Table 1. Synthesis and bioactivity of selected AMBPs a .
No. | Sequence a | H b | + c | MS calc./obs. [M] | MIC BR 151 d | MIC PAO1 d | MBIC e | Dispersal f | MHC g |
1a | 2 K(1)KZ 1KLZ 2L | 2 | 2 | 914.19/914.19 | >256 | >256 | |||
1b | 1 K(2)KZ 1KLZ 2L | 2 | 2 | 914.19/914.19 | 128 | >256 | |||
11a | L1LK(L2L)KLKZ 2KKLZ 1K | 6 | 5 | 1750.11/1750.11 | 64 | >256 | |||
11b | L1LK(L2L)KLKZ 1KKLZ 2K | 6 | 5 | 1750.11/1750.11 | 16 | >256 | |||
13a | K2LLK(K1LL)KLZ 1KKLZ 2 | 6 | 5 | 1750.11/1750.11 | 16 | >256 | |||
13b | K1LLK(K2LL)KLZ 1KKLZ 2 | 6 | 5 | 1750.11/1750.11 | 16 | >256 | |||
15 | L12KK(L12K)KLKZ 21LLKZ 12L | 6 | 5 | 1750.11/1750.11 | 16 | >256 | |||
19 | K12LKK(K12LK)LLLZ 21KLKZ 12L | 7 | 6 | 1991.29/1991.29 | 8 | >256 | |||
20 | 12LLKK(L12LK)LLLZ 21KLKZ 12L | 9 | 4 | 1961.27/1961.27 | 4 | 128 | 32 | 60% | |
24 | 12LLKK(L12LK)KLKZ 21LLKZ 12L | 8 | 5 | 1976.28/1976.28 | 4 | 128 | 16 | 50% | |
26a | 1KLLK(K2LL)KLLZ 2KLKZ 1K | 7 | 6 | 1991.29/1991.30 | 32 | >256 | 125 | ||
26b | 1KLLK(K2LL)KLLZ 1KLKZ 2K | 7 | 6 | 1991.29/1991.30 | 1 | 128 | 32 | 36% | 250 |
27a | 2KLKK(K1LK)KLLZ 1LLLZ 2K | 7 | 6 | 1991.29/1991.30 | 32 | 256 | 1000 | ||
27b | 1KLKK(K2LK)KLLZ 1LLLZ 2K | 7 | 6 | 1991.29/1991.30 | 1 | 32 | 32 | 12% | 2000 |
29a | 2KLLK(K1LL)KLLZ 1KKKZ 2L | 7 | 6 | 1991.29/1991.29 | 16 | >256 | 32 | 0% | 2000 |
29b | 1KLLK(K2LL)KLLZ 1KKKZ 2L | 7 | 6 | 1991.29/1991.29 | 2 | 256 | 8 | 100% | 2000 |
36a | 2KLKK(K1LK)KLLZ 1LLKZ 2K | 6 | 7 | 2006.30/2006.30 | 32 | >256 | >32 | 0% | 2000 |
36b | 1KLKK(K2LK)KLLZ 1LLKZ 2K | 6 | 7 | 2006.30/2006.30 | 16 | 64 | 8 | 100% | 2000 |
37a | 2KLKK(K1LK)KLLZ 1KLKZ 2L | 6 | 7 | 2006.30/2006.30 | 32 | >256 | 16 | 30% | |
37b | 1KLKK(K2LK)KLLZ 1KLKZ 2L | 6 | 7 | 2006.30/2006.30 | 32 | 256 | 16 | 100% | |
39a | 1LLKK(L2LK)KKLZ 2LLLZ 1K | 8 | 5 | 1976.28/1976.28 | 16 | 128 | |||
39b | 2LLKK(L1LK)KKLZ 2LLLZ 1K | 8 | 5 | 1976.28/1976.28 | 4 | 64 | >32 | ||
56a | 1KKKK(K2KK)KLLZ 2LLLZ 1K | 5 | 8 | 2021.31/2021.31 | 4 | 128 | >32 | 0% | |
56b | 2KKKK(K1KK)KLLZ 2LLLZ 1K | 5 | 8 | 2021.31/2022.31 | 2 | 32 | 32 | 75% | |
58a | 2KFKK(K1FK)KFFZ 1FFFZ 2K | 7 | 6 | 2229.18/2230.18 | 2 | >256 | 32 | 80% | |
58b | 1KFKK(K2FK)KFFZ 1FFFZ 2K | 7 | 6 | 2229.18/2229.18 | 2 | >256 | 32 | 0% | |
59 | 12KWKK(K12WK)KWWZ 21WWWZ 12K | 7 | 6 | 2502.25/2502.25 | 1 | 64 | 32 | 0% | |
60a | 2BLBK(B1LB)BLLZ 1LLLZ 2B | 7 | 6 | 1823.10/1824.10 | 4 | 64 | >32 | 0% | |
60b | 1BLBK(B2LB)BLLZ 1LLLZ 2B | 7 | 6 | 1823.10/1823.10 | 4 | 64 | >32 | 0% | |
61 | 12RLRK(R21LR)RLLZ 21LLLZ 12R | 7 | 6 | 2160.62/2160.52 h | 1 | 64 | >32 | 0% | |
62a | 2KLKK(K1LK)KLLZ 1LLLZ 2KK(C10) | 8 | 6 | 2273.52/2273.52 | 4 | 32 | 128 | 15% | 125 |
62b | 1KLKK(K2LK)KLLZ 1LLLZ 2KK(C10) | 8 | 6 | 2273.52/2273.52 | 1 | 16–8 | 128 | 0% | 125 |
Pmx | Polymyxin B | 4 | 5 | 1301.56/1301.56 | 4 | 2 | 16 | 100% | 2000 |
+1 μg mL–1 29b | 1.5 | 100% i | |||||||
+0.5 μg mL–1 36b | 1.5 | 100% i | |||||||
DJK5 | Vqwrairvrvir | 7 | 4 | 1549.47/1549.47 | 16 | 4 | 100% | 2000 |
aSequences use standard one-letter codes for amino acids, K = branching lysine, the peptide extended on the side chain is in parentheses, Z = γ-thia-homoglutamic acid (formed by ClAc ligation of cysteine), 1 and 2 indicate cyclization points using the SMILES formalism, B = diaminobutyric acid. All C-termini are carboxamides.
b H = number of hydrophobic residues.
c+ = number of positive charges.
dMinimal inhibitory concentration in μg mL–1 in Müller–Hinton (MH)-broth.
eMinimal biofilm inhibitory conc. in μg mL–1.
fDispersal of preformed biofilm at 32 μg mL–1. MIC, MBIC and dispersal determinations were performed in independent triplicates with at least two experiments giving the same value.
gMinimal hemolytic concentration in μg mL–1 on human red blood cells (hRBC). MHC determinations were performed in duplicate and averaged.
hIn this case [M + H]+ is observed together with TFA adducts, see ESI.
iMeasured with 8 μg mL–1 of 29b or 36b in the presence of 1.5 μg mL–1 of Pmx, FIC (fractional inhibitory concentration):63 36b + Pmx = 0.155 (MBIC), 0.34 (dispersal), 29b + Pmx = 0.218 (MBIC), 0.34 (dispersal). Empty entries were not determined.