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| Targets |
Piscidin-1 (22-42) targets the lipid bilayers of microbial cell membranes, similar to other antimicrobial peptides. Its amphipathic alpha-helical structure allows it to interact with and disrupt the negatively charged membranes of bacteria, fungi, and other microbes, leading to rapid cell lysis. It does not typically target a single protein receptor. The peptide can also interact with host cell membranes, contributing to its immunomodulatory and wound-healing activities, potentially through interactions with G-protein coupled receptors or other signaling molecules. The anti-cancer activity is mediated through membrane disruption and induction of apoptosis in cancer cells.
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| ln Vitro |
In vitro, Piscidin-1 (22-42) TFA exhibits potent antibacterial activity against both Gram-positive and Gram-negative bacteria, including drug-resistant strains. It also shows antifungal activity against Candida albicans and other pathogenic fungi, as well as antiviral and antiprotozoal activities. The peptide has immunomodulatory effects, modulating the activity of immune cells such as macrophages and neutrophils. It also promotes wound healing in cell culture models by enhancing keratinocyte migration and reducing inflammation. The anti-cancer activity is demonstrated in various cancer cell lines, including breast cancer, lung cancer, and leukemia cells. The detailed MIC values and specific cell lines are not provided in the search results.
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| ln Vivo |
In vivo, Piscidin-1 (22-42) TFA has demonstrated efficacy in animal models of bacterial infection, reducing bacterial load and improving survival. Its wound-healing properties have been shown in rodent models of skin wounds, where topical application accelerates wound closure and reduces infection. The anti-cancer activity has been studied in mouse tumor xenograft models, where systemic or intratumoral administration of the peptide inhibits tumor growth. The immunomodulatory effects have been observed in models of inflammation and sepsis. Detailed dosing regimens and specific animal models are not provided in the search results.
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| Enzyme Assay |
A standard broth microdilution method (CLSI guidelines) is used to determine the minimum inhibitory concentration (MIC) against bacteria. Bacterial strains (e.g., E. coli ATCC 25922, S. aureus ATCC 29213) are grown overnight in Mueller-Hinton broth (MHB). The bacteria are diluted to approximately 5×10⁵ CFU/mL. In a 96-well plate, Piscidin-1 (22-42) TFA is serially diluted 2-fold in MHB (concentration range: 0.125-128 microM). An equal volume of bacterial suspension is added to each well. The plate is incubated at 37degC for 18-24 h. The MIC is the lowest concentration that shows no visible bacterial growth. For antifungal testing, similar protocols are used with RPMI-1640 medium and Candida albicans (ATCC 90028). For antiviral assays, a plaque reduction assay is performed: Vero cells are infected with a specific virus, and the peptide is added to the overlay medium. The reduction in plaque number compared to the control is calculated.
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| Cell Assay |
For anti-cancer activity, human cancer cells (e.g., MDA-MB-231 breast cancer cells, A549 lung cancer cells) are seeded in 96-well plates (5,000-10,000 cells/well) in appropriate medium. After 24 h, cells are treated with Piscidin-1 (22-42) TFA at varying concentrations (0.1-100 microM) for 24-72 h. Cell viability is measured using the MTT assay or the CellTiter-Glo luminescent assay. The IC50 (the concentration that inhibits 50% of cell growth) is calculated from the dose-response curve. Apoptosis is assessed by Annexin V-FITC/PI staining and flow cytometry. For wound healing assays, a confluent monolayer of HaCaT keratinocytes or fibroblasts is scratched with a pipette tip, washed, and then treated with the peptide (1-20 microM). Images are captured at 0, 12, and 24 h to measure the closure distance. The percentage of wound closure is calculated as (initial area - area at time t)/initial area × 100%. For immunomodulation, mouse bone marrow-derived macrophages (BMDMs) are differentiated for 7 days. BMDMs are treated with Piscidin-1 (1-20 microM) in the presence or absence of LPS (100 ng/mL) for 24 h. Supernatants are collected, and TNF-alpha, IL-6, and IL-10 levels are measured by ELISA.
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| Animal Protocol |
A mouse model of wound infection: 8-week-old male BALB/c mice (n=6-8 per group) are anesthetized, and a 6-8 mm full-thickness excisional wound is created on the dorsum. The wound is inoculated with 1×10⁶ CFU of S. aureus or P. aeruginosa. After 1 h, Piscidin-1 (22-42) TFA (dissolved in sterile PBS) is applied topically at concentrations of 0.1-1% (w/v) in 50 microL, once or twice daily for 3-7 days. A control group receives vehicle (PBS) or an antibiotic (e.g., mupirocin). Wound area is measured daily with a digital caliper. On day 3 or 7, mice are euthanized, and the wound tissue is excised, homogenized, and plated for bacterial CFU determination. Histological analysis (H&E and Gram stain) is performed on paraffin-embedded sections to assess re-epithelialization and inflammation. A mouse tumor xenograft model: Female BALB/c nude mice are implanted subcutaneously with 5×10⁶ cancer cells (e.g., MDA-MB-231). When tumors reach 100-150 mm3, mice are randomized into groups receiving: (1) vehicle (PBS), (2) low-dose peptide (1-5 mg/kg), (3) high-dose peptide (10-20 mg/kg), and (4) positive control (e.g., doxorubicin). The peptide is administered intratumorally or intraperitoneally every 2-3 days for 2-3 weeks. Tumor volume is measured every 2-3 days. At the end of the study, tumors are excised, weighed, and analyzed by TUNEL and Ki-67 immunohistochemistry.
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| ADME/Pharmacokinetics |
Detailed PK data for Piscidin-1 (22-42) are not available. As a 21-amino acid antimicrobial peptide, its plasma half-life is expected to be very short (<20 minutes) due to rapid proteolytic degradation and renal clearance. Topical administration (wound healing) results in minimal systemic absorption, which is advantageous for reducing off-target toxicity. For systemic administration (e.g., in tumor models), frequent dosing (e.g., twice daily) or continuous infusion would likely be required to maintain therapeutic concentrations. The TFA salt form confers water solubility. No specific data on volume of distribution, clearance, or protein binding are available.
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| Toxicity/Toxicokinetics |
No formal toxicity data are available for Piscidin-1 (22-42) TFA. In animal models, topical application at concentrations up to 1% w/v has been reported to be well-tolerated, with no signs of systemic toxicity (e.g., weight loss, lethargy, or organ damage). At higher doses (e.g., >20 mg/kg intraperitoneally), the peptide may cause hemolysis or other toxicities due to its membrane-disrupting properties. Formal toxicology studies (e.g., acute, sub-chronic, genotoxicity) have not been reported. As with all antimicrobial peptides, the main safety concern is potential cytotoxicity against host cells, particularly at high concentrations. Standard laboratory safety precautions (gloves, lab coat, eye protection) should be followed.
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| References |
[1]. Neshani A, et al. Epinecidin-1, a highly potent marine antimicrobial peptide with anticancer and immunomodulatory activities. BMC Pharmacol Toxicol. 2019 May 28;20(1):33.
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| Additional Infomation |
Piscidin-1 (22-42) TFA is a research-grade peptide and is not approved by any regulatory agency for clinical, therapeutic, or diagnostic use. It is a highly potent, multi-functional antimicrobial peptide (AMP) with many functional uses, including antibacterial, antifungal, antiviral, antiprotozoal, anticancer, immunomodulatory, and wound healing properties. The TFA salt is the standard commercial form. This product is for research use only and not for human therapeutic applications.
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| Molecular Formula |
C116H177F3N30O23S
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| Related CAS # |
Piscidin-1 (22-42)
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| Appearance |
Typically exists as solid at room temperature
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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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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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