Table 1.
Target pumps, and characteristic antibiotic substrates of some established efflux pump inhibitors from various sources.
| Efflux Pump Inhibitors | Origin | Target Pumps (Bacteria) | Antibiotic Substrates |
References |
|---|---|---|---|---|
| Reserpine | Rauvolfia sp. | NorA, Bmr, TetK, LmrA, PmrA, MepA (B. subtilis, S. aureus, S. pneumoniae, Lactococcus lactis) | Norfloxacin, ciprofloxacin, tetracycline |
[115,116] |
| Piperine | Piper sp. | NorA, MdeA, Rv1258c (E. coli, S. aureus, Mycobacterium spp.) | Ciprofloxacin, norfloxacin | [117] |
| Berberine | Berberis sp. | MexAB-OprM, NorA (P. aeruginosa, S. aureus) | Imipenem | [122] |
| Epicatechin gallate | Camellia sinensis | NorA, TetK (S. aureus, S. epidermidis) | Oxacillin, norfloxacin | [119,120] |
| Epigallocatechin gallate | Camellia sinensis | NorA, TetK (S. aureus, S. epidermidis) | Oxacillin, norfloxacin | [119,120] |
| Carnosic acid | Rosmarinus officinalis | NorA, MsrA (S. aureus) | Erythromycin, tetracycline | [121] |
| Carnosol | Rosmarinus officinalis | NorA, MsrA (S. aureus) | Erythromycin, tetracycline | [121] |
| Baicalein | Thymus vulgaris | NorA, TetK (S. aureus, Salmonella enteridis, E. coli) | Tetracycline, ampicillin, oxacillin, ciprofloxacin | [18] |
| Porphyrin pheophorbide A | Berberis sp. | NorA (S. aureus) | Berberine | [123] |
| 5′-methoxyhydnocarpin | Berberis sp. | NorA (S. aureus) | Norfloxacin | [124] |
| EA-371α | Streptomyces | MexAB-OprM (P. aeruginosa) | Levofloxacin | [126] |
| EA-371δ | Streptomyces | MexAB-OprM (P. aeruginosa) | Levofloxacin | [126] |
| PAβN | Synthetic | MexAB-OprM (P. aeruginosa) | Levofloxacin | [127] |
| 1-(1-Naphthylmethyl)-piperazine | Synthetic | AcrAB, AcrEF (E. coli) | Levofloxacin | [130,131,132,133] |
| D13-9001 | Synthetic | AcrAB-TolC (E. coli), MexAB-OprM (P. aeruginosa) | Wide variety | [114] |
| MBX-2319 | Synthetic | AcrAB (E. coli) | ciprofloxacin, levofloxacin, piperacillin | [93,134,135] |
| Trimethoprim, sertraline | Drug repurposing | Efflux systems of P. aeruginosa | piperacillin, levofloxacin, meropenem | [140] |
| Paroxetine, fluoxetine | Drug repurposing | NorA, Bcr/CflA (S. aureus, Proteus mirabilis) | Norfloxacin, ethidium bromide | [141,142] |
| Omeprazole, lansoprazole | Drug repurposing | NorA (S. aureus) | Ciprofloxacin, norfloxacin | [142] |
| Verapamil | Drug repurposing | ABC (M. tuberculosis) | Bedaquiline | [144,145] |
| Chlorpromazine, prochlorperazine | Drug repurposing | NorA (S. aureus) | - | [146] |
| Biricodar, timcodar | Synthetic/Drug repurposing | EtBr efflux (S. aureus, E. faecalis, S. pneumoniae) | Ciprofloxacin, tetracycline, gentamicin, rifampicin, moxifloxacin, bedaquiline | [137] |
Note: ABC, ATP Binding Cassette; EtBr, Ethidium Bromide; PaβN, Phenylalanine-arginine β-naphthylamide.