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https://www.readbyqxmd.com/read/28087819/electrophysiologic-effects-of-the-ik1-inhibitor-pa-6-are-modulated-by-extracellular-potassium-in-isolated-guinea-pig-hearts
#1
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
#2
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
#3
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...
December 10, 2016: 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
#4
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
#5
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
#6
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
#7
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
https://www.readbyqxmd.com/read/27729250/pentamidine-antagonizes-the-benznidazole-s-effect-in%C3%A2-vitro-and-lacks-of-synergy-in%C3%A2-vivo-implications-about-the-polyamine-transport-as-an-anti-trypanosoma-cruzi-target
#8
Verónica Seguel, Lorena Castro, Chantal Reigada, Leonel Cortes, María V Díaz, Mariana R Miranda, Claudio A Pereira, Michel Lapier, Carolina Campos-Estrada, Antonio Morello, Ulrike Kemmerling, Juan D Maya, Rodrigo López-Muñoz
Benznidazole is the first-line drug used in treating Chagas disease, which is caused by the parasite Trypanosoma cruzi (T. cruzi). However, benznidazole has limited efficacy and several adverse reactions. Pentamidine is an antiprotozoal drug used in the treatment of leishmaniasis and African trypanosomiasis. In T. cruzi, pentamidine blocks the transport of putrescine, a precursor of trypanothione, which constitutes an essential molecule in the resistance of T. cruzi to benznidazole. In the present study, we describe the effect of the combination of benznidazole and pentamidine on isolated parasites, mammalian cells and in mice infected with T...
December 2016: Experimental Parasitology
https://www.readbyqxmd.com/read/27690007/stereoselective-blockage-of-quinidine-and-quinine-in-the-herg-channel-and-the-effect-of-their-rescue-potency-on-drug-induced-herg-trafficking-defect
#9
Meng Yan, Pan Fan, Yanhui Shi, Lifang Feng, Junnan Wang, Ge Zhan, Baoxin Li
Diastereoisomers of quinidine and quinine are used to treat arrhythmia and malaria, respectively. It has been reported that both drugs block the hERG (human ether-a-go-go-related gene) potassium channel which is essential for myocardium repolarization. Abnormality of repolarization increases risk of arrhythmia. The aim of our research is to study and compare the impacts of quinidine and quinine on hERG. Results show that both drugs block the hERG channel, with quinine 14-fold less potent than quinidine. In addition, they presented distinct impacts on channel dynamics...
2016: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/27600039/antileishmanial-mechanism-of-diamidines-involves-targeting-kinetoplasts
#10
Gyongseon Yang, Gahee Choi, Joo Hwan No
Leishmaniasis is a disease caused by pathogenic Leishmania parasites; current treatments are toxic and expensive, and drug resistance has emerged. While pentamidine, a diamidine-type compound, is one of the treatments, its antileishmanial mechanism of action has not been investigated in depth. Here we tested several diamidines, including pentamidine and its analog DB75, against Leishmania donovani and elucidated their antileishmanial mechanisms. We identified three promising new antileishmanial diamidine compounds with 50% effective concentrations (EC50s) of 3...
November 2016: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/27550992/ecil-guidelines-for-preventing-pneumocystis-jirovecii-pneumonia-in-patients-with-haematological-malignancies-and-stem-cell-transplant-recipients
#11
REVIEW
Johan Maertens, Simone Cesaro, Georg Maschmeyer, Hermann Einsele, J Peter Donnelly, Alexandre Alanio, Philippe M Hauser, Katrien Lagrou, Willem J G Melchers, Jannik Helweg-Larsen, Olga Matos, Stéphane Bretagne, Catherine Cordonnier
The 5th European Conference on Infections in Leukaemia (ECIL-5) meeting aimed to establish evidence-based recommendations for the prophylaxis of Pneumocystis jirovecii pneumonia (PCP) in non-HIV-infected patients with an underlying haematological condition, including allogeneic HSCT recipients. Recommendations were based on the grading system of the IDSA. Trimethoprim/sulfamethoxazole given 2-3 times weekly is the drug of choice for the primary prophylaxis of PCP in adults ( A-II: ) and children ( A-I: ) and should be given during the entire period at risk...
September 2016: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/27527618/synthesis-screening-and-in-silico-simulations-of-anti-parasitic-propamidine-benzimidazole-derivatives
#12
Carlos A Méndez-Cuesta, Miguel Ángel Herrera-Rueda, Sergio Hidalgo-Figueroa, Hugo Tlahuext, Rosa Moo-Puc, Juan Bautista Chale-Dzul, Manuel Chan-Bacab, Benjamín Otto Ortega-Morales, Emanuel Hernández-Núñez, Oscar Méndez-Lucio, José L Medina-Franco, Gabriel Navarrete-Vazquez
BACKGROUND: Propamidine, an antiseptic aromatic diamidine is a toxic compound with potential use as antiprotozoal drug. On the other hand, benzimidazole derivatives have shown excellent antiparasitic effects. We designed hybrid molecules between propamidine and benzimidazole in order to retain the antiprotozoal action, but decreasing the toxic effect of the molecule. Objetive: Design and prepare 12 hybrids from propamidine and benzimidazole for testing their antiparasitic effect over three protozoa: Giardia intestinalis, Trichomonas vaginalis and Leishmania Mexicana, as well as conduct several in silico simulations such as toxicological profile, molecular docking and molecular dynamics in order to understand their potential mode of action...
August 11, 2016: Medicinal Chemistry
https://www.readbyqxmd.com/read/27518185/reduced-mitochondrial-membrane-potential-is-a-late-adaptation-of-trypanosoma-brucei-brucei-to-isometamidium-preceded-by-mutations-in-the-%C3%AE-subunit-of-the-f1fo-atpase
#13
Anthonius A Eze, Matthew K Gould, Jane C Munday, Daniel N A Tagoe, Valters Stelmanis, Achim Schnaufer, Harry P De Koning
BACKGROUND: Isometamidium is the main prophylactic drug used to prevent the infection of livestock with trypanosomes that cause Animal African Trypanosomiasis. As well as the animal infective trypanosome species, livestock can also harbor the closely related human infective subspecies T. b. gambiense and T. b. rhodesiense. Resistance to isometamidium is a growing concern, as is cross-resistance to the diamidine drugs diminazene and pentamidine. METHODOLOGY/PRINCIPAL FINDINGS: Two isometamidium resistant Trypanosoma brucei clones were generated (ISMR1 and ISMR15), being 7270- and 16,000-fold resistant to isometamidium, respectively, which retained their ability to grow in vitro and establish an infection in mice...
August 2016: PLoS Neglected Tropical Diseases
https://www.readbyqxmd.com/read/27495391/grind2-based-3d-qsar-and-prediction-of-activity-spectra-for-symmetrical-bis-pyridinium-salts-with-promastigote-antileishmanial-activity
#14
Evelyn Mirella Lopes Pina Diniz, Carlos Henrique Tomich de Paula da Silva, Verónica Gómez Perez, Leonardo Bruno Federico, Joaquín María Campos Rosa
Leishmaniasis is a major group of neglected tropical diseases caused by the protozoan parasite Leishmania. About 12 million people are affected in 98 countries and 350 million people worldwide are at risk of infection. Current leishmaniasis treatments rely on a relatively small arsenal of drugs, including amphotericin B, pentamidine and others, which in general have some type of inconvenience. Recently, we have synthesized antileishmanial bis-pyridinium derivatives and symmetrical bis-pyridinium cyclophanes...
August 5, 2016: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/27491458/zoonotic-trypanosomes-in-south-east-asia-attempts-to-control-trypanosoma-lewisi-using-human-and-animal-trypanocidal-drugs
#15
Marc Desquesnes, Sarawut Yangtara, Pawinee Kunphukhieo, Sathaporn Jittapalapong, Stéphane Herder
Beside typical human trypanosomes responsible of sleeping sickness in Africa and Chagas disease in Latin America, there is a growing number of reported atypical human infections due to Trypanosoma evansi, a livestock parasite, or Trypanosoma lewisi, a rat parasite, especially in Asia. Drugs available for the treatment of T. brucei ssp. in humans are obviously of choice for the control of T. evansi because it is derived from T. brucei. However, concerning T. lewisi, there is an urgent need to determine the efficacy of trypanocidal drugs for the treatment in humans...
October 2016: Infection, Genetics and Evolution
https://www.readbyqxmd.com/read/27442262/trypanocidal-activity-of-flavokawin-b-a-component-of-polygonum-ferrugineum-wedd
#16
Danilo F Rodrigues, David A Maniscalco, Flavia A J Silva, Bruna G Chiari, María V Castelli, Vera L B Isaac, Regina M B Cicarelli, Silvia N López
The trypanocidal potential of the natural chalcone flavokawin B, which was isolated from the hexanic extract of Polygonum ferrugineum Wedd., is reported here. Although flavokawin B is widespread, this is the first report about its trypanocidal properties on both Trypanosoma cruzi (IC50 = 9.5 µM, IC50 = 34.7 µM benznidazol, Y strain) epimastigotes and Trypanosoma brucei (IC50 = 4.8 µM, IC50 = 6.4 µM pentamidine, 29-13 strain) procyclic forms, which was also corroborated on T. brucei strain 427 (IC50 = 6...
July 21, 2016: Planta Medica
https://www.readbyqxmd.com/read/27357655/in-vitro-synergistic-combinations-of-pentamidine-polymyxin-b-tigecycline-and-tobramycin-with-antifungal-agents-against-fusarium-spp
#17
Tarcieli Pozzebon Venturini, Luana Rossato, Francieli Chassot, Jéssica Tairine Keller, Fernanda Baldissera Piasentin, Janio Morais Santurio, Sydney Hartz Alves
The genus Fusarium is characterized by hyaline filamentous fungi that cause infections predominantly in immunocompromised patients. The remarkable primary resistance to antifungal agents of this genus requires a search for new therapeutic possibilities. This study assessed the in vitro susceptibility of 25 clinical isolates of Fusarium against antifungal agents (amphotericin B, caspofungin, itraconazole and voriconazole) and antimicrobials (pentamidine, polymyxin B, tigecycline and tobramycin) according to the broth microdilution method (M38-A2)...
August 2016: Journal of Medical Microbiology
https://www.readbyqxmd.com/read/27353022/serial-use-of-pentamidine-and-miltefosine-for-treating-leishmania-infantum-hiv-coinfection
#18
Jean-François Faucher, David Morquin, Jacques Reynes, Catherine Chirouze, Bruno Hoen, Vincent Le Moing
Liposomal amphotericin B (LAmb) may fail to heal Leishmania infantum visceral leishmaniasis (VL) in the immunodeficient host. There are currently no guidelines on how to treat such patients and efficacy of miltefosine monotherapy seems limited in this indication. We present 2 cases of patients with VL and AIDS for which LAmb had to be interrupted (one because of toxicity, one because of treatment failure) and who were treated effectively with pentamidine followed by miltefosine.
October 2016: Parasitology International
https://www.readbyqxmd.com/read/27297108/pentamidine-blocks-the-interaction-between-mutant-s100a5-and-rage-v-domain-and-inhibits-the-rage-signaling-pathway
#19
Ching Chang Cho, Ruey Hwang Chou, Chin Yu
The human S100 protein family contains small, dimeric and acidic proteins that contain two EF-hand motifs and bind calcium. When S100A5 binds calcium, its conformation changes and promotes interaction with the target protein. The extracellular domain of RAGE (Receptor of Advanced Glycation End products) contain three domains: C1, C2 and V. The RAGE V domain is the target protein of S100A5 that promotes cell survival, growth and differentiation by activating several signaling pathways. Pentamidine is an apoptotic and antiparasitic drug that is used to treat or prevent pneumonia...
August 19, 2016: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/27282640/multi-parametric-assessment-of-cardiomyocyte-excitation-contraction-coupling-using-impedance-and-field-potential-recording-a-tool-for-cardiac-safety-assessment
#20
Xiaoyu Zhang, Liang Guo, Haoyu Zeng, Stephen L White, Michael Furniss, Bharathi Balasubramanian, Edward Lis, Armando Lagrutta, Frederick Sannajust, Li Leyna Zhao, Biao Xi, Xiaobo Wang, Myrtle Davis, Yama A Abassi
INTRODUCTION: The ICH S7B guidelines recommend that all new chemical entities should be subjected to hERG repolarization screening due to its association with life-threatening "Torsades de Pointes" (TdP) arrhythmia. However, it has become evident that not all hERG channel inhibitors result in TdP and not all compounds that induce QT prolongation and TdP necessarily inhibit hERG. In order to address the limitations of the S7B/E14 guidelines, the FDA through a public/private partnership initiated the Comprehensive in vitro Proarrhythmia Assay (CiPA) initiative to examine the possible modification and refinement of the ICH E14/S7B guidelines...
September 2016: Journal of Pharmacological and Toxicological Methods
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