TABLE 2.
Effect of the F2Pal variants on neutrophil activation and bacterial killing
| Pepducin name | Fatty acid and peptide sequence | Superoxide releasea | E. coli inhibitionb | S. aureus inhibitionb |
|---|---|---|---|---|
| F2Pal16 | Pal-KIHKKGMIKSSRPLRV | 10.7 ± 2.9 | 6.5 ± 0.5 | 5.8 ± 0.2 |
| F2Pal12 | Pal-KIHKKGMIKSSR | 52.7 ± 4.7 | 6.3 ± 0.3 | 3.3 ± 1.2 |
| F2Pal10 | Pal-KIHKKGMIKS | 85.6 ± 10.1 | 3.5 ± 0.3 | 2.5 ± 0.3 |
| F2Pal8 | Pal-KIHKKGMI | 0.7 ± 0.3 | 2.5 ± 0 | 2.7 ± 0.2 |
| F2Pal12K1→Q | Pal-QIHKKGMIKSSR | 0.6 ± 0.2 | 0 | 0 |
| F2Pal12K4→Q | Pal-KIHQKGMIKSSR | 1.4 ± 0.4 | 0 | 0 |
| F2Pal12K5→Q | Pal-KIHKQGMIKSSR | 0.9 ± 0.1 | 2.7 ± 0.3 | 0 |
| F2Pal12K9→Q | Pal-KIHKKGMIQSSR | 47.5 ± 7.7 | 1.8 ± 0.2 | 0 |
| F2Myr12 | Myr-KIHKKGMIKSSR | 32.6 ± 6.1 | 7.3 ± 0.6 | 3.3 ± 1.2 |
| F2Lau12 | Lau-KIHKKGMIKSSR | 2.5 ± 0.8 | 5.7 ± 0.6 | 0 |
| F2-12 | KIHKKGMIKSSR | 0 | 0 | 0 |
| F1Pal16 | Pal-KIHKQGLIKSSRPLRV | 0 | 5.7 ± 0.2 | 5 ± 0.3 |
| Polymyxin B | NAc | 7.5 ± 0.3 | 0 | |
a
Superoxide release upon neutrophil activation was measured by isoluminol-amplified chemiluminescence and presented as counts per minute × 106 (Mcpm).
b
Antibacterial activity of pepducin variants (3 μl, 6 nmol; 3.3 μg/ml for F2Pal12) or polymyxin B (16 μg/ml) was examined in the inhibition zone assay, and the zone diameters (mm) after subtracting the well diameter (3 mm) are shown. Polymyxin B at the highest concentration (50 mg/ml) examined did not exert any killing effect on S. aureus. Data are expressed as means ± standard errors of the means (SEM) (n > 3 experiments).
c
NA, not applicable.