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International Journal for Parasitology, Drugs and Drug Resistance

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https://www.readbyqxmd.com/read/29425734/in-vitro-and-in-vivo-pharmacodynamics-of-three-novel-antileishmanial-lead-series
#1
M Van den Kerkhof, D Mabille, E Chatelain, C E Mowbray, S Braillard, S Hendrickx, L Maes, G Caljon
OBJECTIVES: Three new chemical series (bicyclic nitroimidazoles, aminopyrazoles and oxaboroles) were selected by Drugs for Neglected Diseases initiative as potential new drug leads for leishmaniasis. Pharmacodynamics studies included both in vitro and in vivo efficacy, cross-resistance profiling against the current antileishmanial reference drugs and evaluation of their cidal activity potential. METHODS: Efficacy against the reference laboratory strains of Leishmania infantum (MHOM/MA(BE)/67/ITMAP263) and L...
January 31, 2018: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/29414109/p-glycoprotein-9-and-macrocyclic-lactone-resistance-status-in-selected-strains-of-the-ovine-gastrointestinal-nematode-teladorsagia-circumcincta
#2
Frank Turnbull, Nicholas N Jonsson, Fiona Kenyon, Philip J Skuce, Stewart A Bisset
The Teladorsagia circumcincta P-glycoprotein-9 (Tci-pgp-9) gene has previously been implicated in multiple-anthelmintic resistance in this parasite. Here we further characterise genetic diversity in Tci-pgp-9 and its possible role in ivermectin (IVM) and multi-drug resistance using two UK field isolates of T. circumcincta, one susceptible to anthelmintics (MTci2) and the other resistant to most available anthelmintics including IVM (MTci5). A comparison of full-length Tci-pgp-9 cDNA transcripts from the MTci2 and MTci5 isolates (∼3...
January 31, 2018: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/29414107/synthesis-of-aminophenylhydroxamate-and-aminobenzylhydroxamate-derivatives-and-in-vitro-screening-for-antiparasitic-and-histone-deacetylase-inhibitory-activity
#3
C Loeuillet, B Touquet, B Oury, N Eddaikra, J L Pons, J F Guichou, G Labesse, D Sereno
A series of aminophenylhydroxamates and aminobenzylhydroxamates were synthesized and screened for their antiparasitic activity against Leishmania, Trypanosoma, and Toxoplasma. Their anti-histone deacetylase (HDAC) potency was determined. Moderate to no antileishmanial or antitrypanosomal activity was found (IC50 > 10 μM) that contrast with the highly efficient anti-Toxoplasma activity (IC50 < 1.0 μM) of these compounds. The antiparasitic activity of the synthetized compounds correlates well with their HDAC inhibitory activity...
January 31, 2018: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/29414106/metabolism-of-albendazole-ricobendazole-and-flubendazole-in-haemonchus-contortus-adults-sex-differences-resistance-related-differences-and-the-identification-of-new-metabolites
#4
Lucie Raisová Stuchlíková, Petra Matoušková, Ivan Vokřál, Jiří Lamka, Barbora Szotáková, Anna Sečkařová, Diana Dimunová, Linh Thuy Nguyen, Marián Várady, Lenka Skálová
Haemonchus contortus (family Trichostrongylidae, Nematoda), a hematophagous gastrointestinal parasite found in small ruminants, has a great ability to develop resistance to anthelmintic drugs. We studied the biotransformation of the three benzimidazole anthelmintics: albendazole (ABZ), ricobendazole (albendazole S-oxide; RCB) and flubendazole (FLU) in females and males of H. contortus in both a susceptible ISE strain and resistant IRE strain. The ex vivo cultivation of living nematodes in culture medium with or without the anthelmintics was used...
January 27, 2018: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/29414105/discovery-of-ebselen-as-an-inhibitor-of-cryptosporidium-parvum-glucose-6-phosphate-isomerase-cpgpi-by-high-throughput-screening-of-existing-drugs
#5
Rana Eltahan, Fengguang Guo, Haili Zhang, Lixin Xiang, Guan Zhu
Cryptosporidium parvum is a water-borne and food-borne apicomplexan pathogen. It is one of the top four diarrheal-causing pathogens in children under the age of five in developing countries, and an opportunistic pathogen in immunocompromised individuals. Unlike other apicomplexans, C. parvum lacks Kreb's cycle and cytochrome-based respiration, thus relying mainly on glycolysis to produce ATP. In this study, we characterized the primary biochemical features of the C. parvum glucose-6-phosphate isomerase (CpGPI) and determined its Michaelis constant towards fructose-6-phosphate (Km = 0...
January 25, 2018: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/29414108/the-optimal-timing-of-post-treatment-sampling-for-the-assessment-of-anthelminthic-drug-efficacy-against-ascaris-infections-in-humans
#6
Bruno Levecke, Alice V Easton, Piet Cools, Marco Albonico, Shaali Ame, John S Gilleard, Jennifer Keiser, Antonio Montresor, Roger Prichard, Johnny Vlaminck, Jozef Vercruysse
The egg reduction rate (ERR) is the current standard mean to assess the efficacy of drugs against human soil-transmitted helminths (STHs; Ascaris lumbricoides, Trichuris trichiura and hookworm). Although the timing of post-treatment sampling is pivotal for a readily interpretation of drug efficacy, there is lack empirical data that allows recommending the optimal time point for a follow-up egg counting. In the present study, we re-analyzed both the kinetics of worm expulsion and egg output for Ascaris lumbricoides following a single oral dose of albendazole in a series of studies previously conducted in Kenyan communities...
January 13, 2018: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/29324251/potential-role-of-plasmodium-falciparum-exported-protein-1-in-the-chloroquine-mode-of-action
#7
Andreas Martin Lisewski, Joel Patrick Quiros, Monica Mittal, Nagireddy Putluri, Arun Sreekumar, Jesper Z Haeggström, Olivier Lichtarge
In the human malaria parasite Plasmodium falciparum, membrane glutathione S-transferases (GST) have recently emerged as potential cellular detoxifying units and as drug target candidates with the artemisinin (ART) class of antimalarials inhibiting their activity at single-digit nanomolar potency when activated by iron sources such as cytotoxic hematin. Here we put forward the hypothesis that the membrane GST Plasmodium falciparum exported protein 1 (PfEXP1, PF3D7_1121600) might be directly involved in the mode of action of the unrelated antimalarial 4-aminoquinoline drug chloroquine (CQ)...
December 27, 2017: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/29274827/motility-in-the-l3-stage-is-a-poor-phenotype-for-detecting-and-measuring-resistance-to-avermectin-milbemycin-drugs-in-gastrointestinal-nematodes-of-livestock
#8
Melissa M George, Lorraine Lopez-Soberal, Bob E Storey, Sue B Howell, Ray M Kaplan
Motility is a commonly used in vitro phenotype for assessing anthelmintic activity of candidate compounds, and for detecting anthelmintic resistance in nematodes. Third-stage larvae (L3) of parasitic nematodes are commonly used in motility-based assays because L3 are simple to obtain and can remain viable in storage for extended periods. To improve the measurement of motility of microscopic stages of nematodes, our laboratory developed the Worminator, which quantitatively measures motility of parasites. Using the Worminator, we compared the dose-response characteristics of several avermectin/milbemycin (AM) compounds using L3 from both AM-susceptible and AM-resistant Cooperia spp...
December 18, 2017: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/29366967/monepantel-is-a-non-competitive-antagonist-of-nicotinic-acetylcholine-receptors-from-ascaris-suum-and-oesophagostomum-dentatum
#9
Melanie Abongwa, Djordje S Marjanovic, James G Tipton, Fudan Zheng, Richard J Martin, Sasa M Trailovic, Alan P Robertson
Zolvix® is a recently introduced anthelmintic drench containing monepantel as the active ingredient. Monepantel is a positive allosteric modulator of DEG-3/DES-2 type nicotinic acetylcholine receptors (nAChRs) in several nematode species. The drug has been reported to produce hypercontraction of Caenorhabditis elegans and Haemonchus contortus somatic muscle. We investigated the effects of monepantel on nAChRs from Ascaris suum and Oesophagostomum dentatum heterologously expressed in Xenopus laevis oocytes...
December 16, 2017: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/29223747/an-automated-high-throughput-system-for-phenotypic-screening-of-chemical-libraries-on-c-elegans-and-parasitic-nematodes
#10
Frederick A Partridge, Anwen E Brown, Steven D Buckingham, Nicky J Willis, Graham M Wynne, Ruth Forman, Kathryn J Else, Alison A Morrison, Jacqueline B Matthews, Angela J Russell, David A Lomas, David B Sattelle
Parasitic nematodes infect hundreds of millions of people and farmed livestock. Further, plant parasitic nematodes result in major crop damage. The pipeline of therapeutic compounds is limited and parasite resistance to the existing anthelmintic compounds is a global threat. We have developed an INVertebrate Automated Phenotyping Platform (INVAPP) for high-throughput, plate-based chemical screening, and an algorithm (Paragon) which allows screening for compounds that have an effect on motility and development of parasitic worms...
December 2, 2017: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/29207309/polypyridylruthenium-ii-complexes-exert-in-vitro-and-in-vivo-nematocidal-activity-and-show-significant-inhibition-of-parasite-acetylcholinesterases
#11
Madhu Sundaraneedi, Ramon M Eichenberger, Rafid Al-Hallaf, Dai Yang, Javier Sotillo, Siji Rajan, Phurpa Wangchuk, Paul R Giacomin, F Richard Keene, Alex Loukas, J Grant Collins, Mark S Pearson
Over 4.5 billion people are at risk of infection with soil transmitted helminths and there are concerns about the development of resistance to the handful of frontline nematocides in endemic populations. We investigated the anti-nematode efficacy of a series of polypyridylruthenium(II) complexes and showed they were active against L3 and adult stages of Trichuris muris, the rodent homologue of the causative agent of human trichuriasis, T. trichiura. One of the compounds, Rubb12-mono, which was among the most potent in its ability to kill L3 (IC50 = 3...
November 29, 2017: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/29197728/disulfiram-as-a-novel-inactivator-of-giardia-lamblia-triosephosphate-isomerase-with-antigiardial-potential
#12
Adriana Castillo-Villanueva, Yadira Rufino-González, Sara-Teresa Méndez, Angélica Torres-Arroyo, Martha Ponce-Macotela, Mario Noé Martínez-Gordillo, Horacio Reyes-Vivas, Jesús Oria-Hernández
Giardiasis, the infestation of the intestinal tract by Giardia lamblia, is one of the most prevalent parasitosis worldwide. Even though effective therapies exist for it, the problems associated with its use indicate that new therapeutic options are needed. It has been shown that disulfiram eradicates trophozoites in vitro and is effective in vivo in a murine model of giardiasis; disulfiram inactivation of carbamate kinase by chemical modification of an active site cysteine has been proposed as the drug mechanism of action...
December 2017: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/29156431/pathway-of-oxfendazole-from-the-host-into-the-worm-trichuris-suis-in-pigs
#13
Tina V A Hansen, Andrew R Williams, Matthew Denwood, Peter Nejsum, Stig M Thamsborg, Christian Friis
It is well known that the efficacy of a single oral dose of benzimidazoles against Trichuris spp. infections in humans and animals is poor, but is currently still used in control programmes against human trichuriasis. However, the route of the benzimidazoles from the treated host to Trichuris remains unknown. As parts of adult Trichuris are situated intracellularly in the caecum, they might be exposed to anthelmintic drugs in the intestinal content as well as the mucosa. In this study, the pathway of oxfendazole and its metabolites was explored using a T...
December 2017: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/29128302/corrigendum-to-genetic-diversity-of-next-generation-antimalarial-targets-a-baseline-for-drug-resistance-surveillance-programmes-int-j-parasitol-drugs-and-drug-resist-7-2017-174-180
#14
Ana Rita Gomes, Matt Ravenhall, Ernest Diez Benavente, Arthur Talman, Colin Sutherland, Cally Roper, Taane G Clark, Susana Campino
No abstract text is available yet for this article.
November 6, 2017: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/29149701/risk-factor-analysis-of-equine-strongyle-resistance-to-anthelmintics
#15
G Sallé, J Cortet, I Bois, C Dubès, Q Guyot-Sionest, C Larrieu, V Landrin, G Majorel, S Wittreck, E Woringer, A Couroucé, J Guillot, P Jacquiet, F Guégnard, A Blanchard, A Leblond
Intestinal strongyles are the most problematic endoparasites of equids as a result of their wide distribution and the spread of resistant isolates throughout the world. While abundant literature can be found on the extent of anthelmintic resistance across continents, empirical knowledge about associated risk factors is missing. This study brought together results from anthelmintic efficacy testing and risk factor analysis to provide evidence-based guidelines in the field. It involved 688 horses from 39 French horse farms and riding schools to both estimate Faecal Egg Count Reduction (FECR) after anthelmintic treatment and to interview farm and riding school managers about their practices...
November 2, 2017: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/29121562/p-glycoproteins-play-a-role-in-ivermectin-resistance-in-cyathostomins
#16
L E Peachey, G L Pinchbeck, J B Matthews, F A Burden, A Lespine, G von Samson-Himmelstjerna, J Krücken, J E Hodgkinson
Anthelmintic resistance is a global problem that threatens sustainable control of the equine gastrointestinal cyathostomins (Phylum Nematoda; Superfamily Strongyloidea). Of the three novel anthelmintic classes that have reached the veterinary market in the last decade, none are currently licenced in horses, hence current control regimens focus on prolonging the useful lifespan of licenced anthelmintics. This approach would be facilitated by knowledge of the resistance mechanisms to the most widely used anthelmintics, the macrocyclic lactones (ML)...
October 25, 2017: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/29128848/antimalarial-activity-of-malaria-box-compounds-against-plasmodium-falciparum-clinical-isolates
#17
Jersley D Chirawurah, Felix Ansah, Prince B Nyarko, Samuel Duodu, Yaw Aniweh, Gordon A Awandare
Malaria remains a major cause of childhood deaths in resource-limited settings. In the absence of an effective vaccine, drugs and other interventions have played very significant roles in combating the scourge of malaria. The recent reports of resistance to artemisinin necessitate the need for new antimalarial drugs with novel mechanisms of action. Towards the development of new, affordable and easily accessible antimalarial drugs for endemic regions, the Medicines for Malaria Venture (MMV) assembled a total of 400 active antimalarial compounds called the Malaria Box...
October 16, 2017: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/29035735/transcriptome-profiling-identifies-genes-pathways-associated-with-experimental-resistance-to-paromomycin-in-leishmania-donovani
#18
Aditya Verma, Vasundhra Bhandari, Deepak Kumar Deep, Shyam Sundar, Jean Claude Dujardin, Ruchi Singh, Poonam Salotra
Widespread resistance towards antimony and reports of relapses following miltefosine treatment has severely affected the management of visceral leishmaniasis (VL) in the Indian subcontinent. Paromomycin (PMM), an aminoglycoside antibiotic, has been licensed for VL treatment in India in 2007. Although its use is still restricted in the field, unraveling the molecular mechanism of resistance towards PMM is the key to preserve the drug. In this study, PMM resistant lines were selected up to 100 μM of PMM in three distinct field isolates of Leishmania donovani at promastigote stage...
October 10, 2017: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/29040909/treatment-with-fenofibrate-plus-a-low-dose-of-benznidazole-attenuates-cardiac-dysfunction-in-experimental-chagas-disease
#19
Ágata C Cevey, Gerardo A Mirkin, Martín Donato, María J Rada, Federico N Penas, Ricardo J Gelpi, Nora B Goren
Trypanosoma cruzi induces serious cardiac alterations during the chronic infection. Intense inflammatory response observed from the beginning of infection, is critical for the control of parasite proliferation and evolution of Chagas disease. Peroxisome proliferator-activated receptors (PPAR)-α, are known to modulate inflammation. In this study we investigated whether a PPAR-α agonist, Fenofibrate, improves cardiac function and inflammatory parameters in a murine model of T. cruzi infection. BALB/c mice were sequentially infected with two T...
October 7, 2017: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/29035734/comparison-of-constitutive-and-thiabendazole-induced-expression-of-five-cytochrome-p450-genes-in-fourth-stage-larvae-of-haemonchus-contortus-isolates-with-different-drug-susceptibility-identifies-one-gene-with-high-constitutive-expression-in-a-multi-resistant
#20
Esra Yilmaz, Sabrina Ramünke, Janina Demeler, Jürgen Krücken
Benzimidazoles (BZs) remain amongst the most widely used anthelmintic drug classes against gastro-intestinal nematode infections, although their efficacy is increasingly compromised by resistance. The primary underlying mechanisms for BZ resistance are single-nucleotide polymorphisms (SNPs) in the isotype 1 β-tubulin gene causing the substitutions F167Y, E198A or F200Y. However, resistance is believed to be multi-genic and previous studies have shown that isolates carrying 90-100% F200Y can vary considerably in their resistance level in the egg hatch assay (EHA)...
October 7, 2017: International Journal for Parasitology, Drugs and Drug Resistance
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