Detail publikačního výsledku

Phytol Derivatives as Drug Resistance Reversal Agents

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

Originální název

Phytol Derivatives as Drug Resistance Reversal Agents

Anglický název

Phytol Derivatives as Drug Resistance Reversal Agents

Druh

Článek WoS

Originální abstrakt

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.

Anglický abstrakt

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.

Klíčová slova

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

Klíčová slova v angličtině

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

Autoři

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

Rok RIV

2015

Vydáno

01.02.2014

Nakladatel

WILEY-VCH Verlag GmbH & Co. KGaA

Místo

Weinheim

ISSN

1860-7187

Periodikum

ChemMedChem

Svazek

9

Číslo

8

Stát

Spolková republika Německo

Strany od

1860

Strany do

1868

Strany počet

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="1860-7179"
}