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. 2013 May 1;55(1):37. doi: 10.1186/1751-0147-55-37

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

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 - -    

a Number in parenthesis indicates the orbifloxacin concentration (μg/ml) supplemented in the agar from which mutants were derived.

b Minimum inhibitory concentrations (MICs) in the presence of efflux pump inhibitors (EPIs).

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.

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].