Table 3 Sequence and activity of WCopW29 derivatives.

From: Matching amino acids membrane preference profile to improve activity of antimicrobial peptides

Compound

Sequencea

Net charge

MW

Minimum inhibitory concentrations (μM)b

Hemolysis percent (%)c

MDR P. aeruginosa

MDR A. baumannii

MDR S. aureus

MDR E. faecalis

100 μM

50 μM

25 μM

WCopW44

NH2

 

w

v

v

v

v

w

r

r

r

 

CONH2

+4

1254.5

5

2.5

1.25

1.25

4.48 ±1.01

0.87 ±0.36

0.11 ±0.03

WCopW41

NH2

 

w

1

 

w

i

w

r

r

r

 

CONH2

+4

1270.6

>5

2.5

2.5

1.25

0.42 ±0.06

0.04 ± 0.02

0.01 ±0.01

WCopW32

NH2

 

w

1

v

w

i

w

r

r

  

CONH2

+3

1213.5

>5

1.25

1.25

1.25

4.53 ±0.01

2.95 ± 0.21

1.66 ± 0.11

WCopW29

NH2

 

w

1

v

w

i

w

r

r

r

 

CONH2

+4

1369.7

5

0.63

1.25

1.25

10.04 ± 0.88

6.96 ± 0.13

2.18 ± 0.16

WCopW35

NH2

k

w

1

v

w

i

w

r

r

r

 

CONH2

+5

1497.8

2.5

0.63

0.63

0.63

6.07 ±1.01

2.71 ±0.63

1.18 ±0.34

WCopW36

NH2

d

w

1

v

w

i

w

r

r

r

 

CONH2

+3

1484.8

>5

5

1.25

1.25

9.86 ±1.62

7.48 ±0.90

4.03 ±0.40

WCopW37

NH2

 

w

1

v

w

k

w

r

r

r

 

CONH2

+5

1384.7

>5

2.5

5

5

0.16 ±0.03

0.08 ±0.01

0.13 ±0.02

WCopW38

NH2

 

w

1

v

w

d

w

r

r

r

 

CONH2

+3

1371.6

>5

>5

>5

>5

0.06 ± 0.03

0.06 ±0.06

0.06 ±0.06

WCopW61

NH2

 

w

i

i

w

i

w

r

r

r

 

CONH2

+4

1383.7

5

1.25

0.63

0.63

11.6 ±0.99

8.91 ± 0.75

6.90 ± 0.03

WCopW60

NH2

 

r

r

r

w

i

w

i

i

w

 

CONH2

+4

1383.7

5

1.25

0.63

0.63

15.17 ± 0.19

15.14 ± 3.22

15.51 ± 0.64

WCopW54

NH2

  

r

r

w

i

w

v

i

w

r

CONH2

+4

1369.7

2.5

0.63

0.63

0.63

35.13 ± 4.13

11.43 ± 2.42

8.38 ± 1.14

WCopW43

NH2

 

r

r

r

w

i

w

v

i

w

k

CONH2

+5

1497.9

1.25

0.63

0.63

0.63

5.02 ±0.63

2.22 ± 0.67

1.12 ± 0.20

WCopW47

NH2

N

r

r

r

w

i

w

v

i

w

k

CONH2

+5

1815.5

>5

1.25

2.5

2.5

2.07 ±0.23

1.19 ±0.17

0.73 ±0.05

WCopW48

NH2

r

r

r

w

i

w

v

1

w

k

N

CONH2

+5

1815.5

2.5

0.63

2.5

2.5

0.85 ±0.02

0.69 ±0.04

0.45 ±0.03

Melittin

              

2846.5

>5

1.25

1.25

1.25

97.66 ± 1.64

94.83 ±0.22

102.53 ±6.34

Colistin

              

1155.5

0.63

0.31

>5

>5

0.39 ±0.06

0.31 ±0.01

0.24 ±0.09

Daptomycin

              

1619.7

>5

>5

1.25

1.25

0.04 ±0.02

0.03 ±0.01

0.01 ±0.02

  1. aSequences of WCopW29 derivatives. Lower case letters indicate d-form amino acids; capital letters, l-form. Hydrophilic position-preferring residues are remarked as bolded letters. N of WCopW47 and WCopW48 indicate glucosylated asparagine.
  2. bMICs in the high-salt CLSI standard condition. When considering the molecular weight of AMPs (≤1.52 kDa), a MIC of 2.5 μM (≤3.8 μg/ml) remarked as bold letters and a MIC of 1.25 μM (≤1.9 μg/ml) remarked as bold and underlined letters.
  3. cHemolytic activity to 8% human red blood cells in PBS. Colistin (clinical AMP against Gram-negative MDR bacteria), daptomycin (clinical AMP against Gram-positive MDR bacteria), and melittin (one of most potent, nonclinical AMPs) were used as controls (Supplementary Table S1).
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