Table 1 Accumulation of fluoroquinolones: SICARIN and SICAREF indexes.

From: Fluoroquinolone structure and translocation flux across bacterial membrane

Compound

SICARIN

SICAREF

Accumulated drug (10−11 µg/bacterial cell)

R

R′

AG100A*

AG100*

AG102*

AG100A/AG100

AG100A/AG102

5 min accumulation

FLE

0.80 (±0.25)

0.42 (±0.16)

0.44 (±0.07)

1.9

1.8

CIP

1.50 (±0.46)

0.82 (±0.37)

0.69 (±0.26)

1.8

2.2

SANO1

9.26 (±2.81)

2.5 (±1.62)

1.86 (±0.58)

3.7

5.0

15 min accumulation

FLE

0.92 (±0.19)

0.56 (±0.26)

0.48 (±0.09)

1.6

1.9

CIP

1.55 (±0.46)

0.98 (±0.32)

0.83 (±0.12)

1.6

1.9

SANO1

9.12 (±2.41)

2.98 (±1.90)

1.27 (±0.008)

3.1

7.2

  1. Intracellular accumulation of fluoroquinolones (FLE, CIP and SANO1, in 10−11 µg/bacterial cell). The accumulation was performed in AG100 (WT), AG100A (AcrAB-) and AG102 (AcrAB++) E. coli strains incubated 5 and 15 min with 2 mg/L of molecules in the absence and in the presence of CCCP (10 µM) and lysated by HCl-glycine. (Histograms are presented in Figure S1).
  2. *Means of three independent assays performed in triplicates.