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Journal articles on the topic 'Bacterial efflux pumps'

Author: Grafiati

Published: 24 April 2022

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1

Huang, Lulu, Cuirong Wu, Haijiao Gao, et al. "Bacterial Multidrug Efflux Pumps at the Frontline of Antimicrobial Resistance: An Overview." Antibiotics 11, no. 4 (2022): 520. http://dx.doi.org/10.3390/antibiotics11040520.

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Multidrug efflux pumps function at the frontline to protect bacteria against antimicrobials by decreasing the intracellular concentration of drugs. This protective barrier consists of a series of transporter proteins, which are located in the bacterial cell membrane and periplasm and remove diverse extraneous substrates, including antimicrobials, organic solvents, toxic heavy metals, etc., from bacterial cells. This review systematically and comprehensively summarizes the functions of multiple efflux pumps families and discusses their potential applications. The biological functions of efflux

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2

Pasqua, Grossi, Zennaro, et al. "The Varied Role of Efflux Pumps of the MFS Family in the Interplay of Bacteria with Animal and Plant Cells." Microorganisms 7, no. 9 (2019): 285. http://dx.doi.org/10.3390/microorganisms7090285.

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Efflux pumps represent an important and large group of transporter proteins found in all organisms. The importance of efflux pumps resides in their ability to extrude a wide range of antibiotics, resulting in the emergence of multidrug resistance in many bacteria. Besides antibiotics, multidrug efflux pumps can also extrude a large variety of compounds: Bacterial metabolites, plant-produced compounds, quorum-sensing molecules, and virulence factors. This versatility makes efflux pumps relevant players in interactions not only with other bacteria, but also with plant or animal cells. The multid

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Stubenrauch, Christopher J., Rebecca S. Bamert, Jiawei Wang, and Trevor Lithgow. "A noncanonical chaperone interacts with drug efflux pumps during their assembly into bacterial outer membranes." PLOS Biology 20, no. 1 (2022): e3001523. http://dx.doi.org/10.1371/journal.pbio.3001523.

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Bacteria have membrane-spanning efflux pumps to secrete toxic compounds ranging from heavy metal ions to organic chemicals, including antibiotic drugs. The overall architecture of these efflux pumps is highly conserved: with an inner membrane energy-transducing subunit coupled via an adaptor protein to an outer membrane conduit subunit that enables toxic compounds to be expelled into the environment. Here, we map the distribution of efflux pumps across bacterial lineages to show these proteins are more widespread than previously recognised. Complex phylogenetics support the concept that gene c

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4

Kvist, Malin, Viktoria Hancock, and Per Klemm. "Inactivation of Efflux Pumps Abolishes Bacterial Biofilm Formation." Applied and Environmental Microbiology 74, no. 23 (2008): 7376–82. http://dx.doi.org/10.1128/aem.01310-08.

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ABSTRACT Bacterial biofilms cause numerous problems in health care and industry; notably, biofilms are associated with a large number of infections. Biofilm-dwelling bacteria are particularly resistant to antibiotics, making it hard to eradicate biofilm-associated infections. Bacteria rely on efflux pumps to get rid of toxic substances. We discovered that efflux pumps are highly active in bacterial biofilms, thus making efflux pumps attractive targets for antibiofilm measures. A number of efflux pump inhibitors (EPIs) are known. EPIs were shown to reduce biofilm formation, and in combination t

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5

Marquez, Béatrice. "Bacterial efflux systems and efflux pumps inhibitors." Biochimie 87, no. 12 (2005): 1137–47. http://dx.doi.org/10.1016/j.biochi.2005.04.012.

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6

Ebbensgaard, Anna Elisabeth, Anders Løbner-Olesen, and Jakob Frimodt-Møller. "The Role of Efflux Pumps in the Transition from Low-Level to Clinical Antibiotic Resistance." Antibiotics 9, no. 12 (2020): 855. http://dx.doi.org/10.3390/antibiotics9120855.

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Antibiotic resistance is on the rise and has become one of the biggest public health challenges of our time. Bacteria are able to adapt to the selective pressure exerted by antibiotics in numerous ways, including the (over)expression of efflux pumps, which represents an ancient bacterial defense mechanism. Several studies show that overexpression of efflux pumps rarely provides clinical resistance but contributes to a low-level resistance, which allows the bacteria to persist at the infection site. Furthermore, recent studies show that efflux pumps, apart from pumping out toxic substances, are

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Zwama, Martijn, and Kunihiko Nishino. "Ever-Adapting RND Efflux Pumps in Gram-Negative Multidrug-Resistant Pathogens: A Race against Time." Antibiotics 10, no. 7 (2021): 774. http://dx.doi.org/10.3390/antibiotics10070774.

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The rise in multidrug resistance (MDR) is one of the greatest threats to human health worldwide. MDR in bacterial pathogens is a major challenge in healthcare, as bacterial infections are becoming untreatable by commercially available antibiotics. One of the main causes of MDR is the over-expression of intrinsic and acquired multidrug efflux pumps, belonging to the resistance-nodulation-division (RND) superfamily, which can efflux a wide range of structurally different antibiotics. Besides over-expression, however, recent amino acid substitutions within the pumps themselves—causing an increase

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8

Kumar, Sanath, Mun Mun Mukherjee, and Manuel F. Varela. "Modulation of Bacterial Multidrug Resistance Efflux Pumps of the Major Facilitator Superfamily." International Journal of Bacteriology 2013 (December 5, 2013): 1–15. http://dx.doi.org/10.1155/2013/204141.

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Bacterial infections pose a serious public health concern, especially when an infectious disease has a multidrug resistant causative agent. Such multidrug resistant bacteria can compromise the clinical utility of major chemotherapeutic antimicrobial agents. Drug and multidrug resistant bacteria harbor several distinct molecular mechanisms for resistance. Bacterial antimicrobial agent efflux pumps represent a major mechanism of clinical resistance. The major facilitator superfamily (MFS) is one of the largest groups of solute transporters to date and includes a significant number of bacterial d

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9

Durães, Fernando, Madalena Pinto, and Emília Sousa. "Medicinal Chemistry Updates on Bacterial Efflux Pump Modulators." Current Medicinal Chemistry 25, no. 42 (2019): 6030–69. http://dx.doi.org/10.2174/0929867325666180209142612.

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Antibiotic resistance is one of the most pressing health issues of our days. It can arise due to a multiplicity of factors, such as target modification, decrease in the drug uptake, changes in the metabolic pathways and activation of efflux pumps. The overexpression of efflux pumps is responsible for the extrusion of drugs, making antibiotic therapy fail, as the quantity of intracellular antibiotic is not enough to provide the desired therapeutic effect. Efflux pumps can be included in five families according to their composition, nature of substrates, energy source, and number of transmembran

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10

Martins, Marta, Matthew P. McCusker, Miguel Viveiros, et al. "A Simple Method for Assessment of MDR Bacteria for Over-Expressed Efflux Pumps." Open Microbiology Journal 7, no. 1 (2013): 72–82. http://dx.doi.org/10.2174/1874285801307010072.

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It is known that bacteria showing a multi-drug resistance phenotype use several mechanisms to overcome the action of antibiotics. As a result, this phenotype can be a result of several mechanisms or a combination of thereof. The main mechanisms of antibiotic resistance are: mutations in target genes (such as DNA gyrase and topoisomerase IV); over-expression of efflux pumps; changes in the cell envelope; down regulation of membrane porins, and modified lipopolysaccharide component of the outer cell membrane (in the case of Gram-negative bacteria). In addition, adaptation to the environment, suc

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11

Mahamoud, Abdallah, Jacqueline Chevalier, Milad Baitiche, Elissavet Adam, and Jean-Marie Pagès. "An alkylaminoquinazoline restores antibiotic activity in Gram-negative resistant isolates." Microbiology 157, no. 2 (2011): 566–71. http://dx.doi.org/10.1099/mic.0.045716-0.

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To date, various bacterial drug efflux pump inhibitors (EPIs) have been described. They exhibit variability in their activity spectrum with respect to antibiotic structural class and bacterial species. Among the various 4-alkylaminoquinazoline derivatives synthesized and studied in this work, one molecule, 1167, increased the susceptibility of important human-pathogenic, resistant, Gram-negative bacteria towards different antibiotic classes. This 4-(3-morpholinopropylamino)-quinazoline induced an increase in the activity of chloramphenicol, nalidixic acid, norfloxacin and sparfloxacin, which a

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12

Waditzer, Martin, and Franz Bucar. "Flavonoids as Inhibitors of Bacterial Efflux Pumps." Molecules 26, no. 22 (2021): 6904. http://dx.doi.org/10.3390/molecules26226904.

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Flavonoids are widely occurring secondary plant constituents, and are abundant in vegetable and fruit diets as well as herbal medicines. Therapeutic treatment options for bacterial infections are limited due to the spread of antimicrobial resistances. Hence, in a number of studies during the last few years, different classes of plant secondary metabolites as resistance-modifying agents have been carried out. In this review, we present the role of flavonoids as inhibitors of bacterial efflux pumps. Active compounds could be identified in the subclasses of chalcones, flavan-3-ols, flavanones, fl

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13

MALLÉA, Monique, Abdallah MAHAMOUD, Jacqueline CHEVALIER, et al. "Alkylaminoquinolines inhibit the bacterial antibiotic efflux pump in multidrug-resistant clinical isolates." Biochemical Journal 376, no. 3 (2003): 801–5. http://dx.doi.org/10.1042/bj20030963.

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Over the last decade, MDR (multidrug resistance) has increased worldwide in microbial pathogens by efflux mechanisms, leading to treatment failures in human infections. Several Gram-negative bacteria efflux pumps have been described. These proteinaceous channels are capable of expelling structurally different drugs across the envelope and conferring antibiotic resistance in various bacterial pathogens. Combating antibiotic resistance is an urgency and the blocking of efflux pumps is an attractive response to the emergence of MDR phenotypes in infectious bacteria. In the present study, various

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14

Kumar, Sanath, and Manuel F. Varela. "Biochemistry of Bacterial Multidrug Efflux Pumps." International Journal of Molecular Sciences 13, no. 4 (2012): 4484–95. http://dx.doi.org/10.3390/ijms13044484.

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15

Durães, Fernando, Sara Cravo, Joana Freitas-Silva, et al. "Enantioselectivity of Chiral Derivatives of Xanthones in Virulence Effects of Resistant Bacteria." Pharmaceuticals 14, no. 11 (2021): 1141. http://dx.doi.org/10.3390/ph14111141.

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Antimicrobial peptides are one of the lines of defense produced by several hosts in response to bacterial infections. Inspired by them and recent discoveries of xanthones as bacterial efflux pump inhibitors, chiral amides with a xanthone scaffold were planned to be potential antimicrobial adjuvants. The chiral derivatives of xanthones were obtained by peptide coupling reactions between suitable xanthones with enantiomerically pure building blocks, yielding derivatives with high enantiomeric purity. Among 18 compounds investigated for their antimicrobial activity against reference strains of ba

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16

Chitsaz, Mohsen, and Melissa H. Brown. "The role played by drug efflux pumps in bacterial multidrug resistance." Essays in Biochemistry 61, no. 1 (2017): 127–39. http://dx.doi.org/10.1042/ebc20160064.

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Antimicrobial resistance is a current major challenge in chemotherapy and infection control. The ability of bacterial and eukaryotic cells to recognize and pump toxic compounds from within the cell to the environment before they reach their targets is one of the important mechanisms contributing to this phenomenon. Drug efflux pumps are membrane transport proteins that require energy to export substrates and can be selective for a specific drug or poly-specific that can export multiple structurally diverse drug compounds. These proteins can be classified into seven groups based on protein sequ

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Mateus, Cristiana, Ana Rita Nunes, Mónica Oleastro, Fernanda Domingues, and Susana Ferreira. "RND Efflux Systems Contribute to Resistance and Virulence of Aliarcobacter butzleri." Antibiotics 10, no. 7 (2021): 823. http://dx.doi.org/10.3390/antibiotics10070823.

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Aliarcobacter butzleri is an emergent enteropathogen that can be found in a range of environments. This bacterium presents a vast repertoire of efflux pumps, such as the ones belonging to the resistance nodulation cell division family, which may be associated with bacterial resistance, as well as virulence. Thus, this work aimed to evaluate the contribution of three RND efflux systems, AreABC, AreDEF and AreGHI, in the resistance and virulence of A. butzleri. Mutant strains were constructed by inactivation of the gene that encodes the inner membrane protein of these systems. The bacterial resi

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18

Bremner, John B. "Some approaches to new antibacterial agents." Pure and Applied Chemistry 79, no. 12 (2007): 2143–53. http://dx.doi.org/10.1351/pac200779122143.

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Bacteria use a number of resistance mechanisms to counter the antibacterial challenge, and one of these is the expression of transmembrane protein-based efflux pumps which can pump out antibacterials from within the cells, thus lowering the antibacterial concentration to nonlethal levels. For example, in S. aureus, the NorA pump can pump out the antibacterial alkaloid berberine and ciprofloxacin. One general strategy to reduce the health threat of resistant bacteria is to block a major bacterial resistance mechanism at the same time as interfering with another bacterial pathway or target site.

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19

Durães, Fernando, Andreia Palmeira, Bárbara Cruz, et al. "Antimicrobial Activity of a Library of Thioxanthones and Their Potential as Efflux Pump Inhibitors." Pharmaceuticals 14, no. 6 (2021): 572. http://dx.doi.org/10.3390/ph14060572.

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The overexpression of efflux pumps is one of the causes of multidrug resistance, which leads to the inefficacy of drugs. This plays a pivotal role in antimicrobial resistance, and the most notable pumps are the AcrAB-TolC system (AcrB belongs to the resistance-nodulation-division family) and the NorA, from the major facilitator superfamily. In bacteria, these structures can also favor virulence and adaptation mechanisms, such as quorum-sensing and the formation of biofilm. In this study, the design and synthesis of a library of thioxanthones as potential efflux pump inhibitors are described. T

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20

Durães, Fernando, Diana I. S. P. Resende, Andreia Palmeira, et al. "Xanthones Active against Multidrug Resistance and Virulence Mechanisms of Bacteria." Antibiotics 10, no. 5 (2021): 600. http://dx.doi.org/10.3390/antibiotics10050600.

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The emergence of multidrug and extensively drug-resistant pathogenic bacteria able to resist to the action of a wide range of antibiotics is becoming a growing problem for public health. The search for new compounds with the potential to help in the reversion of bacterial resistance plays an important role in current medicinal chemistry research. Under this scope, bacterial efflux pumps are responsible for the efflux of antimicrobials, and their inhibition could reverse resistance. In this study, the multidrug resistance reversing activity of a series of xanthones was investigated. Firstly, do

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21

Colclough, Abigail L., Ilyas Alav, Emily E. Whittle, et al. "RND efflux pumps in Gram-negative bacteria; regulation, structure and role in antibiotic resistance." Future Microbiology 15, no. 2 (2020): 143–57. http://dx.doi.org/10.2217/fmb-2019-0235.

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Rresistance-nodulation-division (RND) efflux pumps in Gram-negative bacteria remove multiple, structurally distinct classes of antimicrobials from inside bacterial cells therefore directly contributing to multidrug resistance. There is also emerging evidence that many other mechanisms of antibiotic resistance rely on the intrinsic resistance conferred by RND efflux. In addition to their role in antibiotic resistance, new information has become available about the natural role of RND pumps including their established role in virulence of many Gram-negative organisms. This review also discusses

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22

Palazzotti, Deborah, Maicol Bissaro, Giovanni Bolcato, et al. "Deciphering the Molecular Recognition Mechanism of Multidrug Resistance Staphylococcus aureus NorA Efflux Pump Using a Supervised Molecular Dynamics Approach." International Journal of Molecular Sciences 20, no. 16 (2019): 4041. http://dx.doi.org/10.3390/ijms20164041.

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The use and misuse of antibiotics has resulted in critical conditions for drug-resistant bacteria emergency, accelerating the development of antimicrobial resistance (AMR). In this context, the co-administration of an antibiotic with a compound able to restore sufficient antibacterial activity may be a successful strategy. In particular, the identification of efflux pump inhibitors (EPIs) holds promise for new antibiotic resistance breakers (ARBs). Indeed, bacterial efflux pumps have a key role in AMR development; for instance, NorA efflux pump contributes to Staphylococcus aureus (S. aureus)

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23

Nishino, Kunihiko. "Physiological Role of Bacterial Multidrug Efflux Pumps." YAKUGAKU ZASSHI 132, no. 1 (2012): 45–50. http://dx.doi.org/10.1248/yakushi.132.45.

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24

Poole, Keith. "Bacterial Multidrug Efflux Pumps Serve Other Functions." Microbe Magazine 3, no. 4 (2008): 179–85. http://dx.doi.org/10.1128/microbe.3.179.1.

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25

Henderson, Peter J. F., Claire Maher, Liam D. H. Elbourne, Bart A. Eijkelkamp, Ian T. Paulsen, and Karl A. Hassan. "Physiological Functions of Bacterial “Multidrug” Efflux Pumps." Chemical Reviews 121, no. 9 (2021): 5417–78. http://dx.doi.org/10.1021/acs.chemrev.0c01226.

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26

Kumar, Ayush, Kim-Lee Chua, and Herbert P. Schweizer. "Method for Regulated Expression of Single-Copy Efflux Pump Genes in a Surrogate Pseudomonas aeruginosa Strain: Identification of the BpeEF-OprC Chloramphenicol and Trimethoprim Efflux Pump of Burkholderia pseudomallei 1026b." Antimicrobial Agents and Chemotherapy 50, no. 10 (2006): 3460–63. http://dx.doi.org/10.1128/aac.00440-06.

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ABSTRACT Construction and integration of recombinant mini-Tn7 expression vectors into the chromosome of a surrogate, efflux-sensitized, and biosafe Pseudomonas aeruginosa host was validated as a generally applicable method for studies of uncharacterized bacterial efflux pumps. Using this method, the Burkholderia pseudomallei bpeEF-oprC operon was shown to encode a chloramphenicol and trimethoprim efflux pump.

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Brissette, Catherine A., та Sheila A. Lukehart. "Mechanisms of Decreased Susceptibility to β-Defensins by Treponema denticola". Infection and Immunity 75, № 5 (2007): 2307–15. http://dx.doi.org/10.1128/iai.01718-06.

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ABSTRACT Treponema denticola, a periodontal pathogen, is relatively resistant to human beta-defensins, which are small cationic antimicrobial peptides produced by a number of cells, including the gingival epithelium. Using two independent methods, we previously demonstrated that T. denticola proteases are not responsible for decreased vulnerability to defensins. In this study, we confirmed that the major outer membrane protease, dentilisin, is not responsible for T. denticola insensitivity to defensins and examined several other possible mechanisms, including reduced binding to the bacterial s

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28

Jamshidi, Shirin, J. Mark Sutton, and Khondaker M. Rahman. "An overview of bacterial efflux pumps and computational approaches to study efflux pump inhibitors." Future Medicinal Chemistry 8, no. 2 (2016): 195–210. http://dx.doi.org/10.4155/fmc.15.173.

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29

Scoffone, Viola Camilla, Gabriele Trespidi, Giulia Barbieri, Samuele Irudal, Elena Perrin, and Silvia Buroni. "Role of RND Efflux Pumps in Drug Resistance of Cystic Fibrosis Pathogens." Antibiotics 10, no. 7 (2021): 863. http://dx.doi.org/10.3390/antibiotics10070863.

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Drug resistance represents a great concern among people with cystic fibrosis (CF), due to the recurrent and prolonged antibiotic therapy they should often undergo. Among Multi Drug Resistance (MDR) determinants, Resistance-Nodulation-cell Division (RND) efflux pumps have been reported as the main contributors, due to their ability to extrude a wide variety of molecules out of the bacterial cell. In this review, we summarize the principal RND efflux pump families described in CF pathogens, focusing on the main Gram-negative bacterial species (Pseudomonas aeruginosa, Burkholderia cenocepacia, Ac

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30

Kraatz, Mareike, Terence R. Whitehead, Michael A. Cotta, Mark A. Berhow, and Mark A. Rasmussen. "Effects of Chlorophyll-Derived Efflux Pump Inhibitor Pheophorbide a and Pyropheophorbide a on Growth and Macrolide Antibiotic Resistance of Indicator and Anaerobic Swine Manure Bacteria." International Journal of Antibiotics 2014 (February 11, 2014): 1–14. http://dx.doi.org/10.1155/2014/185068.

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Natural plant compounds, such as the chlorophyll a catabolites pheophorbide a (php) and pyropheophorbide a (pyp), are potentially active in the gastrointestinal tracts and manure of livestock as antimicrobial resistance-modifying agents through inhibition of bacterial efflux pumps. To investigate whether php, a known efflux pump inhibitor, and pyp influence bacterial resistance, we determined their long-term effects on the MICs of erythromycin for reference strains of clinically relevant indicator bacteria with macrolide or multidrug resistance efflux pumps. Pyp reduced the final MIC endpoint

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Kim, Nayeong, Joo-Hee Son, Kyeongmin Kim, Hyo-Jeong Kim, Minsang Shin, and Je-Chul Lee. "DksA Modulates Antimicrobial Susceptibility of Acinetobacter baumannii." Antibiotics 10, no. 12 (2021): 1472. http://dx.doi.org/10.3390/antibiotics10121472.

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The stringent response regulators, (p)ppGpp and DksA, modulate various genes involved in physiological processes, virulence, and antimicrobial resistance in pathogenic bacteria. This study investigated the role of DksA in the antimicrobial susceptibility of Acinetobacter baumannii. The ∆dksA mutant (KM0248D) of A. baumannii ATCC 17978 and its complemented strain (KM0248C) were used, in addition to the ∆dksA mutant strain (NY0298D) of clinical 1656-2 strain. The microdilution assay was used to determine the minimum inhibitory concentrations (MICs) of antimicrobial agents. Quantitative real-time

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Leus, Inga V., Jon W. Weeks, Vincent Bonifay, Lauren Smith, Sophie Richardson, and Helen I. Zgurskaya. "Substrate Specificities and Efflux Efficiencies of RND Efflux Pumps ofAcinetobacter baumannii." Journal of Bacteriology 200, no. 13 (2018): e00049-18. http://dx.doi.org/10.1128/jb.00049-18.

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ABSTRACTAntibiotic-resistantAcinetobacter baumanniicauses infections that are extremely difficult to treat. A significant role in these resistance profiles is attributed to multidrug efflux pumps, especially those belonging to the resistance-nodulation-cell division (RND) superfamily of transporters. In this study, we analyzed functions and properties of RND efflux pumps inA. baumanniiATCC 17978. This strain is susceptible to antibiotics and does not contain mutations that are commonly selected upon exposure to high concentrations of antibiotics. We constructed derivatives of ATCC 17978 lackin

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Tegos, George P., Kayo Masago, Fatima Aziz, Andrew Higginbotham, Frank R. Stermitz, and Michael R. Hamblin. "Inhibitors of Bacterial Multidrug Efflux Pumps Potentiate Antimicrobial Photoinactivation." Antimicrobial Agents and Chemotherapy 52, no. 9 (2008): 3202–9. http://dx.doi.org/10.1128/aac.00006-08.

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ABSTRACT Antimicrobial photodynamic inactivation (APDI) combines a nontoxic photoactivatable dye or photosensitizer (PS) with harmless visible light to generate singlet oxygen and reactive oxygen species that kill microbial cells. Cationic phenothiazinium dyes, such as toluidine blue O (TBO), are the only PS used clinically for APDI, and we recently reported that this class of PS are substrates of multidrug efflux pumps in both gram-positive and gram-negative bacteria. We now report that APDI can be significantly potentiated by combining the PS with an efflux pump inhibitor (EPI). Killing of S

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Davin-Regli, Anne, Jean-Marie Pages, and Aurélie Ferrand. "Clinical Status of Efflux Resistance Mechanisms in Gram-Negative Bacteria." Antibiotics 10, no. 9 (2021): 1117. http://dx.doi.org/10.3390/antibiotics10091117.

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Antibiotic efflux is a mechanism that is well-documented in the phenotype of multidrug resistance in bacteria. Efflux is considered as an early facilitating mechanism in the bacterial adaptation face to the concentration of antibiotics at the infectious site, which is involved in the acquirement of complementary efficient mechanisms, such as enzymatic resistance or target mutation. Various efflux pumps have been described in the Gram-negative bacteria most often encountered in infectious diseases and, in healthcare-associated infections. Some are more often involved than others and expel virtu

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Sudano Roccaro, Andrea, Anna Rita Blanco, Francesco Giuliano, Dario Rusciano, and Vincenzo Enea. "Epigallocatechin-Gallate Enhances the Activity of Tetracycline in Staphylococci by Inhibiting Its Efflux from Bacterial Cells." Antimicrobial Agents and Chemotherapy 48, no. 6 (2004): 1968–73. http://dx.doi.org/10.1128/aac.48.6.1968-1973.2004.

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ABSTRACT Epigallocatechin-gallate (EGCg), the major catechin present in green tea extracts, has been shown to have several antibacterial activities, limiting bacterial growth and invasion and acting in synergy with β-lactam antibiotics. In this article, we report that EGCg at doses half and below its calculated MIC of 100 μg/ml, is able to reverse tetracycline resistance in staphylococcal isolates expressing the specific efflux pump Tet(K) and appears to improve the MICs of tetracycline for susceptible staphylococcal isolates as well. The visible effect of EGCg is an increased accumulation of

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Ashu, Fred A., Jean Na-Iya, Brice E. N. Wamba, et al. "Antistaphylococcal Activity of Extracts, Fractions, and Compounds of Acacia polyacantha Wild (Fabaceae)." Evidence-Based Complementary and Alternative Medicine 2020 (March 16, 2020): 1–10. http://dx.doi.org/10.1155/2020/2654247.

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Acacia polyacantha is a medicinal plant traditionally used to treat livestock diseases and gastrointestinal infections; our study was undertaken to evaluate the antistaphylococcal activities of the methanolic leaf, bark, and root extracts, fractions, and compounds from Acacia polyacantha against a panel of 14 multidrug-resistant Staphylococcus bacterial strains overexpressing efflux pumps. The study was also extended to investigate two possible modes of action, that is, influence on bacterial growth kinetics and influence on proton-ATPase pumps, of the most active compound against a reference

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Ravirala, Ramani S., Ravi D. Barabote, David M. Wheeler, et al. "Efflux Pump Gene Expression in Erwinia chrysanthemi Is Induced by Exposure to Phenolic Acids." Molecular Plant-Microbe Interactions® 20, no. 3 (2007): 313–20. http://dx.doi.org/10.1094/mpmi-20-3-0313.

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Salicylic acid (SA) is an important signaling molecule in local and systemic plant resistance. Following infection by microbial pathogens and the initial oxidative burst in plants, SA accumulation functions in the amplification of defense gene expression. Production of pathogenesis-related proteins and toxic antimicrobial chemicals serves to protect the plant from infection. Successful microbial pathogens utilize a variety of mechanisms to rid themselves of toxic antimicrobial compounds. Important among these mechanisms are multidrug-resistance pumps that bring about the active efflux of toxic

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Mazando, S., C. Zimudzi, M. Zimba, et al. "High efflux pump activity and gene expression at baseline linked to poor tuberculosis treatment outcomes." Journal of Medical and Biomedical Sciences 6, no. 1 (2017): 8–17. http://dx.doi.org/10.4314/jmbs.v6i1.2.

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Phenotypic TB drug resistance, also known as drug tolerance, has been previously attributed to slowed bacterial growth in vivo. The increased activity and expression of efflux systems can lower the intracellular concentration of many antibiotics thus reducing their efficacy. We hypothesized that efflux pump activation and expression could be a risk factor for TB drug tolerance in patients initiated on treatment. Analyses of gene expression levels of six select efflux pumps associated with drug tolerance in Mycobacterium tuberculosis and its correlation with the cell’s ability to efflux ethidiu

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Ding, Yanpeng, Yoshikuni Onodera, Jean C. Lee, and David C. Hooper. "NorB, an Efflux Pump in Staphylococcus aureus Strain MW2, Contributes to Bacterial Fitness in Abscesses." Journal of Bacteriology 190, no. 21 (2008): 7123–29. http://dx.doi.org/10.1128/jb.00655-08.

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ABSTRACT While remaining a major problem in hospitals, Staphylococcus aureus is now spreading in communities. Strain MW2 (USA400 lineage) and other community methicillin-resistant S. aureus strains most commonly cause skin infections with abscess formation. Multidrug resistance (MDR) efflux pumps contribute to antimicrobial resistance but may also contribute to bacterial survival by removal of environmental toxins. In S. aureus, NorA, NorB, NorC, and Tet38 are chromosomally encoded efflux pumps whose overexpression can confer MDR to quinolones and other compounds (Nor pumps) or tetracyclines a

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Neuberger, Arthur, Dijun Du, and Ben F. Luisi. "Structure and mechanism of bacterial tripartite efflux pumps." Research in Microbiology 169, no. 7-8 (2018): 401–13. http://dx.doi.org/10.1016/j.resmic.2018.05.003.

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Alav, Ilyas, J. Mark Sutton, and Khondaker Miraz Rahman. "Role of bacterial efflux pumps in biofilm formation." Journal of Antimicrobial Chemotherapy 73, no. 8 (2018): 2003–20. http://dx.doi.org/10.1093/jac/dky042.

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Lu, Wen-Jung, Yan-Jyun Huang, Hsuan-Ju Lin, et al. "Phenolic Compound Ethyl 3,4-Dihydroxybenzoate Retards Drug Efflux and Potentiates Antibiotic Activity." Antibiotics 11, no. 4 (2022): 497. http://dx.doi.org/10.3390/antibiotics11040497.

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The World Health Organization indicated that antibiotic resistance is one of the greatest threats to health, food security, and development in the world. Drug resistance efflux pumps are essential for antibiotic resistance in bacteria. Here, we evaluated the plant phenolic compound ethyl 3,4-dihydroxybenzoate (EDHB) for its efflux pump inhibitory (EPI) activity against drug-resistant Escherichia coli. The half-maximal inhibitory concentration, modulation assays, and time-kill studies indicated that EDHB has limited antibacterial activity but can potentiate the activity of antibiotics for drug-

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Ivanov, Mikhail Eduardovich, N. K. Fursova, and V. D. Potapov. "Pseudomonas aeruginosa efflux pump superfamily (review of literature)." Russian Clinical Laboratory Diagnostics 67, no. 1 (2022): 53–58. http://dx.doi.org/10.51620/0869-2084-2022-67-1-53-58.

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The significant increase in the number of antibiotic-resistant microorganisms observed in recent years is a public health problem worldwide. One of the molecular mechanisms for the formation of antimicrobial resistance in bacteria is the presence of efflux pumps. The review presents an analysis of experimental studies related to the study of efflux pumps in clinical strains of Pseudomonas aeruginosa, one of the representatives of hospital pathogens of the ESKAPE group. This review is intended for specialists developing new types of drugs against antibiotic-resistant strains, as well as researc

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Parker, Ashley, and Susan Gottesman. "Small RNA Regulation of TolC, the Outer Membrane Component of Bacterial Multidrug Transporters." Journal of Bacteriology 198, no. 7 (2016): 1101–13. http://dx.doi.org/10.1128/jb.00971-15.

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ABSTRACTBacteria use multidrug efflux pumps to export drugs and toxic compounds out of the cell. One of the most important efflux pumps inEscherichia coliis the AcrAB-TolC system. Small regulatory RNAs (sRNAs) are known to be major posttranscriptional regulators that can enhance or repress translation by binding to the 5′ untranslated region (UTR) of mRNA targets with the help of a chaperone protein, Hfq. In this study, we investigated the expression ofacrA,acrB, andtolCtranslational fusions using 27 Hfq-dependent sRNAs overexpressed from plasmids. No significant sRNA regulation ofacrAoracrBwa

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Rajapaksha, Prasangi, Isoiza Ojo, Ling Yang, Ankit Pandeya, Thilini Abeywansha, and Yinan Wei. "Insight into the AcrAB-TolC Complex Assembly Process Learned from Competition Studies." Antibiotics 10, no. 7 (2021): 830. http://dx.doi.org/10.3390/antibiotics10070830.

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The RND family efflux pump AcrAB-TolC in E. coli and its homologs in other Gram-negative bacteria are major players in conferring multidrug resistance to the cells. While the structure of the pump complex has been elucidated with ever-increasing resolution through crystallography and Cryo-EM efforts, the dynamic assembly process remains poorly understood. Here, we tested the effect of overexpressing functionally defective pump components in wild type E. coli cells to probe the pump assembly process. Incorporation of a defective component is expected to reduce the efflux efficiency of the compl

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Symmons, Martyn F., Evert Bokma, Eva Koronakis, Colin Hughes, and Vassilis Koronakis. "The assembled structure of a complete tripartite bacterial multidrug efflux pump." Proceedings of the National Academy of Sciences 106, no. 17 (2009): 7173–78. http://dx.doi.org/10.1073/pnas.0900693106.

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Bacteria likeEscherichia coliandPseudomonas aeruginosaexpel drugs via tripartite multidrug efflux pumps spanning both inner and outer membranes and the intervening periplasm. In these pumps a periplasmic adaptor protein connects a substrate-binding inner membrane transporter to an outer membrane-anchored TolC-type exit duct. High-resolution structures of all 3 components are available, but a pump model has been precluded by the incomplete adaptor structure, because of the apparent disorder of its N and C termini. We reveal that the adaptor termini assemble a β-roll structure forming the final

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Machado, Diana, Laura Fernandes, Sofia S. Costa, et al. "Mode of action of the 2-phenylquinoline efflux inhibitor PQQ4R againstEscherichia coli." PeerJ 5 (April 26, 2017): e3168. http://dx.doi.org/10.7717/peerj.3168.

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Efflux pump inhibitors are of great interest since their use as adjuvants of bacterial chemotherapy can increase the intracellular concentrations of the antibiotics and assist in the battle against the rising of antibiotic-resistant bacteria. In this work, we have described the mode of action of the 2-phenylquinoline efflux inhibitor (4-(2-(piperazin-1-yl)ethoxy)-2-(4-propoxyphenyl) quinolone – PQQ4R), againstEscherichia coli,by studding its efflux inhibitory ability, its synergistic activity in combination with antibiotics, and compared its effects with the inhibitors phenyl-arginine-β-naphth

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Du, Dijun, Hendrik W. van Veen, and Ben F. Luisi. "Assembly and operation of bacterial tripartite multidrug efflux pumps." Trends in Microbiology 23, no. 5 (2015): 311–19. http://dx.doi.org/10.1016/j.tim.2015.01.010.

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Webber, M. A. "The importance of efflux pumps in bacterial antibiotic resistance." Journal of Antimicrobial Chemotherapy 51, no. 1 (2002): 9–11. http://dx.doi.org/10.1093/jac/dkg050.

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Wiggins, Phillip. "Efflux pumps: an answer to Gram-negative bacterial resistance?" Expert Opinion on Investigational Drugs 13, no. 8 (2004): 899–902. http://dx.doi.org/10.1517/13543784.13.8.899.

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