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Table 1 MICs and MPCs of orbifloxacin and QRDR mutations in the gyrA , parC , and grlA genes of the original stains and mutants used in the study

From: Mutant prevention concentration of orbifloxacin: comparison between Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus pseudintermedius of canine origin

Parent strains and mutantsa

MIC (μg/ml)

MIC (+EPI)b(μg/ml)

QRDR mutationc

MPC (μg/ml)

MPC /MIC

Cmax/MPCd

AUC /MPCd

gyrA

parC( grlA)

E. coli

E1

0.063

<0.015

wt

wt

1

16

6.9

42.9

E2

0.063

<0.015

wt

wt

0.5

8

13.8

85.8

E3

0.063

<0.015

wt

wt

1

16

6.9

42.9

E4

0.125

<0.015

wt

wt

2

16

3.45

21.45

E5

0.125

<0.015

wt

wt

2

16

3.45

21.45

E6

0.25

<0.015

wt

wt

1

4

6.9

42.9

E7

0.5

0.063

S83L

wt

16

32

0.43

2.68

E8

1

0.063

D87N

wt

8

8

0.86

5.36

E9

2

0.125

D87N

wt

8

4

0.86

5.36

E10

2

0.125

S83L

wt

32

16

0.22

1.34

EM1 (0.5)

1

0.125

S83L

wt

-

-

  

EM2 (0.25)

1

0.125

S83L

wt

-

-

  

EM3 (0.5)

1

0.125

S83L

wt

-

-

  

EM4 (1)

2

0.125

S83L

wt

-

-

  

EM5 (1)

2

0.25

S83L

wt

-

-

  

EM6 (0.5)

2

0.125

S83L

wt

-

-

  

EM7 (8)

4

0.125

S83L

wt

-

-

  

EM8 (4)

4

0.25

D87N

wt

-

-

  

EM9 (4)

8

0.25

D87N

wt

-

-

  

EM10 (16)

4

0.125

S83L

wt

-

-

  

P. aeruginosa

P1

1

0.015

wt

wt

32

32

0.22

1.34

P2

1

0.031

wt

wt

16

16

0.43

2.68

P3

1

0.063

wt

wt

32

32

0.22

1.34

P4

2

0.125

wt

wt

64

32

0.11

0.67

P5

2

0.063

wt

wt

32

16

0.22

1.34

P6

2

0.125

wt

wt

32

16

0.22

1.34

P7

2

0.031

wt

wt

64

16

0.11

0.67

P8

2

0.063

wt

wt

128

64

0.05

0.34

P9

4

0.25

wt

wt

64

16

0.11

0.67

P10

4

0.125

wt

wt

64

16

0.11

0.67

PM1 (16)

32

0.063

wt

wt

-

-

  

PM2 (8)

16

0.25

wt

wt

-

-

  

PM3 (16)

16

0.5

wt

wt

-

-

  

PM4 (32)

32

1

T83I

wt

-

-

  

PM5 (16)

32

0.25

wt

wt

-

-

  

PM6 (16)

64

0.125

wt

wt

-

-

  

PM7 (32)

64

1

T83I

wt

-

-

  

PM8 (64)

64

0.125

T83I

wt

-

-

  

PM9 (32)

128

2

T83I

wt

-

-

  

PM10 (32)

16

0.25

wt

wt

-

-

  

S. pseudintermedius

S1

0.25

0.25

wt

wt

2

8

3.45

21.45

S2

0.25

0.5

wt

wt

2

4

3.45

21.45

S3

0.25

0.5

wt

wt

8

16

0.86

5.36

S4

0.5

0.5

wt

wt

2

8

3.45

21.45

S5

0.5

0.5

wt

wt

4

8

1.73

10.73

S6

0.5

0.5

wt

wt

4

4

1.73

10.73

S7

1

1

wt

S80I

128

128

0.05

0.34

S8

1

1

wt

S80I

128

128

0.05

0.34

S9

1

1

wt

S80I

64

64

0.11

0.67

S10

1

1

wt

S80I

16

16

0.43

2.68

SM1 (1)

1

1

wt

wt

-

-

  

SM2 (1)

0.5

0.5

wt

wt

-

-

  

SM3 (4)

1

1

wt

wt

-

-

  

SM4 (1)

2

1

wt

wt

-

-

  

SM5 (2)

0.5

0.5

wt

wt

-

-

  

SM6 (2)

1

2

wt

S80I

-

-

  

SM7 (64)

64

128

S84W

S80I

-

-

  

SM8 (64)

64

128

S84L

S80I

-

-

  

SM9 (32)

8

8

wt

S80I

-

-

  

SM10 (8)

32

32

S84L

S80I

-

-

  
  1. a Number in parenthesis indicates the orbifloxacin concentration (μg/ml) supplemented in the agar from which mutants were derived.
  2. b Minimum inhibitory concentrations (MICs) in the presence of efflux pump inhibitors (EPIs).
  3. cparC of E. coli and P. aeruginosa, and grlA of S. pseudintermedius; wt, wild type; S83L, Ser-83 → Leu; D87N, Asp-87 → Asn; T83I, Thr-83 → Ile; S80I, Ser-80 → Ile; S84W, Ser84 → Trp; S84L, Ser84 → Leu.
  4. d Data for maximum concentration (Cmax: 6.9 mg/l) and area under the concentration time-curve (AUC: 42.9 mg.h/l) of orbifloxacin (dose of 7.5 mg/kg) are from reference [16].