Peptidomimetic as novel antibiotic
Institution: | Roskilde University |
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Department: | |
Year: | 2014 |
Keywords: | peptidomimetic; antimicrobial peptides; novel antibiotic |
Record ID: | 1122295 |
Full text PDF: | http://rudar.ruc.dk/handle/1800/17131 |
Antimicrobial peptides give great promises for the future in finding an alternative to antibiotics, with theirs effect against bacteria, viruses and even parasite infections, but peptides has its drawback specially because of the proteolytic degradation, but a lot of alternative backbone structures have been suggested in hope of keeping the activity and avoid the degradation such as peptoids which also gives promising results. Two peptide-peptoid hybrids were synthesized; GN-2-Nlys1,3,4,7 and GN-2-Nlys1,3,7 using solid phase synthesis with submonomeric approach to peptoid synthesis, and MIC values were determined, against P. aeruginosa and S. aureus MIC was 32µg/ml and against E. coli ATCC 25922 and E. coli CFT073 they showed MICs down to 16 µg/ml. GN-2-Nlys1,3,4,7 showed as well an effect against preformed biofilm from K. pneumonias at 2 times MIC and at 4 times MIC against E coli. The two hybrids were tested on red blood cells to survey the hemolytic activity and within the tested concentrations, which is up to 256µg/ml, there is none or only very little hemolysis, only 1% for GN-2-Nlys1,3,4,7 and up to 2 % for GN-2-Nlys1,3,7. Previously resistance studies shows what many thought was avoided with peptide because of the non-specific low-affinity way they work, explicitly shows that bacteria develop resistance against them which is an important aspect to take into account when considering using antimicrobial peptide as therapeutic agent.