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. 2017 Jul 13;8(10):6784–6798. doi: 10.1039/c7sc01314k

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.