FSL0482

Structure

• InChI=1S/C53H100N16O13/c1-9-30(6)12-10-11-13-41(72)60-33(14-20-54)48(77)69-43(32(8)71)53(82)65-36(17-23-57)45(74)64-38-19-25-59-52(81)42(31(7)70)68-49(78)37(18-24-58)62-44(73)34(15-21-55)63-50(79)39(26-28(2)3)67-51(80)40(27-29(4)5)66-46(75)35(16-22-56)61-47(38)76/h28-40,42-43,70-71H,9-27,54-58H2,1-8H3,(H,59,81)(H,60,72)(H,61,76)(H,62,73)(H,63,79)(H,64,74)(H,65,82)(H,66,75)(H,67,80)(H,68,78)(H,69,77)
• InChIKey=XDJYMJULXQKGMM-UHFFFAOYSA-N

Synonyms

• 1264-72-8
• 7722-44-3
• Belcomycin
• Colimycin
• Colistin
• Colistin A
• Colymycin
• Polymixin E1
• Polymyxin E1
• Polymyxin-E
• Torazin

Origin

Paenibacillus polymyxa var. colistinus

Biological activities

Disruption of the outer cell membrane of Gram-negative bacilli

Therapeutic

Antibacterial

Target

Bacterial outer cell membrane

Assay information

Binding and neutralizing lipopolysaccharide (LPS) and preventing the pathophysiologic effects of endotoxin in the circulation
Binding to phospholipids in the outer cell membrane of Gram-negative bacteria. Competitively displaces divalent cations from the phosphate groups of membrane lipids, which leads to disruption of the outer cell membrane, leakage of intracell
MICs for susceptible strains, 1 to 4 μg/ml MICs for resisrant strains were >gt;128 μg/ml
Effective antimicrobial effect in vivo using E. coli infected mice at 1 mg/Kg

References

• Giacometti A, Cirioni O, Ghiselli R, Orlando F, Mocchegiani F, D'Amato G, Silvestri C, Riva A, Del Prete MS, Saba V, Scalise G
  Antiendotoxin activity of antimicrobial peptides and glycopeptides.
  J Chemother, 15(2): 129-133 (2003)  12797388  doi: 10.1179/joc.2003.15.2.129
• Li J, Turnidge J, Milne R, Nation RL, Coulthard K
  In vitro pharmacodynamic properties of colistin and colistin methanesulfonate against Pseudomonas aeruginosa isolates from patients with cystic fibrosis.
  Antimicrob Agents Chemother, 45(3): 781-785 (2001)  11181360  doi: 10.1128/AAC.45.3.781-785.2001
• Evans ME, Feola DJ, Rapp RP
  Polymyxin B sulfate and colistin: old antibiotics for emerging multiresistant gram-negative bacteria.
  Ann Pharmacother, 33(9): 960-967 (1999)  10492501
• Warren HS, Kania SA, Siber GR
  Binding and neutralization of bacterial lipopolysaccharide by colistin nonapeptide.
  Antimicrob Agents Chemother, 28(1): 107-112 (1985)  2412488
• SUZUKI T, INOUYE H, FUJIKAWA K, SUKETA Y
  STUDIES ON THE CHEMICAL STRUCTURE OF COLISTIN. I. FRACTIONATION, MOLECULAR WEIGHT DETERMINATION, AMINO ACID AND FATTY ACID COMPOSITION.
  J Biochem, 54: 25-33 (1963)  14056349
• J. Antibiot., 3: 457-458 (1950)