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efflux pump inhibition

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https://www.readbyqxmd.com/read/28818459/a-novel-delocalized-lipophilic-cation-chlorambucil-conjugate-inhibits-p-glycoprotein-in-hepg2-adm-cells
#1
Teng Liu, Yongbo Peng, Xiong Li, Lian Liu, Fang Liu, Leye He
Multidrug resistance (MDR) limits the application of a large number of cancer-fighting agents in clinical therapy. One reason is that P-glycoprotein (Pgp) efflux pumps are usually overexpressed and lead to drug efflux in the cancer cells, which limits the viability of many chemotherapeutics. Current available inhibitors which block the Pgp pump efflux are usually not widely used in clinical practice, because they change other drug pharmacokinetic profiles or increase side effects. Here, through covalent linkage of cancer-targeting delocalized lipophilic cation FF and DNA-damaging drug nitrogen mustard chlorambucil (CLB), we rationally designed and synthesized a tumor-targeting anticancer agent FFCLB...
August 4, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28816060/the-broad-spectrum-antimicrobial-potential-of-mn-co-4-s2cnme-ch2co2h-a-water-soluble-co-releasing-molecule-corm-401-intracellular-accumulation-transcriptomic-and-statistical-analyses-and-membrane-polarization
#2
Lauren Katie Wareham, Samantha McLean, Ronald Begg, Namrata Rana, Salar Ali, John J Kendall, Guido Sanguinetti, Brian E Mann, Robert K Poole
AIMS: Carbon monoxide (CO)-releasing molecules (CORMs) are candidates for animal and antimicrobial therapeutics. We aimed to probe the antimicrobial potential of a novel manganese CORM. RESULTS: [Mn(CO)4S2CNMe(CH2CO2H)], CORM-401, inhibits growth of Escherichia coli and several antibiotic-resistant clinical pathogens. CORM-401 releases CO that binds oxidases in vivo but is an ineffective respiratory inhibitor. Extensive CORM accumulation (assayed as intracellular manganese) accompanies antimicrobial activity...
August 17, 2017: Antioxidants & Redox Signaling
https://www.readbyqxmd.com/read/28814831/schiff-base-derived-from-thiosemicarbazone-and-anthracene-showed-high-potential-in-overcoming-multidrug-resistance-in-vitro-with-low-drug-resistance-index
#3
Jie Bai, Rui-Hui Wang, Yan Qiao, Aidong Wang, Chen-Jie Fang
Multidrug resistance (MDR) is a huge obstacle in cancer chemotherapeutics. Overcoming MDR is a great challenge for anticancer drug discovery. Here, DNA binding and cytotoxicity of Schiff base L1 and L2 were explored to assess their efficiency in fighting cancer and overcoming the MDR. L1 and L2 could treat extremely chemoresistant MCF-7/ADR cell as drug-sensitive cell, with drug resistance index (DRI) <2.13, showing high potential in overcoming the MDR. The apoptotic ratio induced by L1 and L2 was low for both MCF-7 and MCF-7/ADR cells...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28806947/conessine-as-a-novel-inhibitor-of-multidrug-efflux-pump-systems-in-pseudomonas-aeruginosa
#4
Thanyaluck Siriyong, Potjanee Srimanote, Sasitorn Chusri, Boon-Ek Yingyongnarongkul, Channarong Suaisom, Varomyalin Tipmanee, Supayang Piyawan Voravuthikunchai
BACKGROUND: Holarrhena antidysenterica has been employed as an ethnobotanical plant for the treatment of dysentery, diarrhoea, fever, and bacterial infections. Biological activities of the principle compound, conessine including anti-diarrhoea and anti-plasmodial effects were documented. Our previous study reported potency of Holarrhena antidysenterica extract and conessine as resistance modifying agents against extensively drug-resistant Acinetobacter baumannii. This study aimed to investigate (i) whether conessine, a steroidal alkaloid compound, could act as a resistance modifying agent against multidrug-resistant Pseudomonas aeruginosa, and (ii) whether MexAB-OprM efflux pump involved in the mechanism...
August 14, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28799332/attaching-the-nora-efflux-pump-inhibitor-inf55-to-methylene-blue-enhances-antimicrobial-photodynamic-inactivation-of-methicillin-resistant-staphylococcus-aureus-in-vitro-and-in-vivo
#5
Ardeshir Rineh, Naveen K Dolla, Anthony R Ball, Maria Magana, John B Bremner, Michael R Hamblin, George P Tegos, Michael J Kelso
Antimicrobial photodynamic inactivation (aPDI) uses photosensitizers (PSs) and harmless visible light to generate reactive oxygen species (ROS) and kill microbes. Multidrug efflux systems can moderate the phototoxic effects of PSs by expelling the compounds from cells. We hypothesized that increasing intracellular concentrations of PSs by inhibiting efflux with a covalently attached efflux pump inhibitor (EPI) would enhance bacterial cell phototoxicity and reduce exposure of neighbouring host cells to damaging ROS...
August 11, 2017: ACS Infectious Diseases
https://www.readbyqxmd.com/read/28782709/mic-distribution-among-wild-type-strains-of-legionella-pneumophila-identifies-a-subpopulation-with-reduced-susceptibility-to-macrolides-owing-to-efflux-pump-genes
#6
Marine Vandewalle-Capo, Clémence Massip, Ghislaine Descours, Joséphine Charavit, Joelle Chastang, Pierre Alain Billy, Sandrine Boisset, Gerard Lina, Christophe Gilbert, Max Maurin, Sophie Jarraud, Christophe Ginevra
Legionnaires' disease is a severe pneumonia mainly caused by Legionella pneumophila, and which is treated by antibiotics. The purpose of this study was to describe the susceptibility of clinical strains of Legionella pneumophila to seven antibiotics used for legionellosis treatment. The minimum inhibitory concentrations (MICs) of 109 well-characterized clinical strains of L. pneumophila serogroup-1 were determined using a broth microdilution method without charcoal and compared to antibiotic-resistant strains selected in vitro...
August 4, 2017: International Journal of Antimicrobial Agents
https://www.readbyqxmd.com/read/28779982/redox-sensitive-cationic-pullulan-for-efficient-gene-transfection-and-drug-retention-in-c6-glioma-cells
#7
Priya S S, Rekha M R
Thiolated cationic pullulan was synthesized by conjugating pullulan with polyethyleneimine (PEI) and mercaptosuccinic acid (MSA). The formed conjugate was oxidized to obtain disulfide linked cationic pullulan (PPMSS). PPMSS exhibited good buffering capacity and nanoplexes formulated were of size less than 150nm. Nanoplexes formed with PPMSS are redox sensitive and susceptible to reductive cleavage by dithiothreitol (DTT) ensuring the intracellular release of DNA. In vitro, cytotoxic evaluation studies of polymers in C6 cell lines established its non-toxic nature...
August 2, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28754701/genome-sequence-and-composition-of-a-tolyporphin-producing-cyanobacterium-microbial-community
#8
Rebecca-Ayme Hughes, Yunlong Zhang, Ran Zhang, Philip G Williams, Jonathan S Lindsey, Eric S Miller
The cyanobacterial culture HT-58-2 was originally described as a strain of Tolypothrix nodosa with the ability to produce tolyporphins, which comprise a family of distinct tetrapyrrole macrocycles with reported efflux pump inhibition properties. Upon reviving the culture from what was thought to be a non-extant collection, studies of culture conditions, strain characterization, phylogeny, and genomics have been undertaken. Herein, HT-58-2 was shown by 16S rRNA analysis to closely align with Brasilonema strains and not with Tolypothrix isolates...
July 28, 2017: Applied and Environmental Microbiology
https://www.readbyqxmd.com/read/28752532/rutin-a-quercetin-glycoside-restores-chemosensitivity-in-human-breast-cancer-cells
#9
Marcello Iriti, Robert Kubina, Andrea Cochis, Rita Sorrentino, Elena M Varoni, Agata Kabała-Dzik, Barbara Azzimonti, Arkadiusz Dziedzic, Lia Rimondini, Robert D Wojtyczka
Several studies have documented the ability of flavonoids to sensitize cancer cells to chemotherapeutics and reverse multidrug resistance by inhibition of efflux pumps (adenosine triphosphate-binding cassette transporters), apoptosis activation, and cell cycle arrest. In this study, the flavonoid rutin (quercetin 3-O-β-d-rutinoside) was investigated as chemosensitizer towards two different human epithelial breast cancer cell lines: (i) MB-MDA-231, selected as representative for triple-negative breast cancer and (ii) MCF-7 used as a well-characterized model of HER2-negative breast cancer...
July 28, 2017: Phytotherapy Research: PTR
https://www.readbyqxmd.com/read/28749666/substituted-n-phenyl-5-2-phenylamino-thiazol-4-yl-isoxazole-3-carboxamides-are-valuable-antitubercular-candidates-that-evade-innate-efflux-machinery
#10
Elisa Azzali, Diana Machado, Amit Kaushik, Federica Vacondio, Sara Flisi, Clotilde Silvia Cabassi, Gyanu Lamichhane, Miguel Viveiros, Gabriele Costantino, Marco Pieroni
Tuberculosis remains one of the deadliest infectious diseases in the world, and the increased number of multidrug-resistant and extremely drug-resistant strains is a significant reason for concern. This makes the discovery of novel antitubercular agents a cogent priority. We have previously addressed this need by reporting a series of substituted 2-aminothiazoles capable to inhibit the growth of actively replicating, nonreplicating persistent, and resistant Mycobacterium tuberculosis strains. Clues from the structure-activity relationships lining up the antitubercular activity were exploited for the rational design of improved analogues...
August 10, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28743651/resistance-to-quinolones-cephalosporins-and-macrolides-in-escherichia-coli-causing-bacteremia-in-peruvian-children
#11
Noemí Palma, Maria J Pons, Cláudia Gomes, Judit Mateu, Maribel Riveros, Wilfredo García, Jan Jacobs, Coralith García, Theresa J Ochoa, Joaquim Ruiz
OBJECTIVE: To characterize the β-lactam, quinolone and macrolide resistance levels and mechanisms in 62 Escherichia coli isolates causing children bacteremia. METHODS: Minimal inhibitory concentration of ciprofloxacin, nalidixic acid (NAL) and azithromycin was determined in presence and absence of Phe-Arg-β-Naphtylamyde. Additionally, the susceptibility levels to other 14 antimicrobial agents was established. Extended Spectrum β-lactamases (ESBLs) were identified, while mutations in gyrA and parC genes, presence of transferable mechanisms of quinolone-resistance (TMQR) and macrolide-resistance (TMMR) was also determined...
July 22, 2017: Journal of Global Antimicrobial Resistance
https://www.readbyqxmd.com/read/28739698/highly-eribulin-resistant-kbv20c-oral-cancer-cells-can-be-sensitized-by-co-treatment-with-the-third-generation-p-glycoprotein-inhibitor-elacridar-at-a-low-dose
#12
Yujin Park, Ji-Yeon Son, Byung-Mu Lee, Hyung Sik Kim, Sungpil Yoon
BACKGROUND/AIM: Eribulin mesylate, also called Halaven® (HAL), was recently developed as a microtubule-targeting drug and is used in the clinic for resistant or metastatic cancer. Previously, we showed that P-glycoprotein (P-gp)-overexpressing KBV20C oral cancer cells are highly resistant to HAL compared to sensitive KB cells. This qualitative study was designed to identify specific P-gp inhibitors that increase the sensitivity of highly resistant cancer cells to HAL. MATERIALS AND METHODS: In order to identify functional P-gp inhibitors, HAL-treated KBV20C cells were co-treated with P-gp inhibitors, verapamil, elacridar, cyclosporine A, mitotane, piperine, fumagillin, curcumin, indomethacin, probenecid, sulindac, tesmilifene, and C-4...
August 2017: Anticancer Research
https://www.readbyqxmd.com/read/28739514/inhibition-of-blood-brain-barrier-efflux-transporters-promotes-seizure-in-pregnant-rats-role-of-circulating-factors
#13
Abbie C Johnson, Erica S Hammer, Sophie Sakkaki, Sarah M Tremble, Gregory L Holmes, Marilyn J Cipolla
Seizure-provoking factors circulate late in gestation during normal pregnancy, but do not readily gain access to the brain due to the protective nature of the blood-brain barrier. In particular, efflux transporters are powerful ATP-driven pumps that actively prevent unwanted compounds from entering the brain. We hypothesized that acute inhibition of efflux transporters at the blood-brain barrier would result in spontaneous seizures in pregnant rats. We further hypothesized that the blood-brain barrier protects the maternal brain from seizure by increasing expression and/or activity of p-glycoprotein (P-gp), a major efflux transporter...
July 21, 2017: Brain, Behavior, and Immunity
https://www.readbyqxmd.com/read/28729070/abc-transporters-in-the-liver-fluke-opisthorchis-felineus
#14
Viatcheslav A Mordvinov, Nikita I Ershov, Darya S Pirozhkova, Yuri V Pakharukov, Maria Y Pakharukova
ATP-binding cassette transporters (ABC transporters) are essential components of normal cellular physiological machinery in all eukaryotic and prokaryotic species, including parasites. Some ABC transporters, e.g., P-glycoproteins, are involved in the efflux of toxins and xenobiotics from the cell. At present, nothing is known about ABC transporter genes in epidemiologically important liver flukes from the Opisthorchiidae family, including European liver fluke Opisthorchis felineus. Opisthorchiasis caused by O...
July 17, 2017: Molecular and Biochemical Parasitology
https://www.readbyqxmd.com/read/28720734/lack-of-acrb-efflux-function-confers-loss-of-virulence-on-salmonella-enterica-serovar-typhimurium
#15
Xuan Wang-Kan, Jessica M A Blair, Barbara Chirullo, Jonathan Betts, Roberto M La Ragione, Alasdair Ivens, Vito Ricci, Timothy J Opperman, Laura J V Piddock
AcrAB-TolC is the paradigm resistance-nodulation-division (RND) multidrug resistance efflux system in Gram-negative bacteria, with AcrB being the pump protein in this complex. We constructed a nonfunctional AcrB mutant by replacing D408, a highly conserved residue essential for proton translocation. Western blotting confirmed that the AcrB D408A mutant had the same native level of expression of AcrB as the parental strain. The mutant had no growth deficiencies in rich or minimal medium. However, compared with wild-type SL1344, the mutant had increased accumulation of Hoechst 33342 dye and decreased efflux of ethidium bromide and was multidrug hypersusceptible...
July 18, 2017: MBio
https://www.readbyqxmd.com/read/28715978/the-role-of-efflux-pumps-in-tuberculosis-treatment-and-their-promise-as-a-target-in-drug-development-unraveling-the-black-box
#16
Lindsey H M Te Brake, Gerjo J de Knegt, Jurriaan E de Steenwinkel, Teunis J P van Dam, David M Burger, Frans G M Russel, Reinout van Crevel, Jan B Koenderink, Rob E Aarnoutse
Insight into drug transport mechanisms is highly relevant to the efficacious treatment of tuberculosis (TB). Major problems in TB treatment are related to the transport of antituberculosis (anti-TB) drugs across human and mycobacterial membranes, affecting the concentrations of these drugs systemically and locally. Firstly, transporters located in the intestines, liver, and kidneys all determine the pharmacokinetics and pharmacodynamics of anti-TB drugs, with a high risk of drug-drug interactions in the setting of concurrent use of antimycobacterial, antiretroviral, and antidiabetic agents...
July 17, 2017: Annual Review of Pharmacology and Toxicology
https://www.readbyqxmd.com/read/28710521/efflux-drug-transporters-at-the-forefront-of-antimicrobial-resistance
#17
REVIEW
Tahmina Rahman, Benjamin Yarnall, Declan A Doyle
Bacterial antibiotic resistance is rapidly becoming a major world health consideration. To combat antibiotics, microorganisms employ their pre-existing defence mechanisms that existed long before man's discovery of antibiotics. Bacteria utilise levels of protection that range from gene upregulation, mutations, adaptive resistance, and production of resistant phenotypes (persisters) to communal behaviour, as in swarming and the ultimate defence of a biofilm. A major part of all of these responses involves the use of antibiotic efflux transporters...
July 14, 2017: European Biophysics Journal: EBJ
https://www.readbyqxmd.com/read/28709374/nanoparticles-as-efflux-pump-and-biofilm-inhibitor-to-rejuvenate-bactericidal-effect-of-conventional-antibiotics
#18
REVIEW
Divya Gupta, Ajeet Singh, Asad U Khan
The universal problem of bacterial resistance to antibiotic reflects a serious threat for physicians to control infections. Evolution in bacteria results in the development of various complex resistance mechanisms to neutralize the bactericidal effect of antibiotics, like drug amelioration, target modification, membrane permeability reduction, and drug extrusion through efflux pumps. Efflux pumps acquire a wide range of substrate specificity and also the tremendous efficacy for drug molecule extrusion outside bacterial cells...
December 2017: Nanoscale Research Letters
https://www.readbyqxmd.com/read/28700974/mechanism-of-berberine-mediated-fluconazole-susceptibility-enhancement-in-clinical-fluconazole-resistant-candida-tropicalis-isolates
#19
GaoXiang Shi, Jing Shao, TianMing Wang, DaQiang Wu, ChangZhong Wang
BACKGROUND: Candida tropicalis was one of the most common non-albicans Candida (NACA) species creating relatively high morbidity and mortality. We previously demonstrated that the antifungal effect of BBR in combination with FLC might be attributed to reactive oxygen species production, ergosterol content and efflux pump levels in a clinical C. tropicalis isolate. METHODS: we employed thirteen clinical C. tropicalis isolates as well as four standard reference strains to evaluate the antifungal activity of BBR in combination with FLC under planktonic and biofilm states by analyzing the mRNA expressions of ERG11, CDR1 and MDR1 by qRT-PCR...
September 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28700656/unexpected-effects-of-azole-transporter-inhibitors-on-antifungal-susceptibility-in-candida-glabrata-and-other-pathogenic-candida-species
#20
Yohsuke Nagayoshi, Taiga Miyazaki, Shintaro Shimamura, Hironobu Nakayama, Asuka Minematsu, Shunsuke Yamauchi, Takahiro Takazono, Shigeki Nakamura, Katsunori Yanagihara, Shigeru Kohno, Hiroshi Mukae, Koichi Izumikawa
The pathogenic fungus Candida glabrata is often resistant to azole antifungal agents. Drug efflux through azole transporters, such as Cdr1 and Cdr2, is a key mechanism of azole resistance and these genes are under the control of the transcription factor Pdr1. Recently, the monoamine oxidase A (MAO-A) inhibitor clorgyline was shown to inhibit the azole efflux pumps, leading to increased azole susceptibility in C. glabrata. In the present study, we have evaluated the effects of clorgyline on susceptibility of C...
2017: PloS One
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