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Colistin Sulfate

Synonyms: Polymixin E Sulfate

Colistin (Polymixin E) is a cyclic cationic decapeptide linked to a fatty acid side chain, it belongs to a group of similarly structured bacterial antimicrobial peptides.

Colistin Sulfate Chemical Structure

Colistin Sulfate Chemical Structure

CAS No. 1264-72-8

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Biological Activity

Description Colistin (Polymixin E) is a cyclic cationic decapeptide linked to a fatty acid side chain, it belongs to a group of similarly structured bacterial antimicrobial peptides.
In vitro
In vitro Colistin (2 μg/mL) is active against most strains of Escherichia coli and P. aeruginosa, and all species of Enterobacter, Salmonella, Shigella, Pasteurella, Brucella, and Bordetella. Proteus, Serratia, Providencia. Colistin inhibits 225 strains of P.aeruginosa with MIC90 and MIC50 of 6.3 μg/mL and 1.6μg/mL, respectively. Colistin sulfate is approved only for topical and oral use because of its toxicity. [1] Colistin sulfate is administered orally (tablets or syrup) for bowel decontamination and topically as a powder for the treatment of bacterial skin infections. Colistin interacts with the bacterial membrane through electrostatic interactions between the cationic polypeptide (colistin) and anionic lipopolysaccharide (LPS) molecules in the outer membrane of the gram-negative bacteria, leading to derangement of the cell membrane. Colistin displaces magnesium (Mg+2) and calcium (Ca+2), which normally stabilize the LPS molecules, from the negatively charged LPS, leading to a local disturbance of the outer membrane. Colistin has also potent anti-endotoxin activity. [2] Colistin sulfate produces a strong postantibiotic effects against Acinetobacter baumannii ranging from 2.5 hours to 7.0 hours in a concentration-dependent manner. [3]
In Vivo
In vivo Colistin sulfate (5%, i.m.) causes the muscle circumference to appear erythematic in mice. Colistin sulfate (i.m., 15 mg/kg/day for 5 days) causes obvious neurotoxicity to piglets with moderate granular degenerations in the epithelial tissues from kidney and liver of mice. Colistin sulfate (i.m.) at dose of 2.5 mg/kg and 5.0 mg/kg results in Cmax of 3.73 mg/mL and 6.40 mg/mL, Tmax of 32 min and 34 min, t(1/2beta) of 256 min and 264 min, and absolute bioavailability of 95.94% and 88.45% in mice. [4]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06087536 Not yet recruiting
Hospital-acquired Bacterial Pneumonia|Ventilator-associated Bacterial Pneumonia
Omnix Medical Ltd
 January 2024 Phase 2
NCT05542446 Terminated
Colistin
St. Anne''s University Hospital Brno Czech Republic|Palacky University
 September 1 2022 Phase 4
NCT04775238 Unknown status
Nosocomial Infections
Sohag University
 February 27 2021 Not Applicable
NCT04208945 Unknown status
Pneumonia Ventilator-associated|Gram-Negative Pneumonia
University of Thessaly
 December 2019 Not Applicable

Chemical Information & Solubility

Molecular Weight 1400.63 Formula

C52H98N16O13.5/2H2SO4
CAS No. 1264-72-8 SDF Download Colistin Sulfate SDF
Smiles CCC(C)CCCC(=O)NC(CCN)C(=O)NC(C(C)O)C(=O)NC(CCN)C(=O)NC1CCNC(=O)C(NC(=O)C(CCN)NC(=O)C(CCN)NC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)C(CCN)NC1=O)C(C)O.CCC(C)CCCC(=O)NC(CCN)C(=O)NC(C(C)O)C(=O)NC(CCN)C(=O)NC2CC
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In vivo
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