Table 5.
The cytotoxicity of tachyplesin I–III (TI-TIII) and cyclic analogues (cTI-cTIII) against cultured cells.
| CC50 (µM) 1 | Melanoma Selectivity 5 | |||||
|---|---|---|---|---|---|---|
| Peptide | MM96L 2 | HT144 2 | WM164 2 | HeLa 3 | HaCaT 4 | |
| TI | 1.5 ± 0.1 | 1.7 ± 0.2 | 2.5 ± 0.1 | 13.1 ± 1.2 | 11.6 ± 1.6 | 2–21 |
| TII | 1.6 ± 0.1 | 2.0 ± 0.1 | 1.6 ± 0.1 | 18.0 ± 3.9 | 3.7 ± 0.2 | 3–35 |
| TIII | 1.8 ± 0.1 | 2.0 ± 0.1 | 1.7 ± 0.1 | 21.7 ± 1.1 | 7.3 ± 0.5 | 5–48 |
| cTI | 1.3 ± 0.1 | 1.4 ± 0.1 | 2.7 ± 0.1 | 6.7 ± 0.6 | 7.9 ± 0.5 | 2–76 |
| cTII | 1.1 ± 0.1 | 0.8 ± 0.04 | 2.4 ± 0.3 | 7.2 ± 0.4 | 2.4 ± 0.3 | 3–58 |
| cTIII | 1.7 ± 0.1 | 0.9 ± 0.03 | 1.3 ± 0.1 | 9.3 ± 0.4 | 7.5 ± 0.3 | 3–98 |
1 The concentration necessary to kill 50% of cells was calculated from dose-response curves (n ≥ 3, ± SEM). 2 Melanoma cell lines: MM96L, HT144, WM164, 3 cervical cancer cell line: HeLa, 4 healthy epithelial control cell line: HaCaT (aneuploid immortal keratinocyte). Description and verification of each cell line are detailed in Supplementary Tables S2 and S3). 5 selectivity for melanoma cell lines was estimated through the activity-toxicity index (ATI). ATI = MHC/MCC50 (modified from Reference [46]), with MHC being the minimal concentration necessary to induce 10% (lower value) or 50% (higher value) cell death in human RBCs and MCC50 being the median of CC50 values of all melanoma cell lines. Values above 1 indicate a higher selectivity for the cancerous cells over RBCs.