Cytotoxic effect of the dimeric peptides against colon cancer cells and non-cancer cells (cells were treated for 2 h at 37°C)
| Code | Sequence | IC50 (μM) | Selectivity index | Haemolysis (%) | |||||
|---|---|---|---|---|---|---|---|---|---|
| HT-29 | Caco-2 | HEK 293 | Fibroblasts | SI1 | SI2 | SI3 | |||
| 26[F] | (RRWQWRFKKLG)2-K-Ahx | 12 | 18* | 22 | 34 | 2.8 | 1.8 | > 5.1 | 6 |
| 1 | (dRRWQWRFKKLG)2-K-Ahx | > 59 | 45 | nd | nd | nd | nd | nd | nd |
| 2 | (Orn-RWQWRFKKLG)2-K-Ahx | 18 | 38 | 25 | 20 | 1.1 | 1.4 | > 3.3 | 3 |
| 3 | (R-Orn-WQWRFKKLG)2-K-Ahx | 30 | 12 | 41 | 17 | 0.6 | 1.4 | > 2.0 | 5 |
| 4 | (RRWQW-Orn-FKKLG)2-K-Ahx | 49 | 10 | > 61 | > 61 | > 1.2 | > 1.2 | > 1.2 | 5 |
| 5 | (dR-Orn-WQWRFKKLG)2-K-Ahx | 20 | 11 | 14 | 9 | 0.5 | 0.7 | > 3.1 | 5 |
| 6 | (dRRWQW-Orn-FKKLG)2-K-Ahx | 35 | 16 | 25 | 23 | 0.7 | 0.7 | > 1.7 | 7 |
| 7 | (Ahx-RRWQWRFKKLG)2-K-Ahx | 19 | 25 | 19 | 29 | 1.5 | 1.0 | > 3.0 | 5 |
| 8 | (Biotin-Ahx-RRWQWRFKKLG)2-K-Ahx | 17 | 20 | 16 | 49 | 2.9 | 0.9 | > 2.9 | 6 |
| 9 | (CH3CO-Ahx-RRWQWRFKKLG)2-K-Ahx | 24 | nd | nd | 19 | 0.8 | nd | > 2.3 | 9 |
SI of peptides is described as the ratio IC50 non-cancer cells/IC50 cancer cells.