Publication detail

Gallic acid based indanone derivative interacts synergistically with tetracycline by inhibiting efflux pump in multidrug resistant E. coli

DWIVEDI, G. TIWARI, N. SINGH, A. KUMAR, A. ROY, S. NEGI, A. PAL, A. CHANDA, D. SHARMA, A. DAROKAR, M.

Original Title

Gallic acid based indanone derivative interacts synergistically with tetracycline by inhibiting efflux pump in multidrug resistant E. coli

English Title

Gallic acid based indanone derivative interacts synergistically with tetracycline by inhibiting efflux pump in multidrug resistant E. coli

Type

journal article in Web of Science

Language

en

Original 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.

English 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.

Keywords

Gallic acid, Indanone derivative, Efflux pump inhibition, Synergy, ATPase, Subacute oral toxicity

Released

01.03.2016

Publisher

Springer-Verlag Berlin Heidelberg

Location

Heidelberg

Pages from

2311

Pages to

2325

Pages count

15

URL

BibTex


@article{BUT121531,
  author="Guarav {Dwivedi} and Nimisha {Tiwari} and Aastha {Singh} and Akhil {Kumar} and Sudeep {Roy} and Arvind Singh {Negi} and Anirban {Pal} and Debabrata {Chanda} and Ashok {Sharma} and Mahendra {Darokar}",
  title="Gallic acid based indanone derivative interacts synergistically with tetracycline by inhibiting efflux pump in multidrug resistant E. coli",
  annote="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.",
  address="Springer-Verlag Berlin Heidelberg",
  chapter="121531",
  doi="10.1007/s00253-015-7152-6",
  howpublished="online",
  institution="Springer-Verlag Berlin Heidelberg",
  number="5",
  volume="100",
  year="2016",
  month="march",
  pages="2311--2325",
  publisher="Springer-Verlag Berlin Heidelberg",
  type="journal article in Web of Science"
}