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https://www.readbyqxmd.com/read/29128607/effects-of-a-new-antiprotozoal-drug-n-n-diphenyl-4-methoxy-benzamidine-on-energy-linked-functions-of-rat-liver-mitochondria
#1
Lyvia Lintzmaier Petiz, Amanda do Rocio Andrade Pires, Aurea Echevarria, Cláudio Eduardo Rodrigues-Santos, Maria Eliane Merlin Rocha, Alexandra Acco, Silvia Maria Suter Correia Cadena
Amidines are chemically characterized by the presence of two nitrogen atoms that bind to the same carbon atom in its structure. Several biological activities have been ascribed to these compounds. Pentamidine, an aromatic diamidine, is effective in the treatment against Pneumocystis carinii and leishmaniasis, but it can also have severe side effects. New amidine derivatives have been synthesized, among them N,N'-diphenyl-4-methoxy-benzamidine (methoxyamidine), which is effective against Leishmania amazonensis (LD50 = 20 μM) and Trypanosoma cruzi (LD50 = 59 nM)...
November 9, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/29126729/indole-and-benzimidazole-bichalcophenes-synthesis-dna-binding-and-antiparasitic-activity
#2
Abdelbasset A Farahat, Mohamed A Ismail, Arvind Kumar, Tanja Wenzler, Reto Brun, Ananya Paul, W David Wilson, David W Boykin
A novel series of indole and benzimidazole bichalcophene diamidine derivatives were prepared to study their antimicrobial activity against the tropical parasites causing African sleeping sickness and malaria. The dicyanoindoles needed to synthesize the target diamidines were obtained through Stille coupling reactions while the bis-cyanobenzimidazoles intermediates were made via condensation/cyclization reactions of different aldehydes with 4-cyano-1,2-diaminobenzene. Different amidine synthesis methodologies namely, lithium bis-trimethylsilylamide (LiN[Si(CH3)3]2) and Pinner methods were used to prepare the diamidines...
October 22, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29109372/marine-algae-as-source-of-novel-antileishmanial-drugs-a-review
#3
REVIEW
Lauve Rachel Tchokouaha Yamthe, Regina Appiah-Opong, Patrick Valere Tsouh Fokou, Nole Tsabang, Fabrice Fekam Boyom, Alexander Kwadwo Nyarko, Michael David Wilson
Leishmaniasis is a vector-borne neglected tropical disease caused by protozoan parasites of the Leishmania genus and transmitted by the female Phlebotomus and Lutzomyia sand flies. The currently prescribed therapies still rely on pentavalent antimonials, pentamidine, paromomycin, liposomal amphotericin B, and miltefosine. However, their low efficacy, long-course treatment regimen, high toxicity, adverse side effects, induction of parasite resistance and high cost require the need for better drugs given that antileishmanial vaccines may not be available in the near future...
October 29, 2017: Marine Drugs
https://www.readbyqxmd.com/read/29020217/long-term-clinical-outcomes-in-visceral-leishmaniasis-hiv-co-infected-patients-during-and-after-pentamidine-secondary-prophylaxis-in-ethiopia-a-single-arm-clinical-trial-authors-and-affiliations
#4
Ermias Diro, Koert Ritmeijer, Marleen Boelaert, Fabiana Alves, Rezika Mohammed, Charles Abongomera, Raffaella Ravinetto, Maaike De Crop, Helina Fikre, Cherinet Adera, Harry van Loen, Achilleas Tsoumanis, Wim Adriaensen, Asrat Hailu, Johan van Griensven
Background: We have conducted a single-arm trial evaluating monthly pentamidine secondary prophylaxis (PSP) to prevent visceral leishmaniasis (VL) relapse in Ethiopian HIV-patients. Outcomes at 12 months of PSP have been previously reported, supporting PSP effectiveness and safety. However, remaining relapse-free after PSP discontinuation is vital. We now report outcomes and associated factors for a period of upto 2.5 years after initiating PSP, including one year follow-up after PSP discontinuation...
September 13, 2017: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
https://www.readbyqxmd.com/read/28993158/high-potency-block-of-kir4-1-channels-by-pentamidine-molecular-basis
#5
Iván A Aréchiga-Figueroa, Leticia G Marmolejo-Murillo, Meng Cui, Mayra Delgado-Ramírez, Marcel A G van der Heyden, José A Sánchez-Chapula, Aldo A Rodríguez-Menchaca
Inward rectifier potassium (Kir) channels are expressed in almost all mammalian tissues and contribute to a wide range of physiological processes. Kir4.1 channel expression is found in the brain, inner ear, eye, and kidney. Loss-of-function mutations in the pore-forming Kir4.1 subunit cause an autosomal recessive disorder characterized by epilepsy, ataxia, sensorineural deafness and tubulopathy (SeSAME/EST syndrome). Despite its importance in physiological and pathological conditions, pharmacological research of Kir4...
October 6, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28898546/taking-the-challenge-a-protocolized-approach-to-optimize-pneumocystis-pneumonia-prophylaxis-in-renal-transplant-recipients
#6
K F Urbancic, F Ierino, E Phillips, P F Mount, A Mahony, J A Trubiano
While trimethoprim-sulfamethoxazole is considered first-line therapy for Pneumocystis pneumonia prevention in renal transplant recipients, reported adverse drug reactions may limit use and increase reliance on costly and less effective alternatives, often aerosolized pentamidine. We report our experience implementing a protocolized approach to trimethoprim-sulfamethoxazole adverse drug reaction assessment and rechallenge to optimize prophylaxis in this patient cohort. We retrospectively reviewed 119 patients receiving Pneumocystis pneumonia prophylaxis prior to and after protocol implementation...
September 12, 2017: American Journal of Transplantation
https://www.readbyqxmd.com/read/28888990/chemicals-or-mutations-that-target-mitochondrial-translation-can-rescue-the-respiratory-deficiency-of-yeast-bcs1-mutants
#7
C Panozzo, A Laleve, D Tribouillard-Tanvier, J Ostojić, C H Sellem, G Friocourt, A Bourand-Plantefol, A Burg, A Delahodde, M Blondel, G Dujardin
Bcs1p is a chaperone that is required for the incorporation of the Rieske subunit within complex III of the mitochondrial respiratory chain. Mutations in the human gene BCS1L (BCS1-like) are the most frequent nuclear mutations resulting in complex III-related pathologies. In yeast, the mimicking of some pathogenic mutations causes a respiratory deficiency. We have screened chemical libraries and found that two antibiotics, pentamidine and clarithromycin, can compensate two bcs1 point mutations in yeast, one of which is the equivalent of a mutation found in a human patient...
December 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28874072/liposomal-formulations-in-the-pharmacological-treatment-of-leishmaniasis-a-review
#8
Vanessa Ortega, Selma Giorgio, Eneida de Paula
Conventional chemotherapy for leishmaniasis includes considerably toxic drugs and reports of drug-resistance are not uncommon. Liposomal encapsulated drugs appear as an option for the treatment of leishmaniasis, providing greater efficacy for the active and reducing its side effects by promoting superior tissue absorption, favouring drug penetration into the macrophages, and retarding its clearance from the site of action. In this paper, a review on the advances achieved with liposome-based anti-leishmaniasis drug delivery systems is presented...
September 2017: Journal of Liposome Research
https://www.readbyqxmd.com/read/28831945/studies-in-vitro-on-infectivity-and-sensitivity-to-antileishmanial-drugs-in-new-world-leishmania-species-transfected-with-the-green-fluorescent-protein-pir3-egfp
#9
Genesis Palacios, Adriana Parodi, Yulieth A Upegui, Andres Montoya, Sergio Pulido, Iván D Vélez, Sara M Robledo
Current chemotherapeutic agents for leishmaniasis have several disadvantages interfering with the effective treatment and therefore more and better antileishmanial drugs are needed. Discovery of candidates for leishmaniasis treatment requires not only accurate and precise methodologies but also well-known biological system to measure infectivity of parasites and antileishmanial activity of the new compounds. Significant variation in the in vitro and in vivo infectivity and sensitivity to established and experimental drugs in Leishmania strains are reported...
November 2017: Parasitology
https://www.readbyqxmd.com/read/28782390/treatment-of-pneumocystis-jirovecii-pneumonia-in-hiv-infected-patients-a-review
#10
Yu-Shan Huang, Jen-Jia Yang, Nan-Yao Lee, Guan-Jhou Chen, Wen-Chien Ko, Hsin-Yun Sun, Chien-Ching Hung
Pneumocystis pneumonia is a potentially life-threatening pulmonary infection that occurs in immunocompromised individuals and HIV-infected patients with a low CD4 cell count. Trimethoprim-sulfamethoxazole has been used as the first-line agent for treatment, but mutations within dihydropteroate synthase gene render potential resistance to sulfamide. Despite advances of combination antiretroviral therapy (cART), Pneumocystis pneumonia continues to occur in HIV-infected patients with late presentation for cART or virological and immunological failure after receiving cART...
September 2017: Expert Review of Anti-infective Therapy
https://www.readbyqxmd.com/read/28756612/clinical-pharmacokinetics-of-systemically-administered-antileishmanial-drugs
#11
REVIEW
Anke E Kip, Jan H M Schellens, Jos H Beijnen, Thomas P C Dorlo
This review describes the pharmacokinetic properties of the systemically administered antileishmanial drugs pentavalent antimony, paromomycin, pentamidine, miltefosine and amphotericin B (AMB), including their absorption, distribution, metabolism and excretion and potential drug-drug interactions. This overview provides an understanding of their clinical pharmacokinetics, which could assist in rationalising and optimising treatment regimens, especially in combining multiple antileishmanial drugs in an attempt to increase efficacy and shorten treatment duration...
July 29, 2017: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/28711067/pa-6-inhibits-inward-rectifier-currents-carried-by-v93i-and-d172n-gain-of-function-kir2-1-channels-but-increases-channel-protein-expression
#12
Yuan Ji, Marlieke G Veldhuis, Jantien Zandvoort, Fee L Romunde, Marien J C Houtman, Karen Duran, Gijs van Haaften, Eva-Maria Zangerl-Plessl, Hiroki Takanari, Anna Stary-Weinzinger, Marcel A G van der Heyden
BACKGROUND: The inward rectifier potassium current IK1 contributes to a stable resting membrane potential and phase 3 repolarization of the cardiac action potential. KCNJ2 gain-of-function mutations V93I and D172N associate with increased IK1, short QT syndrome type 3 and congenital atrial fibrillation. Pentamidine-Analogue 6 (PA-6) is an efficient (IC50 = 14 nM with inside-out patch clamp methodology) and specific IK1 inhibitor that interacts with the cytoplasmic pore region of the KIR2...
July 15, 2017: Journal of Biomedical Science
https://www.readbyqxmd.com/read/28685254/kh-tfmdi-a-novel-sirtuin-inhibitor-alters-the-cytoskeleton-and-mitochondrial-metabolism-promoting-cell-death-in-leishmania-amazonensis
#13
Brunno Renato Farias Verçoza, Joseane Lima Prado Godinho, Sara Teixeira de Macedo-Silva, Kilian Huber, Franz Bracher, Wanderley de Souza, Juliany Cola Fernandes Rodrigues
Treatment of leishmaniasis involves the use of antimonials, miltefosine, amphotericin B or pentamidine. However, the side effects of these drugs and the reports of drug-resistant parasites demonstrate the need for new treatments that are safer and more efficacious. Histone deacetylase inhibitors are a new class of compounds with potential to treat leishmaniasis. Herein, we evaluated the effects of KH-TFMDI, a novel histone deacetylase inhibitor, on Leishmania amazonensis promastigotes and intracellular amastigotes...
July 6, 2017: Apoptosis: An International Journal on Programmed Cell Death
https://www.readbyqxmd.com/read/28623239/-ccug-n-rna-toxicity-in-a-drosophila-model-of-myotonic-dystrophy-type-2-dm2-activates-apoptosis
#14
Vildan Betul Yenigun, Mario Sirito, Alla Amcheslavky, Tomek Czernuszewicz, Jordi Colonques-Bellmunt, Irma García-Alcover, Marzena Wojciechowska, Clare Bolduc, Zhihong Chen, Arturo López Castel, Ralf Krahe, Andreas Bergmann
The myotonic dystrophies are prototypic toxic RNA gain-of-function diseases. Myotonic dystrophy type 1 (DM1) and type 2 (DM2) are caused by different unstable, noncoding microsatellite repeat expansions - (CTG)DM1 in DMPK and (CCTG)DM2 in CNBP Although transcription of mutant repeats into (CUG)DM1 or (CCUG)DM2 appears to be necessary and sufficient to cause disease, their pathomechanisms remain incompletely understood. To study the mechanisms of (CCUG)DM2 toxicity and develop a convenient model for drug screening, we generated a transgenic DM2 model in the fruit fly Drosophila melanogaster with (CCUG)n repeats of variable length (n=16 and 106)...
August 1, 2017: Disease Models & Mechanisms
https://www.readbyqxmd.com/read/28622334/sterol-14%C3%AE-demethylase-mutation-leads-to-amphotericin-b-resistance-in-leishmania-mexicana
#15
Roy Mwenechanya, Julie Kovářová, Nicholas J Dickens, Manikhandan Mudaliar, Pawel Herzyk, Isabel M Vincent, Stefan K Weidt, Karl E Burgess, Richard J S Burchmore, Andrew W Pountain, Terry K Smith, Darren J Creek, Dong-Hyun Kim, Galina I Lepesheva, Michael P Barrett
Amphotericin B has emerged as the therapy of choice for use against the leishmaniases. Administration of the drug in its liposomal formulation as a single injection is being promoted in a campaign to bring the leishmaniases under control. Understanding the risks and mechanisms of resistance is therefore of great importance. Here we select amphotericin B-resistant Leishmania mexicana parasites with relative ease. Metabolomic analysis demonstrated that ergosterol, the sterol known to bind the drug, is prevalent in wild-type cells, but diminished in the resistant line, where alternative sterols become prevalent...
June 2017: PLoS Neglected Tropical Diseases
https://www.readbyqxmd.com/read/28583257/in-vitro-and-in-vivo-comparison-of-two-nebulizers-used-for-inhaled-pentamidine-delivery
#16
Nicolas Audag, Giuseppe Liistro, Dimitri Van der Linden, Françoise Smets, Teresinha Leal, Gregory Reychler
No abstract text is available yet for this article.
June 2, 2017: Archivos de Bronconeumología
https://www.readbyqxmd.com/read/28582438/in-silico-discovery-of-substituted-pyrido-2-3-d-pyrimidines-and-pentamidine-like-compounds-with-biological-activity-in-myotonic-dystrophy-models
#17
Àlex L González, Piotr Konieczny, Beatriz Llamusi, Estefanía Delgado-Pinar, José I Borrell, Jordi Teixidó, Enrique García-España, Manuel Pérez-Alonso, Roger Estrada-Tejedor, Rubén Artero
Myotonic dystrophy type 1 (DM1) is a rare multisystemic disorder associated with an expansion of CUG repeats in mutant DMPK (dystrophia myotonica protein kinase) transcripts; the main effect of these expansions is the induction of pre-mRNA splicing defects by sequestering muscleblind-like family proteins (e.g. MBNL1). Disruption of the CUG repeats and the MBNL1 protein complex has been established as the best therapeutic approach for DM1, hence two main strategies have been proposed: targeted degradation of mutant DMPK transcripts and the development of CUG-binding molecules that prevent MBNL1 sequestration...
2017: PloS One
https://www.readbyqxmd.com/read/28542844/the-inward-rectifier-current-inhibitor-pa-6-terminates-atrial-fibrillation-and-does-not-cause-ventricular-arrhythmias-in-goat-and-dog-models
#18
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: The density of the inward rectifier current (IK1 ) increases in atrial fibrillation (AF), shortening effective refractory period and thus promoting atrial re-entry. The synthetic compound pentamidine analogue 6 (PA-6) is a selective and potent IK1 inhibitor. We tested PA-6 for anti-AF efficacy and potential proarrhythmia, using established models in large animals. EXPERIMENTAL APPROACH: PA-6 was applied i.v. in anaesthetized goats with rapid pacing-induced AF and anaesthetized dogs with chronic atrio-ventricular (AV) block...
August 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28506844/proarrhythmic-risk-assessment-using-conventional-and-new-in%C3%A2-vitro-assays
#19
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
#20
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...
September 2017: Hepatology: Official Journal of the American Association for the Study of Liver Diseases
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