Table 5. Hemolytic Activity, Cytotoxicity, Therapeutical Index (TI), and Plasma Protein Binding (PPB) of β-Hairpin AMPs.
| cytotoxicity (μg/mL) |
|||||||
|---|---|---|---|---|---|---|---|
| HepG2 |
HEK293 |
||||||
| compound | hemolysis (%) at 300 μg/mL | 1% FBS | 10% FBS | 1% FBS | 10% FBS | TIa | PPB (%) |
| arenicin-3 | 4.4 ± 1.1 | 95.2 ± 4.1 | >300 | 104.6 ± 1.8 | >300 | 17 | 68 |
| tachyplesin-1 | 27.8 ± 3.9 | 65.7 ± 1.5 | >300 | 94.7 ± 1.1 | >300 | 335 | 76 |
| polyphemusin-1 | 29.6 ± 2.4 | 36.5 ± 8.6 | 254.3 ± 14.2 | 36.6 ± 1.4 | 188.5 ± 1.1 | 46 | 63 |
| gomesin | 4.4 ± 0.1 | 162.4 ± 1.1 | 219.7 ± 73.3 | 102.3 ± 1.1 | 116.1 ± 25.1 | 6 | 87 |
| protegrin-1 | 64.8 ± 3.5 | 31.4 ± 2.0 | 96.1 ± 1.1 | 19.6 ± 1.2 | 93.9 ± 1.1 | 19 | 89 |
| thanatin | 1.3 ± 0.4 | >300 | >300 | >300 | >300 | 3 | 92 |
a
TI is the therapeutic index calculated as the ratio of the average toxicity (hemolytic and cytotoxic at 1% FBS) to the median of the MIC determined toward all tested bacterium and fungus strains.