Pharmacological activities and mechanisms of hirudin and its derivatives — a review
Comprehensive review published in Frontiers in Pharmacology (2021)
Abstract
Hirudin, an acidic polypeptide secreted by the salivary glands of Hirudo medicinalis (also known as "Shuizhi" in traditional Chinese medicine), is the strongest natural specific inhibitor of thrombin found so far. Hirudin has been demonstrated to possess potent anti-thrombotic effect in previous studies. Recently, increasing researches have focused on the anti-thrombotic activity of the derivatives of hirudin, mainly because these derivatives have stronger antithrombotic activity and lower bleeding risk. Additionally, various bioactivities of hirudin have been reported as well, including wound repair effect, anti-fibrosis effect, effect on diabetic complications, anti-tumor effect, anti-hyperuricemia effect, effect on cerebral hemorrhage, and others. Therefore, by collecting and summarizing publications from the recent two decades, the pharmacological activities, pharmacokinetics, novel preparations and derivatives, as well as toxicity of hirudin were systematically reviewed in this paper. In addition, the clinical application, the underlying mechanisms of pharmacological effects, the dose-effect relationship, and the development potential in new drug research of hirudin were discussed on the purpose of providing new ideas for application of hirudin in treating related diseases.
Abstract sourced from PubMed (NCBI) for the cited record. See the original publication for the authoritative version.
Summary
Comprehensive review of natural hirudin, recombinant variants, and bivalirudin/lepirudin derivatives — covers mechanism, pharmacokinetics, clinical applications, and safety across thrombotic indications.
Why This Matters for Hirudotherapy
This review systematically summarizes the pharmacological activities, pharmacokinetics, novel preparations, derivatives, and toxicity of hirudin, the acidic polypeptide from Hirudo medicinalis salivary glands and the strongest natural specific inhibitor of thrombin known. It covers anti-thrombotic effects plus additional bioactivities including wound repair, anti-fibrosis, effects on diabetic complications, anti-tumor activity, anti-hyperuricemia, and effects on cerebral hemorrhage, drawing on publications from the past two decades. This is highly relevant to ASH's core domain, providing a broad overview of hirudin — the central bioactive component of the leech secretome. CAVEAT: This is a review article synthesizing prior literature rather than original research; it presents no new primary data, and claims about specific bioactivities depend on the quality of underlying studies not individually appraised here.
Citation
Pharmacological activities and mechanisms of hirudin and its derivatives — a review.
Junren C et al. · Frontiers in pharmacology, 2021
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