Lumbrokinase | Supplementopedia

Overview

Lumbrokinase is a group of fibrinolytic enzymes derived primarily from the earth‑worm Lumbricus rubellus (and related species). In supplement form it is used mainly to support normal blood‑clot breakdown (fibrinolysis) and to promote healthy circulatory function.

Benefits

Enhanced fibrinolysis: Clinical trials show that oral Lumbrokinase reduces plasma fibrinogen levels and shortens clot‑lysis time, supporting vascular health (e.g., Zhang et al., 2020).
Cardiovascular protection: Meta‑analyses of randomized trials report modest reductions in systolic blood pressure and improvements in endothelial function in patients with mild hypertension or atherosclerosis.
Peripheral circulation: Studies in patients with peripheral artery disease demonstrate improved ankle‑brachial index and reduced leg‑pain scores after 12 weeks of supplementation.
Anti‑inflammatory effects: In vitro and animal data show down‑regulation of NF‑κB signaling, suggesting potential benefits for chronic inflammatory conditions.
Metabolic support: Small human trials indicate modest improvements in insulin sensitivity and lipid profiles, likely mediated by improved micro‑circulation.
Neuro‑vascular health: By promoting cerebral micro‑circulation, Lumbrokinase may support cognitive performance in older adults, though data remain preliminary.

How It Works

Fibrinolysis: Lumbrokinase consists of serine‑type proteases (≈25–30 kDa) that cleave fibrin at multiple sites, converting insoluble fibrin clots into soluble fragments.
Specificity: The enzymes exhibit high specificity for the β‑chain of fibrin, sparing fibrinogen and minimizing systemic bleeding.
Activation of tPA and Inhibition of PAI-1: Lumbrokinase also activates tissue‑type plasminogen activator (tPA) and inhibits plasminogen activator inhibitor‑1 (PAI‑1), augmenting endogenous fibrinolysis.
Anti-thrombotic and Anti-inflammatory Effects: Concurrently, it reduces platelet aggregation by modulating thromboxane A2 synthesis and down‑regulating the NF‑κB pathway, resulting in anti‑inflammatory and anti‑thrombotic effects.
Improved Blood Rheology: The combined actions improve blood rheology, lower blood viscosity, and promote endothelial nitric‑oxide production, which together support vascular and metabolic health.

Dosage

Standardization: Commercial Lumbrokinase products are standardized in “fibrinolytic units” (FU) rather than milligrams.
Common Dosage Range: The most commonly studied range is 20 000–40 000 FU per day, divided into 1‑2 doses taken with meals to improve absorption.
Cardiovascular Support Dosage: For cardiovascular support, 30 000 FU taken twice daily (total 60 000 FU) is often used in clinical trials.
General Circulatory Health Dosage: Many over‑the‑counter products recommend 10 000–15 000 FU once daily for general circulatory health.
Anticoagulant Combination Dosage: When combined with anticoagulants, a lower dose (5 000–10 000 FU) is advised to mitigate bleeding risk.
Administration: The enzyme is stable in the acidic gastric environment, but some manufacturers advise taking the capsule with food to reduce occasional gastrointestinal discomfort.

Safety & Side Effects

General Tolerance: Lumbrokinase is generally well‑tolerated.
Adverse Events: Reported adverse events include mild gastrointestinal upset (bloating, mild diarrhea) in <5 % of users.
Bleeding Risk: Because it enhances fibrinolysis, there is a modest increased risk of bleeding, especially when combined with anticoagulants (warfarin, DOACs), antiplatelet agents (aspirin, clopidogrel), or high‑dose fish‑oil supplements.
Contraindications: Contraindications include: active bleeding, recent surgery (≤2 weeks), known coagulation disorders, or pregnancy (insufficient data).
Pre-use Consultation: Individuals with severe liver or kidney disease should consult a clinician before use.
Monitoring: Monitoring of coagulation parameters (PT/INR, aPTT) is recommended for patients on anticoagulant therapy.
Drug Interactions: No significant drug–enzyme interactions have been reported beyond the antithrombotic class.

Chemistry

Composition: Lumbrokinase is not a single molecule but a mixture of serine proteases (e.g., lumbrokinase 1, 2, 3) with molecular weights ranging from 25 kDa to 30 kDa.
Structure: Each enzyme is a polypeptide of ~250–300 amino acids, containing the classic catalytic triad (His‑57, Asp‑102, Ser‑195) typical of the trypsin family.
Molecular Formula: The overall “molecular formula” varies by isoform, but an average composition can be approximated as C₁₁₅₀H₁₈₅₀N₃₅₀O₃₇₀S₁₀, reflecting a typical protein.
Nomenclature: No single IUPAC name exists; the enzymes are classified as “serine proteases (EC 3.4.21)”.
Key Structural Features: Key structural features include a conserved “catalytic pocket” that binds the Arg‑Gly‑Asp sequence of fibrin, and a glycosylation pattern that improves stability in the gastrointestinal tract.

Sources & Quality

Source: Commercial Lumbrokinase is extracted primarily from the dried bodies of Lumbricus species (most commonly Lumbricus rubellus and Eisenia fetida) harvested from controlled, pesticide‑free farms.
Extraction Process: The process involves aqueous extraction, filtration, and purification by ion-exchange chromatography to isolate the active protein fractions.
Recombinant Production: Some manufacturers use recombinant expression in E. coli or Pichia pastoris to produce a more defined enzyme mixture, which can improve batch‑to‑batch consistency.
Quality Control: Quality‑control standards include activity assays (FU per milligram), absence of heavy metals, and microbial limits according to USP <111> and GMP guidelines.
Product Selection: For optimal safety, look for products that disclose the source species, extraction method, and provide third‑party testing for potency and contaminants.