Publication detail

Phytol Derivatives as Drug Resistance Reversal Agents

UPADHYAY, H. DWIVEDI, G. ROY, S. SHARMA, A. DAROKAR, M. SRIVASTAVA, S.

Original Title

Phytol Derivatives as Drug Resistance Reversal Agents

Type

journal article in Web of Science

Language

English

Original Abstract

Phytol was chemically transformed into fifteen semi-synthetic derivatives, which were evaluated for their antibacterial and drug resistance reversal potential in combination with nalidixic acid against E. coli strains CA8000 and DH5a. The pivaloyl (4), 3,4,5-trimethoxybenzoyl (9), 2,3-dichlorobenzoyl (10), cinnamoyl (11), and aldehyde (14) derivatives of phytol ((2E,7R,11R)- 3,7,11,15-tetramethyl-2-hexadecen-1-ol) were evaluated by using another antibiotic, tetracycline, against the MDREC-KG4 clinical isolate of E. coli. Derivative 4 decreased the maximal inhibitory concentration (MIC) of the antibiotics by 16-fold, while derivatives 9, 10, 11, and 14 reduced MIC values of the antibiotics up to eightfold against the E. coli strains. Derivatives 4, 9, 10, 11, and 14 inhibited the ATP-dependent efflux pump; this was also supported by their in silico binding affinity and down-regulation of the efflux pump gene yojI, which encodes the multidrug ATP-binding cassette transporter protein. This study supports the possible use of phytol derivatives in the development of cost-effective antibacterial combinations.

Keywords

antibiotics; docking studies; drug resistance; efflux pumps; phytol

Authors

UPADHYAY, H.; DWIVEDI, G.; ROY, S.; SHARMA, A.; DAROKAR, M.; SRIVASTAVA, S.

RIV year

2014

Released

1. 2. 2014

Publisher

WILEY-VCH Verlag GmbH & Co. KGaA

Location

Weinheim

ISBN

1860-7187

Periodical

ChemMedChem

Year of study

9

Number

8

State

Federal Republic of Germany

Pages from

1860

Pages to

1868

Pages count

9

BibTex

@article{BUT108954,
  author="Harish {Upadhyay} and Guarav {Dwivedi} and Sudeep {Roy} and Ashok {Sharma} and Mahendra {Darokar} and Santosh {Srivastava}",
  title="Phytol Derivatives as Drug Resistance Reversal Agents",
  journal="ChemMedChem",
  year="2014",
  volume="9",
  number="8",
  pages="1860--1868",
  doi="10.1002/cmdc.201402027",
  issn="1860-7187"
}