Literature DB >> 34159523

Effect of Carvacrol and Thymol on NorA efflux pump inhibition in multidrug-resistant (MDR) Staphylococcus aureus strains.

Cristina Rodrigues Dos Santos Barbosa1, Jackelyne Roberta Scherf2, Thiago Sampaio de Freitas3, Irwin Rose Alencar de Menezes4, Raimundo Luiz Silva Pereira3, Joycy Francely Sampaio Dos Santos2, Sarah Silva Patrício de Jesus2, Thais Pereira Lopes2, Zildene de Sousa Silveira2, Cícera Datiane de Morais Oliveira-Tintino5, José Pinto Siqueira Júnior6, Henrique Douglas Melo Coutinho7, Saulo Relison Tintino8, Francisco Assis Bezerra da Cunha9.   

Abstract

Undue exposure to antimicrobials has led to the acquisition and development of sophisticated bacterial resistance mechanisms, such as efflux pumps, which are able to expel or reduce the intracellular concentration of various antibiotics, making them ineffective. Therefore, inhibiting this mechanism is a promising way to minimize the phenomenon of resistance in bacteria. In this sense, the present study sought to evaluate the activity of the Carvacrol (CAR) and Thymol (THY) terpenes as possible Efflux Pump Inhibitors (EPIs), by determining the Minimum Inhibitory Concentration (MIC) and the association of these compounds in subinhibitory concentrations with the antibiotic Norfloxacin and with Ethidium Bromide (EtBr) against strains SA-1199 (wild-type) and SA-1199B (overexpresses NorA) of Staphylococcus aureus. In order to verify the interaction of the terpenes with the NorA efflux protein, an in silico molecular modeling study was carried out. The assays used to obtain the MIC of CAR and THY were performed by broth microdilution, while the Efflux Pump inhibitory test was performed by the MIC modification method of the antibiotic Norfloxacin and EtBr. docking was performed using the Molegro Virtual Docker (MVD) program. The results of the study revealed that CAR and THY have moderate bacterial activity and are capable of reducing the MIC of Norfloxacin antibiotic and EtBr in strains of S. aureus carrying the NorA efflux pump. The docking results showed that these terpenes act as possible competitive NorA inhibitors and can be investigated as adjuvants in combined therapies aimed at reducing antibiotic resistance.
© 2021. The Author(s), under exclusive licence to Springer Science+Business Media, LLC, part of Springer Nature.

Entities:  

Keywords:  Antibiotic resistance; Efflux pump inhibitors; Fluoroquinolone; NorA; Terpenes

Mesh:

Substances:

Year:  2021        PMID: 34159523     DOI: 10.1007/s10863-021-09906-3

Source DB:  PubMed          Journal:  J Bioenerg Biomembr        ISSN: 0145-479X            Impact factor:   2.945


  37 in total

1.  Determination of minimum inhibitory concentrations.

Authors:  J M Andrews
Journal:  J Antimicrob Chemother       Date:  2001-07       Impact factor: 5.790

Review 2.  The hydrophobic trap-the Achilles heel of RND efflux pumps.

Authors:  Zachary Aron; Timothy J Opperman
Journal:  Res Microbiol       Date:  2017-11-13       Impact factor: 3.992

3.  Improved Potency of Indole-Based NorA Efflux Pump Inhibitors: From Serendipity toward Rational Design and Development.

Authors:  Federica Buonerba; Susan Lepri; Laura Goracci; Bryan D Schindler; Susan M Seo; Glenn W Kaatz; Gabriele Cruciani
Journal:  J Med Chem       Date:  2016-12-15       Impact factor: 7.446

4.  Antimicrobial activity of carvacrol related to its chemical structure.

Authors:  A Ben Arfa; S Combes; L Preziosi-Belloy; N Gontard; P Chalier
Journal:  Lett Appl Microbiol       Date:  2006-08       Impact factor: 2.858

5.  Inhibition of the NorA multi-drug transporter by oxygenated monoterpenes.

Authors:  Mayara Ladeira Coêlho; Josie Haydée Lima Ferreira; José Pinto de Siqueira Júnior; Glenn W Kaatz; Humberto Medeiros Barreto; Ana Amélia de Carvalho Melo Cavalcante
Journal:  Microb Pathog       Date:  2016-08-24       Impact factor: 3.738

6.  Enhancement of the antibiotic activity against a multiresistant Escherichia coli by Mentha arvensis L. and chlorpromazine.

Authors:  Henrique D M Coutinho; José G M Costa; Edeltrudes O Lima; Vivyanne S Falcão-Silva; José P Siqueira-Júnior
Journal:  Chemotherapy       Date:  2008-08-12       Impact factor: 2.544

7.  Inhibition of multidrug efflux as a strategy to prevent biofilm formation.

Authors:  Stephanie Baugh; Charlotte R Phillips; Aruna S Ekanayaka; Laura J V Piddock; Mark A Webber
Journal:  J Antimicrob Chemother       Date:  2013-10-31       Impact factor: 5.790

8.  The DNA intercalators ethidium bromide and propidium iodide also bind to core histones.

Authors:  Amrita Banerjee; Parijat Majumder; Sulagna Sanyal; Jasdeep Singh; Kuladip Jana; Chandrima Das; Dipak Dasgupta
Journal:  FEBS Open Bio       Date:  2014-02-15       Impact factor: 2.693

9.  Homology modeling, molecular dynamics, and virtual screening of NorA efflux pump inhibitors of Staphylococcus aureus.

Authors:  Baki Vijaya Bhaskar; Tirumalasetty Muni Chandra Babu; Netala Vasudeva Reddy; Wudayagiri Rajendra
Journal:  Drug Des Devel Ther       Date:  2016-10-03       Impact factor: 4.162

10.  The hydroxyl moiety on carbon one (C1) in the monoterpene nucleus of thymol is indispensable for anti-bacterial effect of thymol.

Authors:  Alex Boye; Justice Kwaku Addo; Desmond Omane Acheampong; Ama Kyeraa Thomford; Emmanuel Asante; Regina Elorm Amoaning; Dominic Nkwantabisa Kuma
Journal:  Heliyon       Date:  2020-03-17
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  5 in total

Review 1.  Targeting the Holy Triangle of Quorum Sensing, Biofilm Formation, and Antibiotic Resistance in Pathogenic Bacteria.

Authors:  Ronit Vogt Sionov; Doron Steinberg
Journal:  Microorganisms       Date:  2022-06-16

2.  Chalcone Derivatives as Potential Inhibitors of P-Glycoprotein and NorA: An In Silico and In Vitro Study.

Authors:  Minh-Tri Le; Dieu-Thuong Thi Trinh; Trieu-Du Ngo; Viet-Khoa Tran-Nguyen; Dac-Nhan Nguyen; Tung Hoang; Hoang-Minh Nguyen; Tran-Giang-Son Do; Tan Thanh Mai; Thanh-Dao Tran; Khac-Minh Thai
Journal:  Biomed Res Int       Date:  2022-03-26       Impact factor: 3.411

3.  In Silico Evaluation of the Antimicrobial Activity of Thymol-Major Compounds in the Essential Oil of Lippia thymoides Mart. & Schauer (Verbenaceae).

Authors:  Jorddy Neves Cruz; Sebastião Gomes Silva; Daniel Santiago Pereira; Antônio Pedro da Silva Souza Filho; Mozaniel Santana de Oliveira; Rafael Rodrigues Lima; Eloisa Helena de Aguiar Andrade
Journal:  Molecules       Date:  2022-07-26       Impact factor: 4.927

4.  In-Depth Study of Thymus vulgaris Essential Oil: Towards Understanding the Antibacterial Target Mechanism and Toxicological and Pharmacological Aspects.

Authors:  Sarra Akermi; Slim Smaoui; Mariam Fourati; Khaoula Elhadef; Moufida Chaari; Ahlem Chakchouk Mtibaa; Lotfi Mellouli
Journal:  Biomed Res Int       Date:  2022-07-21       Impact factor: 3.246

5.  Modulation of Drug Resistance by Furanochromones in NorA Overexpressing Staphylococcus Aureus.

Authors:  Damara F Rodrigues; Nathalie H P B Borges; Carlos Emídio S Nogueira; Josean F Tavares; Daniel Dias Rufino Arcanjo; Humberto M Barreto; José P Siqueira-Junior
Journal:  Evid Based Complement Alternat Med       Date:  2022-09-17       Impact factor: 2.650

  5 in total

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