Amerikanische Gesellschaft für Hirudotherapie

A novel integrated strategy for discovering absorbable anticoagulant bioactive peptides: a case study on leech protein hydrolysates

Discovery pipeline published in Molecules (2025)

Zuletzt aktualisiert: June 18, 2026Geprüft von: ASH Editorial Board
Research article — evidence reviewArticle reference
Evidence: Research reportGenomik & ProteomikSpeichel-PharmakologieFang KX et al. · Molecules, 2025

Abstract

Medicinal plants and animal-derived proteins represent valuable natural sources of bioactive components with pharmaceutical potential. Whilst some medicinal plants and animal-derived proteins also offer rich sources of anticoagulant bioactive peptides, their development faces multiple challenges: anticoagulant evaluation relies on single-parameter assays with limited reliability, native proteins demonstrate suboptimal activity without enzymatic treatment, and few researchers investigate bioavailable peptides. Our study establishes an innovative framework using the leech as a case study to overcome these barriers. A novel anticoagulant evaluation model was first established with the Critic-G1 weighting method. And we optimized the enzymatically hydrolyzed extracts with high activity using Box-Behnken response surface methodology. Subsequently, the everted gut sac model was implemented to simulate intestinal absorption and screen for absorbable peptide fractions. Furthermore, peptidomics was employed to identify the bioactive peptides. Lastly, we identified the bioactivity using anticoagulation assays. Results indicated that the optimal hydrolysis conditions were achieved with trypsin at 50.48 °C, an enzyme-to-substrate ratio of 6.78%, 7.51 h, and pH of 8.06. The peptide DLRWM was identified through integrated peptidomics and molecular docking approaches, with subsequent activity validation demonstrating its potent anticoagulant effects. This study has successfully identified a novel anticoagulant peptide (DLRWM) with confirmed intestinal absorption properties and provides a template for unlocking the pharmaceutical potential of medicinal animal proteins.

Abstract sourced from PubMed (NCBI) for the cited record. See the original publication for the authoritative version.

Publication typeJournal Article
Indexed MeSH termsAnticoagulantsAnimalsPeptidesLeechesMolecular Docking SimulationProtein HydrolysatesHydrolysisHumans

Zusammenfassung

Integrated discovery strategy combining enzymatic hydrolysis, fractionation, in vitro assays, and bioinformatic screening to identify orally absorbable anticoagulant peptides from Whitmania pigra.

Warum dies für die Hirudotherapie relevant ist

This study established an integrated framework for discovering absorbable anticoagulant peptides using the leech as a case study, combining optimized enzymatic hydrolysis (trypsin, 50.48 °C, enzyme-to-substrate ratio 6.78%, 7.51 h, pH 8.06), an everted gut sac model for simulated intestinal absorption, peptidomics, and molecular docking. The researchers identified a novel pentapeptide, DLRWM, with validated anticoagulant effects and confirmed intestinal absorption properties, providing a template for unlocking the pharmaceutical potential of medicinal animal proteins. This work is relevant to ASH's domain as it systematically explores leech-derived proteins as a source of orally bioavailable anticoagulant peptides. However, the anticoagulant activity was validated through in vitro assays and simulated absorption models only; no in vivo efficacy, pharmacokinetic, or clinical data are presented.

Zitation

A novel integrated strategy for discovering absorbable anticoagulant bioactive peptides: a case study on leech protein hydrolysates.

Fang KX et al. · Molecules, 2025

Verwandter klinischer Kontext

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