Table 2.
Hemolytic grades against human erythrocytes, cytotoxicity (IC50) against rat cardiomyocytes, HEK293 cells, and HeLa cells, and half-life times in mouse serum determined for Api137 and the four new apidaecin analogs.
| Hemolytic grade [%] | IC50 on cell viability [g/L] | Half-life time mouse serum (min) | ||||
|---|---|---|---|---|---|---|
| 0.1 g/L | 0.6 g/L | Rat cardiomyocytes | HEK293 | HeLa | ||
| Api137* | 0.4 ± 0.5 | 1.0 ± 0.2 | >0.6 | >0.6 | >0.6 | 345 |
| Api793 | 1.3 ± 0.4 | 1.6 ± 0.5 | >0.6 | 0.64 ± 0.05 | 0.64 ± 0.15 | 246 |
| Api794 | 1.7 ± 0.2 | 1.9 ± 0.3 | >0.6 | 0.28 ± 0.03 | 0.23 ± 0.09 | 311 |
| Api795 | −0.8 ± 0.4 | 0.0 ± 0.7 | >0.6 | >0.6 | >0.6 | 354 |
| Api796 | −0.8 ± 0.2 | −0.1 ± 0.8 | >0.6 | >0.6 | >0.6 | 249 |