Table 2 Antimicrobial activity and cellular toxicity.

From: A pleurocidin analogue with greater conformational flexibility, enhanced antimicrobial potency and in vivo therapeutic efficacy

Isolate

Peptide concentration (µg/ml)

Pleurocidin

d-pleurocidin

Pleurocidin-KR

d-pleurocidin-KR

Pleurocidin-VA

d-pleurocidin-VA

Gram-negative

Klebsiella pneumoniae NCTC 13368

4–8 (32)

4 (8–16)

2–4 (32)

2 (4)

4–8 (32)

8 (32)

Klebsiella pneumoniae M6

4 (32)

4 (4–8)

2 (32)

2 (4)

4–8 (32)

4 (32)

Acinetobacter baumannii AYE

1–2 (4–8)

1 (2)

1–2 (8–16)

2 (2)

2 (16)

1 (8–32)

Acinetobacter baumannii ATCC 17978

1–2 (8)

1 (8)

1 (8)

2 (4)

1–2 (32)

1 (16)

Pseudomonas aeruginosa PAO1

64 (>32)

2 (16)

4 (>32)

4 (16)

16–32 (>32)

4 (32)

Pseudomonas aeruginosa NCTC 13437

16–32 (>32)

8 (16–32)

8 (>32)

4 (16)

32 (>32)

32 (>32)

Escherichia coli NCTC 12923

1–2 (16)

1 (2–4)

1 (16)

1 (2)

1 (32)

1 (8)

Gram-positive

 MS Staphylococcus aureus ATCC 9144

4 (2)

2 (0.5)

2 (4)

2 (0.25–0.5)

8 (32)

4 (8)

 EMR Staphylococcus aureus-15 NCTC 13616

16 (4)

16 (1)

4 (4)

2 (0.5)

64 (32)

32 (8)

 EMR Staphylococcus aureus-16 NCTC 13277

16 (4)

16 (1)

4 (8)

4 (1)

64–128 (>32)

64 (32)

 VS Enterococcus faecalis NCTC 775

64 (NG)

32 (NG)

16 (NG)

8 (NG)

64–128 (NG)

64 (NG)

 VR Enterococcus faecium NCTC 12204

16–32 (32)

16 (4)

4 (16)

2 (2)

32–64 (32)

16 (32–64)

Toxicity

 HEK293

(87.5 ± 11.1)

(61.4 ± 3.9)

(40.1 ± 4.1)

(36.4 ± 4.3)

(~400)

(217.3 ± 46.5)

 HeLa

(58.2 ± 3.9)

(47.1 ± 2.1)

(30.7 ± 2.6)

(25.3 ± 2.2)

(>400)

(198.2 ± 10.2)

 A549

n.d.

(79.3 ± 7.2)

n.d.

(56.5 ± 4.5)

n.d.

(>250)

 Calu-3

n.d.

(41.9 ± 1.8)

n.d.

(39.1 ± 1.8)

n.d.

(>250)

 SI

 HEK293 /EMRSA-15

5.5 (21.9)

3.8 (61.4)

10.0 (10.0)

18.2 (72.8)

6.25 (12.5)

6.8 (27.2)

 A549/EMRSA-15

n.d.

5.0 (79.3)

n.d.

28.3 (113.0)

n.d.

>7.8 (>31.2)

  1. Values are given for peptides tested in Mueller Hinton broth with values obtained in RPMI given in parentheses. The selectivity index is the EC50 divided by the MIC in the indicated conditions. Italic or bold values indicate, respectively, a significant (factor of 2 or more) reduction or improvement in potency in RPMI.
  2. MS methicillin sensitive, EMR epidemic methicillin resistant, VS vancomycin sensitive, VR vancomycin resistant.