Table 3.
Peptides a | MHC b (μmol/L) | IC50 c (μmol/L) | Therapeutic Index d | Fold e |
---|---|---|---|---|
P | 5.20 ± 0.02 | 1.71 ± 0.07 | 3.04 | 1.0 |
K7D | 10.4 ± 0.04 | 1.29 ± 0.03 | 8.07 | 2.7 |
K14D | 5.20 ± 0.02 | 1.52 ± 0.05 | 3.42 | 1.1 |
K22D | 20.81 ± 0.10 | 1.39 ± 0.02 | 14.97 | 4.9 |
K7D/K14D | 20.81 ± 0.15 | 2.06 ± 0.01 | 10.10 | 3.3 |
K14D/K22D | 20.81 ± 0.06 | 1.40 ± 0.09 | 14.86 | 4.9 |
K7D/K14D/K22D | 81.31 ± 0.17 | 4.45 ± 0.19 | 18.27 | 6.0 |
K7D/K10D/K14D/K22D | 325.20 ± 0.82 | 4.79 ± 0.23 | 67.89 | 22.3 |
K3D/K7D/K10D/K14D/K22D | >325.20 | 20.41 ± 0.64 | 31.87 | 10.5 |
K1D/K3D/K7D/K10D/K14D/K22D | >325.20 | 18.07 ± 0.48 | 35.99 | 11.8 |
L6D | 10.40 ± 0.08 | 2.23 ± 0.10 | 4.67 | 1.5 |
L12D | 20.81 ± 0.03 | 2.63 ± 0.07 | 7.91 | 2.6 |
L20D | 20.81 ± 0.13 | 2.33 ± 0.06 | 8.93 | 2.9 |
L6D/L12D | 20.81 ± 0.10 | 3.01 ± 0.08 | 6.91 | 2.3 |
L12D/L20D | 81.31 ± .43 | 3.14 ± 0.06 | 25.89 | 8.5 |
L6D/L12D/L20D | 162.61 ± 0.19 | 7.80 ± 0.26 | 20.85 | 6.9 |
L6D/L12D/L17D/L20D | 81.31 ± 1.05 | 9.69 ± 0.38 | 8.39 | 2.8 |
L6D/L12D/L17D/L20D/L21D | >325.20 | 12.88 ± 0.15 | 50.50 | 16.6 |
Peptides are ordered by relative hydrophobicity;
Hemolytic activity (minimal hemolytic concentration) was determined on human red blood cells after incubating with peptides for 1 h (hRBC); When no hemolytic activity was observed at 325.2 μmol/L, a value of 650.4 μmol/L was used for calculation of the therapeutic index;
Anticancer activity (IC50) represents the concentration of peptides at which cell viability was reduced by 50% in comparison to untreated cells; The MTT assay was repeated in triplicate and IC50 value was determined by averaging three repeated experiments;
Therapeutic index = MHC/IC50, Larger values indicate greater anticancer specificity;
The fold improvement in the therapeutic index was determined as relative to that of parent peptide P.