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Gallic acid-based indanone derivative interacts synergistically with tetracycline by inhibiting efflux pump in multidrug resistant E. coli.
- Source :
-
Applied microbiology and biotechnology [Appl Microbiol Biotechnol] 2016 Mar; Vol. 100 (5), pp. 2311-25. Date of Electronic Publication: 2015 Dec 12. - Publication Year :
- 2016
-
Abstract
- The purpose of the present study was to study the synergy potential of gallic acid-based derivatives in combination with conventional antibiotics using multidrug resistant cultures of Escherichia coli. Gallic acid-based derivatives significantly reduced the MIC of tetracycline against multidrug resistant clinical isolate of E. coli. The best representative, 3-(3',4,'5'-trimethoxyphenyl)-4,5,6-trimethoxyindanone-1, an indanone derivative of gallic acid, was observed to inhibit ethidium bromide efflux and ATPase which was also supported by in silico docking. This derivative extended the post-antibiotic effect and decreased the mutation prevention concentration of tetracycline. This derivative in combination with TET was able to reduce the concentration of TNFα up to 18-fold in Swiss albino mice. This derivative was nontoxic and well tolerated up to 300 mg/kg dose in subacute oral toxicity study in mice. This is the first report of gallic acid-based indanone derivative as drug resistance reversal agent acting through ATP-dependent efflux pump inhibition.
- Subjects :
- Administration, Oral
Animals
Disease Models, Animal
Drug-Related Side Effects and Adverse Reactions
Gallic Acid administration & dosage
Gallic Acid adverse effects
Indans administration & dosage
Indans adverse effects
Macrophages drug effects
Mice
Microbial Sensitivity Tests
Molecular Docking Simulation
Shock, Septic prevention & control
Anti-Bacterial Agents pharmacology
Drug Synergism
Enzyme Inhibitors pharmacology
Escherichia coli drug effects
Gallic Acid pharmacology
Indans pharmacology
Tetracycline pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1432-0614
- Volume :
- 100
- Issue :
- 5
- Database :
- MEDLINE
- Journal :
- Applied microbiology and biotechnology
- Publication Type :
- Academic Journal
- Accession number :
- 26658982
- Full Text :
- https://doi.org/10.1007/s00253-015-7152-6