Gramicidin (Synonyms: Gramicidin D) |
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Catalog No.GC32076
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La gramicidina es un péptido antimicrobiano que se ensambla como canales en las membranas y aumenta su permeabilidad hacia los cationes.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1405-97-6
Sample solution is provided at 25 µL, 10mM.
Gramicidin is a linear polypeptide antibiotic mixture, also known as Gramicidin D (GrD), composed of Gramicidin A, Gramicidin B and Gramicidin C[1,6]. Gramicidin molecules dimerize within lipid bilayers to form transmembrane channels permeable to monovalent cations, thereby dissipating sodium, potassium, and proton gradients, disrupting membrane potential, and impairing adenosine triphosphate (ATP) production[1,5]. Gramicidin is used in research on antimicrobial membrane activity, ion homeostasis, cancer-cell bioenergetics and apoptosis, tumor angiogenesis, and ionophore-mediated antimalarial activity[1-6].
In vitro, Gramicidin (0μM, 0.3μM, 1μM, and 3μM; 24h and 48h) increased apoptosis and G2/mitosis (G2/M) cell-cycle arrest and reduced migration, cyclin D1, B-cell lymphoma 2 (Bcl-2), and phosphorylated forkhead box O1 in SGC-7901 gastric cancer cells; Gramicidin produced IC50 values of 0.183μM and 0.191μM in SGC-7901 and BGC-823 cells, respectively[2]. Gramicidin (0μM, 0.33μM, 1μM, and 3μM; 24h, 48h, and 72h) reduced OVCAR8, SKOV3, and A2780 ovarian cancer cell proliferation in concentration- and time-dependent patterns; Gramicidin (0μM, 0.1μM, 0.3μM, and 1μM; 24h and 48h) increased deoxyribonucleic acid fragmentation, the sub-G1 population, caspase-3 cleavage, and poly(adenosine diphosphate-ribose) polymerase (PARP) cleavage[3]. Gramicidin (0.04mg/mL; 24h) reduced HeLa cervical cancer cell growth by 40%, while Gramicidin (0.3mg/mL; 24h) combined with lipophilic bismuth nanoparticles (BisBAL NPs) (1μM, 10μM, 25μM, 50μM, 100μM, and 150μM) increased growth inhibition to 86% from 10μM BisBAL NPs and disrupted cell-membrane integrity[4].
In vivo, Gramicidin A, the predominant component of Gramicidin (0.11mg/kg; intratumoral injection twice weekly for 14 days), reduced mean tumor mass by approximately 40% in female hairless Nu/J mice bearing SN12C renal cell carcinoma xenografts without a significant change in body weight[5]. Gramicidin (1.4mg/kg/day; intraperitoneal injection once daily for 4 days) reduced parasitemia in Plasmodium vinckei petteri-infected mice with ED50 of 1.4mg/kg/day[6].
References:[1] Ragioto DAMT, Carrasco LDM, Carmona-Ribeiro AM. Novel gramicidin formulations in cationic lipid as broad-spectrum microbicidal agents. Int J Nanomedicine. 2014;9:3183-3192. doi:10.2147/IJN.S65289.
[2] Chen T, Wang Y, Yang Y, Yu K, Cao X, Su F, et al. Gramicidin inhibits human gastric cancer cell proliferation, cell cycle and induced apoptosis. Biol Res. 2019;52(1):57. doi:10.1186/s40659-019-0264-1.
[3] Choi MS, Lee CY, Kim JH, Lee YM, Lee S, Kim HJ, et al. Gramicidin, a bactericidal antibiotic, is an antiproliferative agent for ovarian cancer cells. Medicina (Kaunas). 2023;59(12):2059. doi:10.3390/medicina59122059.
[4] Cabral-Romero C, García-Cuellar CM, Hernandez-Delgadillo R, Sánchez-Pérez Y, Meester I, Solís-Soto JM, et al. Synergistic antitumor activity of gramicidin/lipophilic bismuth nanoparticles (BisBAL NPs) on human cervical tumor cells. Front Nanotechnol. 2021;3:633604. doi:10.3389/fnano.2021.633604.
[5] David JM, Owens TA, Barwe SP, Rajasekaran AK. Gramicidin A induces metabolic dysfunction and energy depletion leading to cell death in renal cell carcinoma cells. Mol Cancer Ther. 2013;12(11):2296-2307. doi:10.1158/1535-7163.MCT-13-0445.
[6] Gumila C, Ancelin ML, Delort AM, Jeminet G, Vial HJ. Characterization of the potent in vitro and in vivo antimalarial activities of ionophore compounds. Antimicrob Agents Chemother. 1997;41(3):523-529. doi:10.1128/AAC.41.3.523.
| Cell experiment [1]: | |
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Cell lines |
Human SGC-7901 and BGC-823 gastric cancer cells |
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Preparation Method |
SGC-7901 and BGC-823 cells were cultured with different Gramicidin concentrations. Cell viability was assessed using the cell counting kit-8 assay; apoptosis and cell cycle were assessed using Annexin V-fluorescein isothiocyanate/propidium iodide staining and flow cytometry; cyclin D1, B-cell lymphoma 2, and forkhead box O1 phosphorylation were analyzed by western blotting. |
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Reaction Conditions |
0μM, 0.3μM, 1μM, and 3μM; 24h and 48h |
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Applications |
Gramicidin increased apoptosis and G2/M cell-cycle arrest and reduced migration, cyclin D1, Bcl-2, and phosphorylated forkhead box O1 in SGC-7901 cells; Gramicidin produced IC50 values of 0.183μM and 0.191μM in SGC-7901 and BGC-823 cells. |
| Animal experiment [2: | |
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Animal models |
Plasmodium vinckei petteri-infected mouse model |
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Preparation Method |
Mice infected with Plasmodium vinckei petteri received intraperitoneal Gramicidin, and parasitemia was evaluated using a 4-day suppressive test. |
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Dosage form |
1.4mg/kg/day; intraperitoneal injection; 4 days |
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Applications |
Gramicidin reduced parasitemia in infected mice with an ED50 of 1.4mg/kg/day. |
| References: [1] Chen T, Wang Y, Yang Y, Yu K, Cao X, Su F, et al. Gramicidin inhibits human gastric cancer cell proliferation, cell cycle and induced apoptosis. Biol Res. 2019;52(1):57. doi:10.1186/s40659-019-0264-1. [2] Gumila C, Ancelin ML, Delort AM, Jeminet G, Vial HJ. Characterization of the potent in vitro and in vivo antimalarial activities of ionophore compounds. Antimicrob Agents Chemother. 1997;41(3):523-529. doi:10.1128/AAC.41.3.523. | |
| Cas No. | 1405-97-6 | SDF | |
| Sinónimos | Gramicidin D | ||
| Canonical SMILES | [Gramicidin] | ||
| Formula | C99H140N20O17 | M.Wt | 1882.3 |
| Solubility | DMSO : ≥ 100 mg/mL (53.13 mM);Water : < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 531.3 μL | 2.6563 mL | 5.3126 mL |
| 5 mM | 106.3 μL | 531.3 μL | 1.0625 mL |
| 10 mM | 53.1 μL | 265.6 μL | 531.3 μL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)