In-vitro antileishmanial potential of peptide drug hirudin
Research article published in Chemical biology & drug design (2017)
Abstract
Hirudin is clinically an important drug used for the treatment of cardiac diseases, but has never been elucidated for antileishmanial potential. This study was designed to determine the therapeutic utility of hirudin against leishmaniasis. Binding affinities of 28 potent proteinase inhibitors were screened computationally against leishmanolysin (GP63), out of which hirudin exhibited higher binding affinity with GP63 and good expected IC50 values. Experimentally, hirudin showed most promising activity against promastigote and axenic amastigote forms of leishmanial parasites with IC50 values of 0.60 ± 0.36 μg/mL and 0.43 ± 0.23 μg/mL, respectively, in a dose- and time-dependent assay. The cytotoxicity assay revealed no adverse effects on human macrophages with LD50 value of 860.11 ± 53.44 μg/mL. Hirudin caused leishmanial cell death mainly by apoptosis and membrane permeability. In spite of the basic knowledge obtained, hirudin mechanism is considerably less prone to the induction of resistance than classical drugs. Collectively, this study fosters further studies for the hirudin as new antileishmania lead with a new mode of action.
Abstract sourced from PubMed (NCBI) for the cited record. See the original publication for the authoritative version.
Resumen
Hirudin is clinically an important drug used for the treatment of cardiac diseases, but has never been elucidated for antileishmanial potential. This study was designed to determine the therapeutic utility of hirudin against leishmaniasis.
Por qué esto importa para la hirudoterapia
Este estudio evaluó computacionalmente la hirudina contra la enzima parasitaria leishmanolisina (GP63) y luego la probó en el laboratorio, informando actividad contra las formas promastigote y amastigote axénicas de Leishmania (IC50 ~0,60 y ~0,43 µg/mL) con ninguna toxicidad observada en macrófagos humanos (LD50 ~860 µg/mL), y proponiendo apoptosis y permeabilización de la membrana como el mecanismo de muerte del parásito. Para ASH, amplía la historia del descubrimiento de fármacos del secreto de sanguijuela más allá de la anticoagulación, sugiriendo que la hirudina — ya conocida como un inhibidor de la trombina — puede tener un modo de acción antiparasitario completamente separado que merece ser explorado contra la leishmaniasis. Esto es estrictamente un ensayo in vitro e in silico: los resultados provienen de parásitos y células cultivados, no de animales o pacientes, por lo que solo establecen una línea de investigación y no pueden respaldar ninguna afirmación de que la hirudina o la terapia de sanguijuelas trate la leishmaniasis en humanos.
Citación
In-vitro antileishmanial potential of peptide drug hirudin.
Khan H et al. · Chemical biology & drug design, 2017
Contexto clínico relacionado
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Añadido a la biblioteca ASH: March 18, 2026 · Última actualización del sitio: June 18, 2026