Inhibition of in vitro clot growth by r-hirudin is more effective and longer sustained than by an analogous peptide.
Por qué esto importa para la hirudoterapia
Este estudio comparó los inhibidores específicos de trombina r-hirudina y un péptido sintético (D-FPRP(G)4-NGDFEEIPEEYL) en pruebas in vitro de hidrólisis de sustratos amidolíticos, activación de fibrinógeno y un modelo de coágulo in vitro. La r-hirudina fue el compuesto superior, formando complejos estables trombina-hirudina, mientras que el péptido sintético formó complejos lábiles que permitieron la reanudación de la actividad trombínica y, dentro de ciertos rangos de concentración, incluso aumentaron la actividad trombínica y el crecimiento del coágulo. Los hallazgos ponen de manifiesto diferencias en la estabilidad y durabilidad de los complejos, pero el resumen describe solo 'pruebas in vitro' sin especificar la fuente de sangre y no involucra sanguijuelas vivas ni resultados clínicos; su relevancia para la hirudoterapia se limita a la caracterización de las propiedades de la hirudina recombinante.
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Añadido a la biblioteca ASH: May 27, 2026 · Última actualización del sitio: 18 de junio de 2026