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. 2012 Jun 5;13(6):6849–6862. doi: 10.3390/ijms13066849

Table 3.

Biological data of peptide analogs.

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
a

Peptides are ordered by relative hydrophobicity;

b

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;

c

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;

d

Therapeutic index = MHC/IC50, Larger values indicate greater anticancer specificity;

e

The fold improvement in the therapeutic index was determined as relative to that of parent peptide P.