Table 3. Summary of the Potentiating Effects of Efflux Pump Inhibitors.
no. | OM permeabilizers | molecular structure | combined drug | microbial species | proposed mechanisms | MICa of drug alone | MICa in combination | fold decrease | FIC | ref |
---|---|---|---|---|---|---|---|---|---|---|
a | PAβN | Scheme 3a | ciprofloxacin | P. aeruginosa | bind to the drug-binding pocket | 0.125 | 0.032 | 4 | N.A. | (105) |
b | D13-9001 | Scheme 3b | carbenicillin | P. aeruginosa | jam the machinery of efflux | 64/128 | 4 | 16/32 | N.A. | (110) |
c | BDM88855 | Scheme 3c | oxacillin | E. coli | jam the machinery of efflux | >100* | 3.0* | >33.3 | N.A. | (91) |
d | MBX3132 | Scheme 3d | minocycline | E. coli | bind to the drug-binding pocket | 1 | 0.25 | 4 | N.A. | (111) |
e | MBX3132 | Scheme 3e | levofloxacin | K. pneumoniae | bind to the drug-binding pocket | 1 | 0.25 | 4 | N.A. | (111) |
f | MBX4191 | Scheme 3f | minocycline | E. coli, K. pneumoniae | bind to the drug-binding pocket | 32–128 | 4 | 8–32 | N.A. | (112) |
g | β-thujaplicin analogs | Scheme 3g | doxycycline | E. coli | downregulate the expression of efflux pumps | 156* | 122* | 1.3 | N.A. | (103) |
h | Loperamide | Scheme 3h | minocycline | P. aeruginosa | PMF collapse | 32 | 1 | 32 | <0.28 | (104) |
i | IITR08027 | Scheme 3i | norfloxacin | E. coli | PMF collapse | 0.3215 | 0.0098 | 32 | N.A. | (116) |
j | econazole | Scheme 3j | colistin | E. coli | PMF collapse | >64 | 0.5 | 128 | <0.5 | (118) |
k | tobramycin-efflux pump inhibitor hybrid | Scheme 3k | minocycline | P. aeruginosa | PMF collapse | 8 | 0.5 | 16 | 0.19 | (120) |
l | tobramycin-lysine hybrid | Scheme 3l | novobiocin | P. aeruginosa | PMF collapse | 1024 | 8 | 128 | 0.04 | (122) |
m | C12(ω7) K-β12 | Scheme 3m | erythromycin | E. coli | PMF collapse | 512 | 0.5 | 1024 | ≤0.20 | (124) |
n | PAS8-b-PDM12 | Scheme 2g | novobiocin | E. coli | PMF collapse | 100 | 0.195 | 512 | 0.25 | (82) |
The MIC is given as μg/mL, except when specified by “*”, which indicates that the MIC is given as μM. PMF, proton motive force; N.A., not available.