SKU: C058  / 
    CAS Number: 52152-93-9

    Cefsulodin Sodium

    $43.28 - $223.41

    Cefsulodin Sodium is a third-generation cephalosporin antibiotic.  TOKU-E researchers have found that the main cause of cefsulodin instability stems from a key impurity in one of the raw materials used in Cefsulodin synthesis,  7-aminocephalosporanic acid (7-ACA).  In order to produce highly pure and Cefsulodin with high stability, industrial HPLC is used to remove significant quantities of this impurity for improved purity, potency, and stability. 

    Cefsulodin is also used in Coronavirus (SARS-CoV-2) research for compound repurposing campaigns.  In silico screening of 2421 approved small molecules and molecular dynamics simulations at Coventry University has revealed that Cefsulodin can bind to the SARS-CoV-2 S glycoprotein receptor binding domain (RBD).  

    Mechanism of Action Like β-lactams, cephalosporins interfere with PBP (penicillin binding protein) activity involved in the final phase of peptidoglycan synthesis. PBP’s are enzymes which catalyze a pentaglycine crosslink between alanine and lysine residues providing additional strength to the cell wall. Without a pentaglycine crosslink, the integrity of the cell wall is severely compromised and ultimately leads to cell lysis and death. Resistance to cephalosporins is commonly due to cells containing plasmid encoded β-lactamases.
    Spectrum Cefsulodin Sodium has a very limited spectrum, specifically targeting Pseudomonas aeruginosa
    Impurity Profile

    LD50 in mice (mg/kg): >4000 i.p.; >15000 orally (Bryskier).

    Microbiology Applications Cefsulodin Sodium is commonly used in clinical in vitro microbiological antimicrobial susceptibility tests (panels, discs, and MIC strips) primarily against Pseudomonas aeruginosa.  Medical microbiologists use AST results to recommend antibiotic treatment options.

    One line of SARS-CoV-2 reserach involves disrupting the entrance of the coronavirus into host cells.  Researchers at Coventry University found that Cefsulodin can bind to the SARS-CoV-2 S glycoprotein receptor binding domain (RBD) in silico. The S glycoprotein gives the  coronavirus SARS-CoV-2 it's 'crown' phenotype by forming prominent structures on the virion envelope.  The spike protein mediates the first interactions with the host cell and drives virulence and induces immune responses.  THe S glycoprotein has 2 subunits (S1 and S2).  S1 comprises the receptor -binding domain (RBD) for the antiotensin-converting enzyme 2 (ACE2).  S2 drives the fusion  along with the human antiotensin-converting enzyme (ACE2). 

    Media Supplements

    Cefsulodin can be used as a selective agent in several types of isolation media:

    Yersinia Selective Agar - Yersinia Selective Supplement

    Columbia Blood Agar - Helicobacter pylori Selective Supplement (Dent)

    mTSB - VCC Selective Supplement

    Salmonella Chromogenic Agar - Salmonella Selective Supplement

    Molecular Formula C22H19N4NaO8S2 · xH2O
    Impurity Profile

    LD50 in mice (mg/kg): >4000 i.p.; >15000 orally (Bryskier).

    References

    Cefsulodin Sodium (TOKU-E) was used to study the mechanisms of resistance in Cefsulodin-resistant Pseudomonas aeruginosa in: "CpxR activates MexAB-OprM efflux pump expression and enhances antibiotic resistance in both laboratory and clinical nalB-type isolates of Pseudomonas aeruginosa." Link to article.

    General Reference

    Geganutti G, Prischi F and Reynolds CA (2020  Supervised molecular dynamics for exploring the druggability of the SARS-CoV-2 spike protein. Research Square. DOI 10.21203/rs.3.rs-64722/v1. Link to preprint.

    Georgopapadakou NH (1992)  Mechanisms of action of cephalosporin 3'-quinolone esters, carbamates, and tertiary amines in Escherichia coliAntimicrob. Agents Chemother. 37(3):559-565

    MIC Enterobacteriaceae| 64 - >512 || Escherichia coli| 2 - 32|| Helicobacter pylori| 5.12 - 41|| Pseudomonas acidovorans| 512|| Pseudomonas aeruginosa| 1 - 256|| Pseudomonas cepacia| 32 - >128|| Pseudomonas diminuta| 16 - 128|| Pseudomonas flourescens| 256 - ≤512|| Pseudomonas maltophilia| 8 - 32|| Pseudomonas paucimobilis| 16 - 128|| Pseudomonas pseudoalcaligenes| 16 - 128|| Pseudomonas putida| 128 - 256|| Pseudomonas putrefaciens| 16 - 128|| Pseudomonas stutzeri| 16 - 128||