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| Targets |
ε-Poly-L-lysine does not target a specific protein receptor. Its antimicrobial mechanism is primarily based on its cationic charge. The positively charged peptide electrostatically interacts with the negatively charged phospholipid components of the microbial cell membrane. This interaction disrupts membrane integrity, increasing permeability and leading to cell lysis and death. It can also cause cell membrane damage by interacting with the cell wall and inducing an osmotic effect. It has broad-spectrum activity against bacteria, yeasts, and molds, including Gram-positive and Gram-negative bacteria, but is less effective against Gram-negatives due to their outer membrane.
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| ln Vitro |
In vitro, ε-Poly-L-lysine hydrochloride has potent and rapid antimicrobial activity. It has a minimum inhibitory concentration (MIC) in the range of 0.1-10 ug/mL against various foodborne pathogens and spoilage microorganisms. It is particularly effective against Bacillus subtilis and Saccharomyces cerevisiae. It exhibits high thermal stability (withstanding 120degC for 30 minutes) and retains its antimicrobial activity across a broad pH range of 2.5-9.0. It does not have an EC₅0 or IC₅0 for a therapeutic effect because it is not a drug; it is a biocide. In cell culture, it is cytotoxic at high concentrations but is generally non-toxic to mammalian cells at its working concentrations (e.g., <500 ug/mL).
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| ln Vivo |
In vivo, ε-Poly-L-lysine is not a drug administered for systemic effects. Its primary in vivo application is as a food preservative. When ingested as part of food, it is considered safe (GRAS - Generally Recognized As Safe). It is also used in vivo as a coating agent for medical devices (e.g., cardiovascular stents) to prevent biofilm formation and subsequent infections. It can also be used as a transfection reagent to deliver nucleic acids into cells, leveraging its positively charged nature to bind DNA. No therapeutic efficacy in animal disease models has been reported for systemic administration.
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| Enzyme Assay |
No enzyme or receptor binding assays are applicable, as ε-Poly-L-lysine is a biocide, not a drug. Its activity is assessed by measuring antimicrobial efficacy. The Minimum Inhibitory Concentration (MIC) is determined using the broth microdilution method. A 96-well plate is prepared with two-fold serial dilutions of ε-PL (0.1-500 ug/mL) in a suitable growth medium (e.g., Mueller-Hinton broth for bacteria). A standardized suspension of the test microorganism (e.g., 5 x 10⁵ CFU/mL) is added to each well. The plate is incubated at the appropriate temperature for the organism (e.g., 37degC for 24 h for bacteria). The MIC is the lowest concentration of ε-PL that results in no visible turbidity. For fungicidal activity, the compound is tested against yeast in Yeast Nitrogen Base (YNB) broth.
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| Cell Assay |
Cell-based assays are used to assess the antimicrobial activity against specific microbes or to assess cytotoxicity against mammalian cells. For antimicrobial tests, the standard broth microdilution method described in the cell-free protocol is used. For cytotoxicity, mammalian cells (e.g., mouse fibroblast L929 cells) are cultured in 96-well plates in DMEM with 10% FBS. Cells are treated with ε-PL at concentrations ranging from 0 to 5000 ug/mL for 24-72 hours. Cell viability is measured using an MTT or a resazurin assay (alamarBlue). The CC₅0 (half-maximal cytotoxic concentration) can be calculated. This is important for evaluating the safety margin for potential biomedical applications.
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| Animal Protocol |
In vivo animal experiments for ε-Poly-L-lysine are not standard for drug development. For safety evaluations, acute oral toxicity (LD₅0) studies are conducted in rats. Rats are given a single oral dose of ε-PL at very high levels (up to 5,000 mg/kg) and observed for 14 days. For medical device applications, the compound is coated onto a material (e.g., a stent or catheter) and implanted in a rabbit or rat model of infection. The device is implanted subcutaneously or at the target site. The animals are monitored for clinical signs of infection, and at the end of the study, the implant is explanted to evaluate bacterial adherence and biofilm formation. These studies test the device, not the compound alone.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) data for ε-Poly-L-lysine itself are not typically studied because it is not systemically administered as a drug. When used as a food additive, it is ingested. It is partially hydrolyzed into L-lysine, an essential amino acid, in the gastrointestinal tract, and is then absorbed and utilized as a nutrient. It is not expected to be systemically absorbed as the intact polymer. The PK properties of poly-L-lysine polymers of higher molecular weight have been studied as drug delivery carriers. In rats, after intravenous injection, the plasma elimination half-life (t1/2) of poly-L-lysine is short, on the order of minutes, due to rapid distribution to the liver and kidneys, followed by degradation.
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| Toxicity/Toxicokinetics |
ε-Poly-L-lysine hydrochloride has a very low toxicity profile and is considered safe for use as a food preservative. The acute oral LD₅0 in rats is >5,000 mg/kg, which is comparable to table salt (NaCl). It is not mutagenic in the Ames test. It is not a skin irritant or sensitizer. In humans, it is recognized as safe when consumed within the approved limits (e.g., a maximum of 30 mg/kg body weight). It has no known carcinogenic or reproductive toxicity. However, at high doses, it may have a mild laxative effect. For laboratory handling, standard precautions (gloves, lab coat) are sufficient. It is a non-hazardous material.
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| References |
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| Additional Infomation |
ε-Poly-L-lysine hydrochloride (MV 2000-5000) is not a drug and has no regulatory approval as a human drug. It is an approved food additive (e.g., INS No. 258, E number E243) in many countries, including Japan, the United States, and the European Union. Its primary application is as a natural, "green" preservative to extend the shelf-life of a wide variety of food and beverage products, including rice and flour-based products, cereals, meat, and beverages. It is also used in research as an antimicrobial, in drug delivery (as a DNA carrier), and as a coating for medical devices to prevent infections. It is heat-stable and active over a wide pH range.
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| Molecular Formula |
(C6H12N2O.CLH)N
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| Molecular Weight |
2000-5000
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| Appearance |
Typically exists as solids at room temperature
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| Synonyms |
ε-Poly-L-lysine hydrochloride (MV 2000-5000); Epsilon-polylysine hydrochloride (MV 2000-5000); ε-Polylysine hydrochloride (MV 2000-5000); ε-PL hydrochloride (MV 2000-5000)
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~100 mg/mL (with ultrasonication)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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