English: Omiganan
English: Omiganan
CAS number: 204248-78-2
Molecular formula: C₉₀H₁₂₇N₂₇O₁₂
Molecular weight: 1779.15
Sequence: ILRWPWWPWRRK-NH2
Appearance: white or off-white powder powder
How Omiganan acts:
It is a very small peptide and therefore difficult to identify and label for proteolysis; It is amidated at the C terminus to further resist proteolysis and remove the negative charge of the carboxyl group. It is amphiphilic and can interact strongly with the cell membrane. Cell membrane is expected to be one of their main targets. It is a polycation that favors their interaction with negatively charged bacterial membranes and the zomeric outer surface of lipopolysaccharide (LPS) with mammalian membranes rather than with peptidoglycan. In bacteria, the membrane potential is also more negative than in mammalian cells, which may enhance antibiotic binding and translocation. A final factor is the clinical defect that antiinflammatory cytidine also has activity on erythrocytes, whereas Omiganan appears to be less hemolytic. As mentioned above, the charged residues of omiga-nan are located near each terminal, away from the central hydrophobic region of the peptide, and the total positive charge of the peptide increases from 4+ to 5+, which can be explained by reduced hemolysis, since these changes are not favorable for peptide-like substances associated with zwitt-rionic mammalian membranes. This is corroborated by the results of Staubitz and others, where the central fragment of the conserved antiinflammatory cetin in omiganan is associated with activity, whereas the terminal fragment appears to adjust the specificity of the target.
Omiganan is used for:
Omiganan is a novel synthetic cationic antimicrobial peptide currently under development for the prevention of catheter-related infections and for the treatment of acne and rosacea. In this study, we evaluated the efficacy of topical application of omiganan gel in two skin implant models (in vivo porcine skin and in vivo guinea pig skin). omiganan0 was tested in an ex vivo porcine skin colonization model 1 to 2% of the gel agent showed a strong dose-dependent effect against Gram-positive and Gram-negative bacteria and yeasts, with maximum effects observed between 1 and 2%. There was no significant difference in activity between methicillin-resistant and susceptible Staphylococcus aureus, and drug activity was not affected by the size of the inoculated object. Omiganan1% gel had rapid antimicrobial activity, with a 2.7log(10) reduction in colony-forming units of Staphylococcus epidermolis/site at 1 h and a 5.2log(10) reduction in flagella/site at 24 h after application. The potent antibacterial and antifungal activity of Omiganan1% gel was confirmed by other studies in a dolphin skin colonization model. In summary, Omiganem gels have been shown to have rapid bactericidal and bactericidal effects with a clear dose-dependent effect on a broad spectrum of infectious organisms. These results further demonstrate the potential of the drug as a topical antimicrobial agent.
Post time: Jun-27-2023