Colistin Sulfate是一种结构独特的非核糖体环状寡肽抗菌剂。
Cas No.:1264-72-8
Sample solution is provided at 25 µL, 10mM.
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Colistin Sulfate is a structurally distinct class of nonribosomal, cyclic oligopeptides antimicrobials. Colistin Sulfate is mainly active against multidrug-resistant Gram-negative bacteria (GNB), exerting its antibacterial effect by directly interacting with the lipid A component of lipopolysaccharide (LPS) in the outer membrane (OM). The mainstream mechanism is: The cationic diaminobutyric acid (Dab) residues of Colistin Sulfate electrostatically bind to the anionic phosphate groups of lipid A, competitively displacing divalent cations (such as Mg²⁺ and Ca²⁺) from the membrane. This interaction disrupts the outer membrane, increases its permeability, leads to leakage of intracellular contents, and ultimately results in bacterial cell death[1].
In vitro, different Klebsiella pneumoniae isolates show variable susceptibility to Colistin Sulfate, with susceptible strains having Minimum Inhibitory Concentration (MIC) of 0.125-1mg/L and resistant strains exhibiting MIC of 32–128mg/L. Colistin Sulfate exerts rapid bactericidal activity against Klebsiella pneumoniae within 1 hour, but substantial regrowth may subsequently occur[2]. Colistin Sulfate has an MIC of 2μg/mL against the Ab396 strain of carbapenem-resistant Acinetobacter baumannii (CRAB)[3].
In vivo, Colistin Sulfate (75000U/kg; i.t.), administered every 8 hours for a total of 48 hours, significantly reduced lung bacterial loads and normalized the lung wet weight/body weight ratio in acute pneumonia mice inoculated with 2.5×10⁷ CFU (Colony Forming Unit) of Ab396 and 10% porcine mucin. Colistin Sulfate (75000U/kg; i.t.) showed superior efficacy compared to colistin Sulfate (150000U/kg; i.p.)[3].
References:
[1] El-Sayed Ahmed, Mohamed Abd El-Gawad et al. “Colistin and its role in the Era of antibiotic resistance: an extended review (2000-2019).” Emerging microbes & infections vol. 9,1 (2020): 868-885.
[2] Poudyal, Anima et al. “In vitro pharmacodynamics of colistin against multidrug-resistant Klebsiella pneumoniae.” The Journal of antimicrobial chemotherapy vol. 62,6 (2008): 1311-8.
[3] Chiang, Shyh-Ren et al. “Intratracheal colistin sulfate for BALB/c mice with early pneumonia caused by carbapenem-resistant Acinetobacter baumannii.” Critical care medicine vol. 37,9 (2009): 2590-5.
Colistin Sulfate是一种结构独特的非核糖体环状寡肽抗菌剂。Colistin Sulfate主要作用于耐多药革兰氏阴性菌（GNB），它通过与外膜脂多糖（LPS）的脂质A组分直接相互作用来发挥其抗菌作用。主流机制认为Colistin Sulfate中的阳离子二氨基丁酸（Dab）残基可与脂质A的阴离子磷酸基团发生静电结合，竞争性地取代膜上的二价阳离子（如Mg²⁺和Ca²⁺），从而破坏细菌外膜结构并增加其通透性，导致细胞内物质泄漏，最终引起细菌死亡[1]。
体外实验中，不同的肺炎克雷伯菌（Klebsiella pneumoniae）分离株对Colistin Sulfate的敏感性存在差异，其中敏感株的最小抑菌浓度（MIC）为0.125-1mg/L，而耐药株的MIC为32-128mg/L。Colistin Sulfate在1小时内对肺炎克雷伯菌具有快速的杀菌活性，但随后可能发生大量的再生[2]。Colistin Sulfate对耐碳青霉烯类鲍曼不动杆菌（Acinetobacter baumannii; CRAB）Ab396菌株的MIC为2μg/mL[3]。
体内实验中，Colistin Sulfate（75000U/kg；i.t.），每8小时给药一次，共持续48小时，可显著降低接种了2.5×107菌落形成单位（CFU）的Ab396菌株及10%猪黏蛋白的急性肺炎小鼠肺部细菌负荷，并使肺湿重/体重比恢复至正常水平。Colistin sulfate（75000U/kg; i.t.）的给药效果优于Colistin sulfate（150000U/kg; i.p.）[3]。
| Animal experiment [1]: | |
Animal models | Female BALB/c mice (Acute pneumonia) |
Preparation Method | Mice were inoculated intratracheally with 50L of 0.85% saline containing 2.5x107 cfu of Ab396 and 10% porcine mucin (for acute pneumonia). Two hours later, mice were treated with saline i.t. (control group), a combination of imipenem/cilastatin and sulbactam(i.p.; 80/80mg/kg and 40mg/kg), Colistin Sulfate (i.p.; 150000U/kg), and diluted in 50L of 0.85% saline, Colistin Sulfate (i.t.; 75000U/kg) every 8hrs for a total of 48hrs. Survival rates were recorded every 12hrs for 72hrs after bacterial inoculation. |
Dosage form | 150000U/kg, i.p.; 75000U/kg, i.t.; every 8hrs for a total of 48hrs |
Applications | Compared with the mice in all groups, those in intratracheal Colistin Sulfate group had a significantly favorable outcome at 72hrs after infection (survival rate=0%, 10%, 0% and 100%, respectively). Furthermore, intratracheal therapy decreased significantly the bacterial loads in the lungs and normalized the wet lung/body weight ratios in mice with acute pneumonia. |
References: | |
| Cas No. | 1264-72-8 | SDF | |
| 别名 | 硫酸粘杆菌素; Polymyxin E sulfate | ||
| 分子式 | C52H103N16O23S2.5 | 分子量 | 1400.64 |
| 溶解度 | ≥ 42.475mg/mL in Water with gentle warming | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 714 μL | 3.5698 mL | 7.1396 mL |
| 5 mM | 142.8 μL | 714 μL | 1.4279 mL |
| 10 mM | 71.4 μL | 357 μL | 714 μL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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Purity: >98.00% Potency: ≥19500U/mg Appearance: A solid
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