Table 1.
Biophysical attributes of relevant lipopeptide analogs.
| Lipopeptide Sequence | H (%) |
CAC (µM) |
HC50 (µM) |
MIC (µM) | |
|---|---|---|---|---|---|
| LB a Medium |
Human b Plasma |
||||
| * C14KKc12K | 55 | 20 ± 5 | 12 ± 1 | 3–6 | >20 |
| C14OOc12O | 55 | 15 ± 1 | 14 ± 4 | 3–6 | >20 |
| C14OOc10O | 53 | 45 ± 14 | 28 ± 2 | 12.5–25 | 10–20 |
| C14(ω5)OOc10O | 50 | >100 | >100 | >50 | 2.5–5 |
| C14(ω5)OOc8O | 48 | >100 | >100 | >50 | 2.5–5 |
| C14(ω5)OOc6O | 47 | >100 | >100 | >50 | 5 |
| OOc12O | 24 | >100 | >100 | >50 | >20 |
*, Reference peptide [32], shown for comparison purposes. Grey background specifies published data; H, hydrophobicity, defined as % acetonitrile required for elution in reversed phase HPLC using a C18 column. Values were rounded to nearest whole number; CAC, critical aggregation concentration, determined by light scattering in PBS; HC50, lipopeptide concentration that caused 50% hemolysis compared to water (determined by measuring hemoglobin leakage after 3 h incubation in PBS at 37 °C, using 1% washed human erythrocytes); MIC, minimal inhibitory concentration, determined in LB medium and in plasma, using OD measurements and CFU counts, respectively; a, mean of 12 GNB strains, specified in Section 2; b, mean of three donors, assessed on E. coli 25922.