Table 2. Antimicrobial activities of the peptides against standard bacterial strains.
MICsa | Papiliocin | Papiliocin-2A | Papiliocin-5A | Papiliocin-2A5A | PapN | PapN-2A | PapN-5A | PapN-2A5A | PapN-2F5W | PapC | Melittin | |
---|---|---|---|---|---|---|---|---|---|---|---|---|
Gram│negative | Escherichia coli | 0.250 | 0.250 | 0.250 | 0.500 | 1.00 | 2.00 | 1.00 | 2.00 | 1.00 | 128 | 4.00 |
Pseudomonas aeruginosa | 0.500 | 0.500 | 0.500 | 0.500 | 2.00 | 4.00 | 2.00 | 8.00 | 2.00 | >128 | 4.00 | |
Salmonella typhimurium | 0.500 | 0.500 | 0.500 | 1.00 | 2.00 | 4.00 | 2.00 | 4.00 | 2.00 | >128 | 4.00 | |
GMb | 0.417 | 0.417 | 0.417 | 0.667 | 1.67 | 3.33 | 1.67 | 4.67 | 1.67 | 213 | 4.00 | |
MHCc | 200 | 200 | 200 | 200 | 200 | 200 | 200 | 200 | 200 | 1.56 | 0.391 | |
Therapeutic Indexd (MHC/GM) | 480 | 480 | 480 | 480 | 120 | 60.0 | 120 | 42.9 | 120 | 0.007 | 0.098 | |
Gram│Positive | MICsa | Papiliocin | Papiliocin-2A | Papiliocin-5A | Papiliocin-2A5A | PapN | PapN-2A | PapN-5A | PapN-2A5A | PapN-2F5W | PapC | Melittin |
Bacillus subtilis | 16.0 | 64.0 | 64.0 | 128 | 8.00 | 32.0 | 16.0 | >128 | 8.00 | >128 | 4.00 | |
Eenterococcus faecalis | 64.0 | 128 | 128 | >128 | 64.0 | 128 | 128 | >128 | 64.0 | >128 | 2.00 | |
Staphylococcus aureus | 32.0 | 128 | 128 | >128 | 8.00 | 32.0 | 16.0 | 128 | 16.0 | >128 | 4.00 | |
GMb | 37.3 | 107 | 107 | 213 | 26.7 | 64.0 | 53.3 | 213 | 29.3 | 256 | 3.33 | |
MHCc | 200 | 200 | 200 | 200 | 200 | 200 | 200 | 200 | 200 | 1.56 | 0.390 | |
Therapeutic Indexd (MHC/GM) | 5.36 | 1.87 | 1.87 | 0.939 | 7.50 | 3.13 | 3.75 | 0.939 | 6.82 | 0.006 | 0.117 |
aMinimum inhibitory concentrations (MICs) were determined in three independent experiments performed in triplicate with a standard deviation of 14.0%.
bThe geometric means (GM) of the MIC values from all six bacterial strains are shown. When no antimicrobial activity was observed at 128 μM, a value of 256 μM was used to calculate the therapeutic index.
cThe minimal peptide concentration that produces hemolysis. When no detectable hemolysis was observed at 100 μM, a value of 200 μM was used to calculate the therapeutic index.
dThe ratio of the minimum hemolytic concentration (MHC; μM) over the GM of the MIC (μM). Larger values indicate greater cell selectivity.