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efflux pump inhibition

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https://www.readbyqxmd.com/read/28935182/eudesmane-sesquiterpenes-from-chinese-liverwort-are-substrates-of-cdrs-and-display-antifungal-activity-by-targeting-erg6-and-erg11-of-candida-albicans
#1
Siwen Li, Hongzhuo Shi, Wenqiang Chang, Yi Li, Ming Zhang, Yanan Qiao, Hongxiang Lou
We isolated twelve sesquiterpenes from Chinese liverwort Tritomaria quinquedentata (Huds.) Buch., including four new compounds. Among them, five eudesmane sesquiterpenes were ineffective against Candida albicans wild strain SC5314 but active towards efflux pumps-deficient strain DSY654 using Alamar blue assay. Further test of the most active agent of ent-isoalantolactone (8, ent-iLL) showed that it also inhibited the yeast-to-hyphal switch of DSY654 cells. The intracellular content measurement using high performance liquid chromatography (HPLC) revealed that ent-iLL was intracellularly accumulated in C...
September 9, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28915956/dual-inhibition-of-p-glycoprotein-and-midkine-may-increase-therapeutic-effects-of-anticancer-drugs
#2
A Şükrü Aynacıoğlu, Ayhan Bilir, Kenji Kadomatsu
Multidrug resistance (MDR) to chemotherapy may significantly affect the outcome of cancer treatment. ATP-dependent drug efflux pumps, including P-glycoprotein (P-gp), contribute to the resistance of various chemotherapeutic agents. Overexpression of P-gp in tumor cells induces chemoresistance via pumping the anticancer drugs out of the cells. In addition to taking part in many biological processes such as development, reproduction and repair, midkine (MK) also plays important roles in the pathogenesis of malignant diseases as well as in the regulation of MDR...
September 2017: Medical Hypotheses
https://www.readbyqxmd.com/read/28912036/dual-effects-of-the-pi3k-inhibitor-zstk474-on-multidrug-efflux-pumps-in-resistant-cancer-cells
#3
Divya Muthiah, Richard Callaghan
ZSTK474 is a potent phosphoinositide 3-kinase (PI3K) inhibitor that reduces cell proliferation via G1-arrest. However, there is little information on the susceptibility of this anticancer drug to resistance conferred by the multidrug pumps P-glycoprotein (ABCB1) and ABCG2. We have demonstrated that ZSTK474 generated cytotoxicity in cells over-expressing either pump with potency similar to that in drug sensitive cells. In addition, the co-administration of ZSTK474 with the cytotoxic anti-cancer drugs vinblastine and mitoxantrone caused a potentiated cytotoxic effect in both drug sensitive and efflux pump expressing cells...
September 11, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28900249/effect-of-efflux-pump-inhibition-on-pseudomonas-aeruginosa-transcriptome-and-virulence
#4
Giordano Rampioni, Cejoice Ramachandran Pillai, Francesca Longo, Roslen Bondì, Valerio Baldelli, Marco Messina, Francesco Imperi, Paolo Visca, Livia Leoni
Efflux pumps of the resistance-nodulation-cell-division (RND) family increase antibiotic resistance in many bacterial pathogens, representing candidate targets for the development of antibiotic adjuvants. RND pumps have also been proposed to contribute to bacterial infection, implying that efflux pump inhibitors (EPIs) could also act as anti-virulence drugs. Nevertheless, EPIs are usually investigated only for their properties as antibiotic adjuvants, while their potential anti-virulence activity is seldom taken into account...
September 12, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28899514/citral-a-monoterpenoid-aldehyde-interacts-synergistically-with-norfloxacin-against-methicillin-resistant-staphylococcus-aureus
#5
Priyanka Gupta, Dinesh Kumar Patel, Vivek Kumar Gupta, Anirban Pal, Sudeep Tandon, M P Darokar
BACKGROUND: Staphylococcus aureus (SA), is a major human pathogen causing wide range of clinical infections, which has been further complicated by drug resistance like methicillin resistant S. aureus (MRSA), vancomycin intermediate S. aureus (VISA)/vancomycin resistant S. aureus (VRSA), etc. The present study was aimed at determining anti-staphylococcal potential of citral against drug resistant clinical isolates alone and in combination with antibiotics. PURPOSE: To assess the potential of citral in combination with norfloxacin in treating drug resistant infections of SA...
October 15, 2017: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/28893785/in-vitro-activity-of-the-novel-pleuromutilin-lefamulin-bc-3781-and-effect-of-efflux-pump-inactivation-on-multidrug-resistant-and-extensively-drug-resistant-neisseria-gonorrhoeae
#6
Susanne Jacobsson, Susanne Paukner, Daniel Golparian, Jörgen S Jensen, Magnus Unemo
We evaluated the activity of the novel semi-synthetic pleuromutilin lefamulin, inhibiting protein synthesis and growth, and effect of efflux pump inactivation on clinical gonococcal isolates and reference strains (n=251), including numerous multidrug-resistant and extensively-drug resistant isolates. Lefamulin showed potent activity against all gonococcal isolates and no significant cross-resistance to other antimicrobials was identified. Further studies of lefamulin are warranted, including in-vitro selection and mechanisms of resistance, pharmacokinetics/pharmacodynamics, optimal dosing, and performance in randomized controlled trials...
September 11, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28890187/kinetic-analysis-of-the-inhibition-of-the-drug-efflux-protein-acrb-using-surface-plasmon-resonance
#7
Rumana Mowla, Yinhu Wang, Shutao Ma, Henrietta Venter
Multidrug efflux protein complexes such as AcrAB-TolC from Escherichia coli are paramount in multidrug resistance in Gram-negative bacteria and are also implicated in other processes such as virulence and biofilm formation. Hence efflux pump inhibition, as a means to reverse antimicrobial resistance in clinically relevant pathogens, has gained increased momentum over the past two decades. Significant advances in the structural and functional analysis of AcrB have informed the selection of efflux pump inhibitors (EPIs)...
September 7, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28887666/the-potential-of-multi-compound-nanoparticles-to-bypass-drug-resistance-in-cancer
#8
REVIEW
C G Da Silva, Godefridus J Peters, Ferry Ossendorp, Luis J Cruz
PURPOSE: The therapeutic efficacy of conventional chemotherapy against several solid tumors is generally limited and this is often due to the development of resistance or poor delivery of the drugs to the tumor. Mechanisms of resistance may vary between cancer types. However, with current development of genetic analyses, imaging, and novel delivery systems, we may be able to characterize and bypass resistance, e.g., by inhibition of the right target at the tumor site. Therefore, combined drug treatments, where one drug will revert or obstruct the development of resistance and the other will concurrently kill the cancer cell, are rational solutions...
September 8, 2017: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/28882485/zinc-chloride-rapidly-stimulates-efflux-transporters-in-renal-proximal-tubules-of-killifish-fundulus-heteroclitus
#9
Alexander Zaremba, David S Miller, Gert Fricker
Multidrug resistance-related protein 2 (Mrp2) is an ATP-driven efflux pump at the luminal membrane in renal proximal tubules. It acts as detoxification mechanism by transporting xenobiotics and metabolic products into urine. The trace element zinc is essential for cellular growth, differentiation and survival. It modulates immune response and is used as dietary supplement. Here, we found that 0.1-10μM ZnCl2 rapidly stimulated transport of the Mrp2 probe substrate Texas Red (TR) in isolated killifish renal proximal tubules, which provide an established model system to measure efflux transporter activity by using fluorescent probe substrates, confocal microscopy and image analysis...
September 4, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28874476/mechanisms-of-resistance-to-folate-pathway-inhibitors-in-burkholderia-pseudomallei-deviation-from-the-norm
#10
Nicole L Podnecky, Katherine A Rhodes, Takehiko Mima, Heather R Drew, Sunisa Chirakul, Vanaporn Wuthiekanun, James M Schupp, Derek S Sarovich, Bart J Currie, Paul Keim, Herbert P Schweizer
The trimethoprim and sulfamethoxazole combination, co-trimoxazole, plays a vital role in the treatment of Burkholderia pseudomallei infections. Previous studies demonstrated that the B. pseudomallei BpeEF-OprC efflux pump confers widespread trimethoprim resistance in clinical and environmental isolates, but this is not accompanied by significant resistance to co-trimoxazole. Using the excluded select-agent strain B. pseudomallei Bp82, we now show that in vitro acquired trimethoprim versus co-trimoxazole resistance is mainly mediated by constitutive BpeEF-OprC expression due to bpeT mutations or by BpeEF-OprC overexpression due to bpeS mutations...
September 5, 2017: MBio
https://www.readbyqxmd.com/read/28874380/the-global-regulatory-protein-crp-controls-multifactorial-fluoroquinolone-susceptibility-in-salmonella-enterica-serovar-typhimurium
#11
Stefani C Kary, Joshua R K Yoneda, Stephen C Olshefsky, Laura A Stewart, Steven B West, Andrew D S Cameron
Fluoroquinolone antibiotics are prescribed for the treatment of Salmonella enterica infections, but resistance to this family of antibiotics is growing. Here we report that loss of the global regulatory protein, CRP, or its allosteric effector, cAMP, reduces susceptibility to fluoroquinolones. A Δcrp mutation was synergistic with the primary fluoroquinolone resistance allele gyrA83, thus can contribute to clinically-relevant resistance. Decreased susceptibility to fluoroquinolones could be partly explained by decreased expression of the outer membrane porin genes ompA and ompF with a concomitant increase in the expression of the ciprofloxacin-resistance efflux pump gene acrB in Δcrp cells...
September 5, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28841421/tannic-acid-affects-the-phenotype-of-staphylococcus-aureus-resistant-to-tetracycline-and-erythromycin-by-inhibition-of-efflux-pumps
#12
Saulo R Tintino, Cícera D Morais-Tintino, Fábia F Campina, Maria do S Costa, Irwin R A Menezes, Yedda Maria L S de Matos, João T Calixto-Júnior, Pedro S Pereira, José P Siqueira-Junior, Teresa C Leal-Balbino, Henrique D M Coutinho, Valdir Q Balbino
The widespread use of antibiotics created selective pressure for the emergence of strains that would persist despite antibiotic toxicity. The bacterial resistance mechanisms are several, with efflux pumps being one of the main ones. These pumps are membrane proteins with the function of removing antibiotics from the cell cytoplasm. Due to this importance, the aim of this work was to evaluate the inhibitory effect of tannic acid against efflux pumps expressed by the Staphylococcus aureus RN4220 and IS-58 strains...
August 12, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28841301/cytotoxicity-and-efflux-pump-inhibition-induced-by-molybdenum-disulfide-and-boron-nitride-nanomaterials-with-sheetlike-structure
#13
Su Liu, Zhuoyan Shen, Bing Wu, Yue Yu, Hui Hou, Xu-Xiang Zhang, Hong-Qiang Ren
Sheetlike molybdenum disulfide (MoS2) and boron nitride (BN) nanomaterials have attracted attention in the past few years due to their unique material properties. However, information on adverse effects and their underlying mechanisms for sheetlike MoS2 and BN nanomaterials is rare. In this study, cytotoxicities of sheetlike MoS2 and BN nanomaterials on human hepatoma HepG2 cells were systematically investigated at different toxic end points. Results showed that MoS2 and BN nanomaterials decreased cell viability at 30 μg/mL and induced adverse effects on intracellular ROS generation (≥2 μg/mL), mitochondrial depolarization (≥4 μg/mL), and membrane integrity (≥8 μg/mL for MoS2 and ≥2 μg/mL for BN)...
September 6, 2017: Environmental Science & Technology
https://www.readbyqxmd.com/read/28821631/6-methoxyethylamino-numonafide-inhibits-hepatocellular-carcinoma-xenograft-growth-as-a-single-agent-and-in-combination-with-sorafenib
#14
Yanning Liu, Guohua Lou, John T Norton, Chen Wang, Irawati Kandela, Shuai Tang, Nathaniel I Shank, Pankaj Gupta, Min Huang, Michael J Avram, Richard Green, Andrew Mazar, Daniel Appella, Zhi Chen, Sui Huang
Hepatocellular carcinoma (HCC) is the third leading form of cancer worldwide, and its incidence is increasing rapidly in the United States, tripling over the past 3 decades. The current chemotherapeutic strategies against localized and metastatic HCC are ineffective. Here we report that 6-methoxyethylamino-numonafide (MEAN) is a potent growth inhibitor of murine xenografts of 2 human HCC cell lines. At the same dose and with the same treatment strategies, MEAN was more efficacious in inhibiting tumor growth in mice than sorafenib, the only approved drug for HCC...
August 17, 2017: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/28818459/a-novel-delocalized-lipophilic-cation-chlorambucil-conjugate-inhibits-p-glycoprotein-in-hepg2-adm-cells
#15
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
#16
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
#17
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
#18
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
#19
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 neighboring host cells to damaging ROS...
August 17, 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
#20
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
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