Gallic acid-based indanone derivative interacts synergistically with tetracycline by inhibiting efflux pump in multidrug resistant E. coli
Language English Country Germany Media print-electronic
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
26658982
DOI
10.1007/s00253-015-7152-6
PII: 10.1007/s00253-015-7152-6
Knihovny.cz E-resources
- Keywords
- ATPase, Efflux pump inhibition, Gallic acid, Indanone derivative, Subacute oral toxicity, Synergy,
- MeSH
- Anti-Bacterial Agents pharmacology MeSH
- Administration, Oral MeSH
- Escherichia coli drug effects MeSH
- Indans administration & dosage adverse effects pharmacology MeSH
- Enzyme Inhibitors pharmacology MeSH
- Gallic Acid administration & dosage adverse effects pharmacology MeSH
- Macrophages drug effects MeSH
- Microbial Sensitivity Tests MeSH
- Disease Models, Animal MeSH
- Mice MeSH
- Drug-Related Side Effects and Adverse Reactions MeSH
- Shock, Septic prevention & control MeSH
- Molecular Docking Simulation MeSH
- Drug Synergism * MeSH
- Tetracycline pharmacology MeSH
- Animals MeSH
- Check Tag
- Mice MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Anti-Bacterial Agents MeSH
- indacrinone MeSH Browser
- Indans MeSH
- Enzyme Inhibitors MeSH
- Gallic Acid MeSH
- Tetracycline MeSH
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.
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