Table 4. Summary of bioassay data for synthetic ponericin analogues.
IC50, concentrations that caused 50% inhibition of H. contortus lruval development; PD50, median paralytic dose, and LD50, median lethal dose for insecticidal effects on L. cuprina; CC50, concentration required to induce 50% death of HEK293 cells; HC50, concentrations required to lyse 50% of human red blood cells; EC50, effective concentration for activation of F11 cells in a FLIPR assay. All errors are SEM. Active peptides are shaded.
| Peptide | Anthelmintic (IC50 μM) | Insecticidal activity (nmol g−1) |
Cytotoxicity (CC50 μM) | Hemolysis (HC50 μM) | DRG assay | FLIPR (EC50 μM) |
||
|---|---|---|---|---|---|---|---|---|
| (PD50 1 h) | (LD50 24 h) | F11 | HEK293 | |||||
|
| ||||||||
| Nc3a | 5.6 ± 1.3 | 0.5 ± 0.03 | 3.5 ± 0.8 | 5.2–6.8 | >100 | Strong | 22.9 ± 1.95 | 57.9 ± 5.87 |
| [1A-]Nc3b | 31.2 ± 3.9 | 12.1 ± 3.9 | 41.7 ± 18.3 | >250 | >150 | Inactive | >100 | >100 |
| [T3W]Nc3b | 16.6 ± 2.5 | 1.1 ± 0.9 | 12.1 ± 3.3 | 16.9 | >100 | Strong | 24.5 ± 0.01 | >100 |
| [L1 9P]Nc3b | 52.1 ± 11.8 | >50 | >50 | >250 | >250 | Inactive | >100 | >100 |
| [G20E]Nc3b | >100 | >50 | >50 | >250 | >150 | Inactive | >100 | >100 |
| [S32R]Nc3b | 23.5 ± 8.3 | 2.5 ± 1.8 | 16.2 ± 4.8 | >100 | >150 | Strong | 12.1 ± 0.67 | >100 |
| [swap]Nc3b | 31.6 ± 7.6 | 37.1 ± 4.9 | >50 | >250 | >200 | Inactive | >100 | >100 |
| Nc3b | 37.8 ± 7.4 | 26.4 ± 5.9 | 32.1 ± 8.6 | >300 | >300 | Inactive | >100 | >100 |