Isolation and characterization of poeciguamerin, a peptide with dual analgesic and antithrombotic activity from leech salivary glands
Basic science / drug discovery published in Int J Mol Sci (2023)
Abstract
When Poecilobdella manillensis attacks its prey, the prey bleeds profusely but feels little pain. We and other research teams have identified several anticoagulant molecules in the saliva of P. manillensis, but the substance that produces the paralyzing effect in P. manillensis is not known. In this study, we successfully isolated, purified, and identified a serine protease inhibitor containing an antistasin-like domain from the salivary secretions of P. manillensis. This peptide (named poeciguamerin) significantly inhibited elastase activity and slightly inhibited FXIIa and kallikrein activity, but had no effect on FXa, trypsin, or thrombin activity. Furthermore, poeciguamerin exhibited analgesic activity in the foot-licking and tail-withdrawal mouse models and anticoagulant activity in the FeCl3-induced carotid artery thrombosis mouse model. In this study, poeciguamerin was found to be a promising elastase inhibitor with potent analgesic and antithrombotic activity for the inhibition of pain and thrombosis after surgery or in inflammatory conditions.
Abstract sourced from PubMed (NCBI) for the cited record. See the original publication for the authoritative version.
Summary
Isolation and characterization of poeciguamerin, a novel leech-saliva peptide with dual analgesic and antithrombotic activity. Potential novel drug-candidate molecule.
Why This Matters for Hirudotherapy
This study isolated and characterized poeciguamerin, a serine protease inhibitor with an antistasin-like domain, from the salivary secretions of the leech Poecilobdella manillensis. The peptide significantly inhibited elastase activity and slightly inhibited FXIIa and kallikrein, while demonstrating analgesic activity in mouse foot-licking and tail-withdrawal models and anticoagulant activity in a FeCl3-induced carotid artery thrombosis model. This work is directly relevant to ASH's domain, as it characterizes a novel bioactive component of the leech secretome with dual analgesic and antithrombotic properties, suggesting potential therapeutic relevance for post-surgical or inflammatory pain and thrombosis. However, the findings are preclinical (in mouse models and in vitro enzyme assays), and no human clinical data, dosing, or safety information is presented.
Citation
Isolation and characterization of poeciguamerin, a peptide with dual analgesic and antithrombotic activity from leech salivary glands.
Wang et al. · International journal of molecular sciences, 2023
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