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https://www.readbyqxmd.com/read/28542844/the-inward-rectifier-current-inhibitor-pa-6-terminates-atrial-fibrillation-and-does-not-cause-ventricular-arrhythmias-in-dedicated-goat-and-dog-models
#1
Yuan Ji, Rosanne Varkevisser, Dragan Opacic, Alexandre Bossu, Marion Kuiper, Jet D M Beekman, Sihyung Yang, Azinwi Phina Khan, Dobromir Dobrev, Niels Voigt, Michael Zhuo Wang, Sander Verheule, Marc A Vos, Marcel A G Van der Heyden
BACKGROUND AND PURPOSE: Inward rectifier current (IK1 ) density increases in atrial fibrillation (AF), shortening effective refractory period and thus promotes atrial reentry. Pentamidine-Analogue 6 (PA-6) is a selective and potent IK1 inhibitor. We tested PA-6 for anti-AF efficacy and potential proarrhythmia, in established large animal models. EXPERIMENTAL APPROACH: PA-6 was applied i.v. in anaesthetized goats with rapid pacing induced AF and anaesthetized chronic AV block dogs...
May 24, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28506844/proarrhythmic-risk-assessment-using-conventional-and-new-in%C3%A2-vitro-assays
#2
Sonia Goineau, Vincent Castagné
Drug-induced QT prolongation is a major safety issue in the drug discovery process. This study was conducted to assess the electrophysiological responses of four substances using established preclinical assays usually used in regulatory studies (hERG channel or Purkinje fiber action potential) and a new assay (human-induced pluripotent stem cell-derived cardiomyocytes (hiPSC-CMs)-field potential). After acute exposure, moxifloxacin and dofetilide concentration-dependently decreased IKr amplitude (IC50 values: 102 μM and 40 nM, respectively) and lengthened action potential (100 μM moxifloxacin: +23% and 10 nM dofetilide: +18%) and field potential (300 μM moxifloxacin: +76% and 10 nM dofetilide: +38%) durations...
May 12, 2017: Regulatory Toxicology and Pharmacology: RTP
https://www.readbyqxmd.com/read/28470665/pentamidine-blocks-hepatotoxic-injury-in-mice
#3
Enpeng Zhao, Ghulam Ilyas, Francesca Cingolani, Jae Ho Choi, François Ravenelle, Kathryn E Tanaka, Mark J Czaja
Toxin-induced liver diseases lack effective therapies despite increased understanding of the role factors such as an overactive innate immune response play in the pathogenesis of this form of hepatic injury. Pentamidine is an effective antimicrobial agent against several human pathogens, but studies have also suggested that this drug inhibits inflammation. This potential anti-inflammatory mechanism of action, together with the development of a new oral form of pentamidine isethionate VLX103, led to investigations of the effectiveness of this drug in the prevention and treatment of hepatotoxic liver injury...
May 3, 2017: Hepatology: Official Journal of the American Association for the Study of Liver Diseases
https://www.readbyqxmd.com/read/28443518/limitations-of-current-therapeutic-options-possible-drug-targets-and-scope-of-natural-products-in-control-of-leishmaniasis
#4
Neeraj Tiwari, Mallikarjuna Rao Gedda, Vinod K Tiwari, Surya P Singh, Rakesh K Singh
Soon after the identification of Leishmania parasites,the pentavalent antimony compounds have been the mainstay to treat leishmanial infections, worldwide. These compounds were also considered true antileishmanial but the growing incidences of resistance have forced clinicians to use other options. However, due to unavailability of antileishmanial compounds, few drugs like pentamidine (antimicrobial), amphotericin B (antifungal) or miltefosine (antitumor) agents, which are associated with serious side effects, are currently being used...
April 24, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28437733/the-establishment-of-in%C3%A2-vitro-culture-and-drug-screening-systems-for-a-newly-isolated-strain-of-trypanosoma-equiperdum
#5
Keisuke Suganuma, Shino Yamasaki, Nthatisi Innocentia Molefe, Peter Simon Musinguzi, Batdorj Davaasuren, Ehab Mossaad, Sandagdorj Narantsatsral, Banzragch Battur, Badgar Battsetseg, Noboru Inoue
Dourine is caused by Trypanosoma equiperdum via coitus with an infected horse. Although dourine is distributed in Equidae worldwide and is listed as an internationally important animal disease by the World Organization for Animal Health (OIE), no effective treatment strategies have been established. In addition, there are no reports on drug discovery, because no drug screening system exists for this parasite. A new T. equiperdum strain was recently isolated from the genital organ of a stallion that showed typical symptoms of dourine...
April 13, 2017: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/28406408/leishmaniose-cutan%C3%A3-e-et-pentamidine
#6
P Bourée
No abstract text is available yet for this article.
February 1, 2017: Médecine et Santé Tropicales
https://www.readbyqxmd.com/read/28362799/organic-cation-transporter-1-oct1-is-involved-in-pentamidine-transport-at-the-human-and-mouse-blood-brain-barrier-bbb
#7
Gayathri N Sekhar, Ana R Georgian, Lisa Sanderson, Gema Vizcay-Barrena, Rachel C Brown, Paula Muresan, Roland A Fleck, Sarah A Thomas
Pentamidine is an effective trypanocidal drug used against stage 1 Human African Trypanosomiasis (HAT). At the blood-brain barrier (BBB), it accumulates inside the endothelial cells but has limited entry into the brain. This study examined transporters involved in pentamidine transport at the human and mouse BBB using hCMEC/D3 and bEnd.3 cell lines, respectively. Results revealed that both cell lines expressed the organic cation transporters (OCT1, OCT2 and OCT3), however, P-gp was only expressed in hCMEC/D3 cells...
2017: PloS One
https://www.readbyqxmd.com/read/28358927/aquaglyceroporin-null-trypanosomes-display-glycerol-transport-defects-and-respiratory-inhibitor-sensitivity
#8
Laura Jeacock, Nicola Baker, Natalie Wiedemar, Pascal Mäser, David Horn
Aquaglyceroporins (AQPs) transport water and glycerol and play important roles in drug-uptake in pathogenic trypanosomatids. For example, AQP2 in the human-infectious African trypanosome, Trypanosoma brucei gambiense, is responsible for melarsoprol and pentamidine-uptake, and melarsoprol treatment-failure has been found to be due to AQP2-defects in these parasites. To further probe the roles of these transporters, we assembled a T. b. brucei strain lacking all three AQP-genes. Triple-null aqp1-2-3 T. b. brucei displayed only a very moderate growth defect in vitro, established infections in mice and recovered effectively from hypotonic-shock...
March 2017: PLoS Pathogens
https://www.readbyqxmd.com/read/28327439/an-in-silico-functional-annotation-and-screening-of-potential-drug-targets-derived-from-leishmania-spp-hypothetical-proteins-identified-by-immunoproteomics
#9
Miguel A Chávez-Fumagalli, Mônica S Schneider, Daniela P Lage, Ricardo A Machado-de-Ávila, Eduardo A F Coelho
Leishmaniasis is a parasitic disease caused by the protozoan of the Leishmania genus. While no human vaccine is available, drugs such as pentavalent antimonials, pentamidine and amphotericin B are used for treat the patients. However, the high toxicity of these pharmaceutics, the emergence of parasite resistance and/or their high cost have showed to the urgent need of identify new targets to be employed in the improvement of the treatment against leishmaniasis. In a recent immunoproteomics approach performed in the Leishmania infantum species, 104 antigenic proteins were recognized by antibodies in sera of visceral leishmaniasis (VL) dogs...
May 2017: Experimental Parasitology
https://www.readbyqxmd.com/read/28280256/late-onset-cerebral-toxoplasmosis-after-allogeneic-hematopoietic-stem-cell-transplantation
#10
Ahmed M Khalaf, Mahmoud A Hashim, Mohammed Alsharabati, Kenneth Fallon, Joel K Cure, Peter Pappas, Shin Mineishi, Ayman Saad
BACKGROUND Toxoplasmosis is an uncommon but potentially fatal complication following allogeneic hematopoietic stem cell transplantation (HCT). Post-transplant toxoplasmosis is often a reactivation of prior infection and typically occurs within the first 6 months of transplant. Herein, we report that cerebral toxoplasmosis may occur 22 months after allogeneic hematopoietic stem cell transplantation. CASE REPORT We describe a case of cerebral toxoplasmosis that occurred 22 months after an allogeneic HCT while the patient was on aerosolized pentamidine for Pneumocystis jiroveci pneumonia (PCP) prophylaxis...
March 10, 2017: American Journal of Case Reports
https://www.readbyqxmd.com/read/28263303/pentamidine-sensitizes-gram-negative-pathogens-to-antibiotics-and-overcomes-acquired-colistin-resistance
#11
Jonathan M Stokes, Craig R MacNair, Bushra Ilyas, Shawn French, Jean-Philippe Côté, Catrien Bouwman, Maya A Farha, Arthur O Sieron, Chris Whitfield, Brian K Coombes, Eric D Brown
The increasing use of polymyxins(1) in addition to the dissemination of plasmid-borne colistin resistance threatens to cause a serious breach in our last line of defence against multidrug-resistant Gram-negative pathogens, and heralds the emergence of truly pan-resistant infections. Colistin resistance often arises through covalent modification of lipid A with cationic residues such as phosphoethanolamine-as is mediated by Mcr-1 (ref. 2)-which reduce the affinity of polymyxins for lipopolysaccharide(3). Thus, new strategies are needed to address the rapidly diminishing number of treatment options for Gram-negative infections(4)...
March 6, 2017: Nature Microbiology
https://www.readbyqxmd.com/read/28174101/evaluation-on-the-leishmanicidal-activity-of-2-n-n-dialkylamino-1-4-naphthoquinone-derivatives
#12
Morgana V de Araújo, Cibelle Cabral David, José Clementino Neto, Luiz A P L de Oliveira, Karoline Cristina Jatobá da Silva, Jefferson Miguel Dos Santos, João Kayke S da Silva, Victoria B C de A Brandão, Tania M S Silva, Celso A Camara, Magna S Alexandre-Moreira
Parasites of the Leishmania genus are the causative agents of leishmaniasis in humans, a disease that affects more than 12 million people worldwide. In this study was evaluated in vitro leishmanicidal activity of 2-N,N'-dialkylamino-1,4-naphthoquinone derivatives, covering a series of fourteen 2-N-morpholino-, 2-N-thiomorpholino, 2-N-piperidino, 2-N-(N(4)-methyl)-piperazino naphthoquinones (1a-n) derived from nor-lapachol and lawsone, belong to some other di-alkyaminoderivatives. At the cytotoxicity assay on peritoneal macrophages, the compounds possessing larger alkyl groups and N-methyl-piperazino moiety (1d, 1h, 1i and 1k), showed toxic effects similar to the standard drug used pentamidine...
May 2017: Experimental Parasitology
https://www.readbyqxmd.com/read/28167598/in-vitro-sensitivity-of-cutaneous-leishmania-promastigote-isolates-circulating-in-french-guiana-to-a-set-of-drugs
#13
Marine Ginouvès, Stéphane Simon, Mathieu Nacher, Magalie Demar, Bernard Carme, Pierre Couppié, Ghislaine Prévot
AbstractAnti-leishmaniasis drug resistance is a common problem worldwide. The aim of this study was to inventory the general in vitro level of sensitivity of Leishmania isolates circulating in French Guiana and to highlight potential in vitro pentamidine-resistant isolates. This sensitivity study was conducted on 36 patient-promastigote isolates for seven drugs (amphotericin B, azithromycin, fluconazole, meglumine antimoniate, miltefosine, paromomycin, and pentamidine) using the Cell Counting Kit-8 viability test...
May 2017: American Journal of Tropical Medicine and Hygiene
https://www.readbyqxmd.com/read/28087819/electrophysiologic-effects-of-the-ik1-inhibitor-pa-6-are-modulated-by-extracellular-potassium-in-isolated-guinea-pig-hearts
#14
Gregory S Hoeker, Mark A Skarsfeldt, Thomas Jespersen, Steven Poelzing
The pentamidine analog PA-6 was developed as a specific inward rectifier potassium current (IK1) antagonist, because established inhibitors either lack specificity or have side effects that prohibit their use in vivo. We previously demonstrated that BaCl2, an established IK1 inhibitor, could prolong action potential duration (APD) and increase cardiac conduction velocity (CV). However, few studies have addressed whether targeted IK1 inhibition similarly affects ventricular electrophysiology. The aim of this study was to determine the effects of PA-6 on cardiac repolarization and conduction in Langendorff-perfused guinea pig hearts...
January 2017: Physiological Reports
https://www.readbyqxmd.com/read/28074607/the-use-of-intravenous-pentamidine-for-the-prophylaxis-of-pneumocystis-pneumonia-in-pediatric-patients
#15
Matthijs D Kruizinga, Dorine Bresters, Frans J Smiers, Arjan C Lankester, Robbert G M Bredius
Pneumocystis jiroveci pneumonia was common in the immunocompromised host before the widespread use of prophylaxis. When trimethoprim-sulfamethoxazole is not tolerated, prophylaxis with intravenous pentamidine (IVP) may be initiated. We performed a retrospective analysis of all pediatric patients who received IVP regarding efficacy, safety, and reason for initiation. Of 106 patients included in our analysis, one patient tested positive for Pneumocystis DNA. Adverse events were reported in 18% of IVP courses, and main reason for initiation was cytopenia (59%)...
January 11, 2017: Pediatric Blood & Cancer
https://www.readbyqxmd.com/read/28012342/synthesis-and-molecular-modelling-studies-of-phenyl-linked-oxadiazole-phenylhydrazone-hybrids-as-potent-antileishmanial-agents
#16
Muhammad Taha, Nor Hadiani Ismail, Syahrul Imran, El Hassane Anouar, Manikandan Selvaraj, Waqas Jamil, Muhammad Ali, Syed Muhammad Kashif, Fazal Rahim, Khalid Mohammed Khan, Mohd Ilham Adenan
Molecular hybridization yielded phenyl linked oxadiazole-benzohydrazones hybrids 6-35 and were evaluated for their antileishmanial potentials. Compound 10, a 3,4-dihydroxy analog with IC50 value of 0.95 ± 0.01 μM, was found to be the most potent antileishmanial agent (7 times more active) than the standard drug pentamidine (IC50 = 7.02 ± 0.09 μM). The current series 6-35 conceded in the identification of thirteen (13) potent antileishmanial compounds with the IC50 values ranging between 0.95 ± 0...
January 27, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28009804/evaluation-of-chemical-composition-and-antileishmanial-and-antituberculosis-activities-of-essential-oils-of-piper-species
#17
Karine Zanoli Bernuci, Camila Cristina Iwanaga, Carla Maria Mariano Fernandez-Andrade, Fabiana Brusco Lorenzetti, Eduardo Caio Torres-Santos, Viviane Dos Santos Faiões, José Eduardo Gonçalves, Wanderlei do Amaral, Cícero Deschamps, Regiane Bertin de Lima Scodro, Rosilene Fressatti Cardoso, Vanessa Pietrowski Baldin, Diógenes Aparício Garcia Cortez
Essential oils from fresh Piperaceae leaves were obtained by hydrodistillation and analyzed by gas chromatography mass spectrometry (GC-MS), and a total of 68 components were identified. Principal components analysis results showed a chemical variability between species, with sesquiterpene compounds predominating in the majority of species analyzed. The composition of the essential oil of Piper mosenii was described for the first time. The cytotoxicity of the essential oils was evaluated in peritoneal macrophages and the oils of P...
December 12, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/27973453/evaluation-of-chemical-composition-and-antileishmanial-and-antituberculosis-activities-of-essential-oils-of-piper-species
#18
Karine Zanoli Bernuci, Camila Cristina Iwanaga, Carla Maria Mariano Fernadez-Andrade, Fabiana Brusco Lorenzetti, Eduardo Caio Torres-Santos, Viviane Dos Santos Faiões, José Eduardo Gonçalves, Wanderlei do Amaral, Cícero Deschamps, Regiane Bertin de Lima Scodro, Rosilene Fressatti Cardoso, Vanessa Pietrowski Baldin, Diógenes Aparício Garcia Cortez
Essential oils from fresh Piperaceae leaves were obtained by hydrodistillation and analyzed by gas chromatography mass spectrometry (GC-MS), and a total of 68 components were identified. Principal components analysis results showed a chemical variability between species, with sesquiterpene compounds predominating in the majority of species analyzed. The composition of the essential oil of Piper mosenii was described for the first time. The cytotoxicity of the essential oils was evaluated in peritoneal macrophages and the oils of P...
December 12, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/27939960/synthesis-and-in-vitro-anti-leishmanial-activity-of-4-arylpiperazin-1-yl-1-thiophen-2-yl-9h-pyrido-3-4-b-indol-3-yl-methanone-derivatives
#19
Penta Ashok, Subhash Chander, Larry M C Chow, Iris L K Wong, Rajnish Prakash Singh, Prabhat Nath Jha, Murugesan Sankaranarayanan
In the present study, we have reported synthesis and biological evaluation of a series of fifteen 1-(thiophen-2-yl)-9H-pyrido[3,4-b]indole derivatives against both promastigotes and amastigotes of Leishmania parasites responsible for visceral (L. donovani) and cutaneous (L. amazonensis) leishmaniasis. Among these reported analogues, compounds 7b, 7c, 7f, 7g, 7i, 7j, 7m, 7o displayed potent activity (15.55, 7.70, 7.00, 3.80, 14.10, 9.25, 3.10, 4.85μM, respectively) against L. donovani promastigotes than standard drugs miltefosine (15...
December 2, 2016: Bioorganic Chemistry
https://www.readbyqxmd.com/read/27876275/development-of-leishmania-donovani-stably-expressing-dsred-for-flow-cytometry-based-drug-screening-using-chalcone-thiazolyl-hydrazone-as-a-new-antileishmanial-target
#20
Anil Kumar Jaiswal, K Bhaskara Rao, Pragati Kushwaha, Keerti Rawat, Ram K Modukuri, Prashant Khare, Sumit Joshi, Shikha Mishra, Ambak Rai, Koneni V Sashidhara, Anuradha Dube
Green fluorescent protein produces significant fluorescence and is extremely stable, however its excitation maximum is close to the ultraviolet range and thus can damage living cells. Hence, Leishmania donovani stably expressing DsRed were developed and their suitability for flow cytometry-based antileishmanial screening was assessed by evaluating the efficacies of standard drugs as well as newly synthesised chalcone thiazolyl-hydrazone compounds. The DsRed gene was successfully integrated at the 18S rRNA locus of L...
December 2016: International Journal of Antimicrobial Agents
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