International Journal for Parasitology: Drugs and Drug Resistance This is an RSS file. You can use it to subscribe to this data in your favourite RSS reader or to display this data on your own website or blog.

An Abeis procera-derived tetracyclic triterpene containing a steroid-like nucleus core and a lactone side chain attenuates in vitro survival of both Fasciola hepatica and Schistosoma mansoni
Publication date: December 2018Source: International Journal for Parasitology: Drugs and Drug Resistance, Volume 8, Issue 3Author(s): Helen L. Whiteland, Anand Chakroborty, Josephine E. Forde-Thomas, Alessandra Crusco, Alan Cookson, Jackie Hollinshead, Caroline A. Fenn, Barbara Bartholomew, Peter A. Holdsworth, Maggie Fisher, Robert J. Nash, Karl F. HoffmannAbstractTwo economically and biomedically important platyhelminth species, Fasciola hepatica (liver fluke) and Schistosoma mansoni (blood fluke), are responsible for the neglected tropical diseases (NTDs) fasciolosis and schistosomiasis. Due to the absence of prophylact...
Source: International Journal for Parasitology: Drugs and Drug Resistance - November 3, 2018 Category: Parasitology Source Type: research

Repurposing of an old drug: In vitro and in vivo efficacies of buparvaquone against Echinococcus multilocularis
In this study, we screened the 400 compounds of the Medicines for Malaria Venture (MMV) Pathogen Box against E. multilocularis metacestodes. For the screen, we employed the phosphoglucose isomerase (PGI) assay which assesses drug-induced damage on metacestodes, and identified ten new compounds with activity against the parasite. The anti-theilerial drug MMV689480 (buparvaquone) and MMV671636 (ELQ-400) were the most promising compounds, with an IC50 of 2.87 μM and 0.02 μM respectively against in vitro cultured E. multilocularis metacestodes. Both drugs suggested a therapeutic window based on their cytotoxicity against...
Source: International Journal for Parasitology: Drugs and Drug Resistance - October 31, 2018 Category: Parasitology Source Type: research

Anthelmintic drug actions in resistant and susceptible C. elegans revealed by electrophysiological recordings in a multichannel microfluidic device
Publication date: Available online 30 October 2018Source: International Journal for Parasitology: Drugs and Drug ResistanceAuthor(s): Janis C. Weeks, Kristin J. Robinson, Shawn R. Lockery, William M. RobertsAbstractMany anthelmintic drugs used to treat parasitic nematode infections target proteins that regulate electrical activity of neurons and muscles: ion channels (ICs) and neurotransmitter receptors (NTRs). Perturbation of IC/NTR function disrupts worm behavior and can lead to paralysis, starvation, immune attack and expulsion. Limitations of current anthelmintics include a limited spectrum of activity across species a...
Source: International Journal for Parasitology: Drugs and Drug Resistance - October 30, 2018 Category: Parasitology Source Type: research

An Abeis procera - Derived tetracyclic triterpene containing a steroid-like nucleus core and a lactone side chain attenuates in vitro survival of both Fasciola hepatica and Schistosoma mansoni
Publication date: Available online 26 October 2018Source: International Journal for Parasitology: Drugs and Drug ResistanceAuthor(s): HelenL. Whiteland, Anand Chakroborty, Josephine E. Forde-Thomas, Alessandra Crusco, Alan Cookson, Jackie Hollinshead, Caroline A. Fenn, Barbara Bartholomew, PeterA. Holdsworth, Maggie Fisher, RobertJ. Nash, KarlF. HoffmannAbstractTwo economically and biomedically important platyhelminth species, Fasciola hepatica (liver fluke) and Schistosoma mansoni (blood fluke), are responsible for the neglected tropical diseases (NTDs) fasciolosis and schistosomiasis. Due to the absence of prophylactic v...
Source: International Journal for Parasitology: Drugs and Drug Resistance - October 27, 2018 Category: Parasitology Source Type: research

Investigating the function and possible biological role of an acetylcholine-gated chloride channel subunit (ACC-1) from the parasitic nematode Haemonchus contortus
Publication date: Available online 27 October 2018Source: International Journal for Parasitology: Drugs and Drug ResistanceAuthor(s): Micah K. Callanan, Sarah A. Habibi, Wen Jing Law, Kristen Nazareth, Richard L. Komuniecki, Sean G. ForresterAbstractThe cys-loop superfamily of ligand-gated ion channels are well recognized as important drug targets for many invertebrate specific compounds. With the rise in resistance seen worldwide to existing anthelmintics, novel drug targets must be identified so new treatments can be developed. The acetylcholine-gated chloride channel (ACC) family is a unique family of cholinergic recept...
Source: International Journal for Parasitology: Drugs and Drug Resistance - October 27, 2018 Category: Parasitology Source Type: research

Terror in the dirt: Sensory determinants of host seeking in soil-transmitted mammalian-parasitic nematodes
Publication date: Available online 26 October 2018Source: International Journal for Parasitology: Drugs and Drug ResistanceAuthor(s): Astra S. Bryant, Elissa A. HallemAbstractInfection with gastrointestinal parasitic nematodes is a major cause of chronic morbidity and economic burden around the world, particularly in low-resource settings. Some parasitic nematode species, including the human-parasitic threadworm Strongyloides stercoralis and human-parasitic hookworms in the genera Ancylostoma and Necator, feature a soil-dwelling infective larval stage that seeks out hosts for infection using a variety of host-emitted senso...
Source: International Journal for Parasitology: Drugs and Drug Resistance - October 26, 2018 Category: Parasitology Source Type: research

The Toll-Like Receptor 2 agonist PEG-Pam2Cys as an immunochemoprophylactic and immunochemotherapeutic against the liver and transmission stages of malaria parasites
We describe a new approach to both protection from and treatment of malaria parasites that involves the direct stimulation of the host innate immune response through the administration of a Toll-Like Receptor-2 (TLR2) agonist. The activity of PEG-Pam2Cys against the hepatocytic stages, erythrocytic stages and gametocytes of the rodent malaria parasite Plasmodium yoelii was investigated in laboratory mice. We show that administration of PEG-Pam2Cys, a soluble form of the TLR2 agonist S-[2,3-bis(palmitoyloxy)propyl] cysteine (Pam2Cys), significantly and dramatically reduces the numbers of malaria parasites that grow in the l...
Source: International Journal for Parasitology: Drugs and Drug Resistance - October 24, 2018 Category: Parasitology Source Type: research

Tamoxifen inhibits the biosynthesis of inositolphosphorylceramide in Leishmania
Publication date: Available online 24 October 2018Source: International Journal for Parasitology: Drugs and Drug ResistanceAuthor(s): Cristiana T. Trinconi, Danilo C. Miguel, Ariel M. Silber, Christopher Brown, John G.M. Mina, Paul W. Denny, Norton Heise, Silvia R.B. UlianaAbstractPrevious work from our group showed that tamoxifen, an oral drug that has been in use for the treatment of breast cancer for over 40 years, is active both in vitro and in vivo against several species of Leishmania, the etiological agent of leishmaniasis. Using a combination of metabolic labeling with [3H]-sphingosine and myo-[3H]-inositol, alkali...
Source: International Journal for Parasitology: Drugs and Drug Resistance - October 24, 2018 Category: Parasitology Source Type: research

Chloroquine analogs as antimalarial candidates with potent in vitro and in vivo activity
Publication date: Available online 13 October 2018Source: International Journal for Parasitology: Drugs and Drug ResistanceAuthor(s): Anna C.C. Aguiar, Erika Murce, Wilian A. Cortopassi, Andre S. Pimentel, Maria M.F.S. Almeida, Daniele C.S. Barros, Jéssica S. Guedes, Mario R. Meneghetti, Antoniana U. KrettliAbstractIn spite of recent efforts to eradicate malaria in the world, this parasitic disease is still considered a major public health problem, with a total of 216 million cases of malaria and 445,000 deaths in 2016. Artemisinin-based combination therapies remain effective in most parts of the world, but recent cases o...
Source: International Journal for Parasitology: Drugs and Drug Resistance - October 14, 2018 Category: Parasitology Source Type: research

A mutational and molecular dynamics study of the cys-loop GABA receptor Hco-UNC-49 from Haemonchus contortus: Agonist recognition in the nematode GABA receptor family
Publication date: Available online 6 October 2018Source: International Journal for Parasitology: Drugs and Drug ResistanceAuthor(s): Josh Foster, Everett Cochrane, Mohammad Hassan Khatami, Sarah A. Habibi, Hendrick de Haan, Sean G. ForresterAbstractThe UNC-49 receptor is unique nematode γ-aminobutyric acid (GABA)-gated chloride channel that may prove to be a novel target for the development of nematocides. Here we have characterized various charged amino acid residues in and near the agonist binding site of the UNC-49 receptor from the parasitic nematode Haemonchus contorts. Utilizing the Caenorhabditis elegans GluCl crys...
Source: International Journal for Parasitology: Drugs and Drug Resistance - October 6, 2018 Category: Parasitology Source Type: research

Recognition and killing of Brugia malayi microfilariae by human immune cells is dependent on the parasite sample and is not altered by ivermectin treatment
Publication date: Available online 22 September 2018Source: International Journal for Parasitology: Drugs and Drug ResistanceAuthor(s): Barbara J. Reaves, Connor Wallis, Ciaran J. McCoy, W. Walter Lorenz, Balazs Rada, Adrian J. WolstenholmeAbstractMass administration of macrocyclic lactones targets the transmission of the causative agents of lymphatic filariasis to their insect vectors by rapidly clearing microfilariae (Mf) from the circulation. It has been proposed that the anti-filarial action of these drugs may be mediated through the host immune system. We recently developed an in vitro assay for monitoring the attachm...
Source: International Journal for Parasitology: Drugs and Drug Resistance - October 4, 2018 Category: Parasitology Source Type: research

Molecular and pharmacological characterization of an acetylcholine-gated chloride channel (ACC-2) from the parasitic nematode Haemonchus contortus
Publication date: Available online 22 September 2018Source: International Journal for Parasitology: Drugs and Drug ResistanceAuthor(s): Sarah A. Habibi, Micah Callanan, Sean G. ForresterAbstractNematode cys-loop ligand-gated ion channels (LGICs) have been shown to be attractive targets for the development of novel anti-parasitic drugs. The ACC-1 family of receptors are a unique group of acetylcholine-gated chloride channels present only in invertebrates, and sequence analysis suggests that they contain a novel binding site for acetylcholine. We have isolated a novel member of this family, Hco-ACC-2, from the parasitic nema...
Source: International Journal for Parasitology: Drugs and Drug Resistance - October 4, 2018 Category: Parasitology Source Type: research

UDP-glycosyltransferase family in Haemonchus contortus: Phylogenetic analysis, constitutive expression, sex-differences and resistance-related differences
Publication date: Available online 26 September 2018Source: International Journal for Parasitology: Drugs and Drug ResistanceAuthor(s): Petra Matoušková, Lenka Lecová, Roz Laing, Diana Dimunová, Heiko Vogel, Lucie Raisová Stuchlíková, Linh Thuy Nguyen, Pavlína Kellerová, Ivan Vokřál, Jiří Lamka, Barbora Szotáková, Marián Várady, Lenka SkálováAbstractUDP-glycosyltransferases (UGT), catalysing conjugation of UDP-activated sugar donors to small lipophilic chemicals, are widespread in living organisms from bacteria to fungi, plant, or animals. The progress of genome sequencing has enabled an assessment of th...
Source: International Journal for Parasitology: Drugs and Drug Resistance - October 4, 2018 Category: Parasitology Source Type: research

Challenges in drug discovery targeting TriTryp diseases with an emphasis on leishmaniasis
Publication date: Available online 28 September 2018Source: International Journal for Parasitology: Drugs and Drug ResistanceAuthor(s): Laura M. Alcântara, ThalitaC.S. Ferreira, Fernanda R. Gadelha, Danilo C. MiguelAbstractTritryps diseases are devastating parasitic neglected infections caused by Leishmania spp., Trypanosoma cruzi and Trypanosoma brucei subspecies. Together, these parasites affect more than 30 million people worldwide and cause high mortality and morbidity. Leishmaniasis comprises a complex group of diseases with clinical manifestation ranging from cutaneous lesions to systemic visceral damage. Antimonial...
Source: International Journal for Parasitology: Drugs and Drug Resistance - October 4, 2018 Category: Parasitology Source Type: research

Structure-activity profiling of alkaloid natural product pharmacophores against a Schistosoma serotonin receptor
Publication date: Available online 28 September 2018Source: International Journal for Parasitology: Drugs and Drug ResistanceAuthor(s): Jonathan S. Marchant, Wayne W. Harding, John D. ChanAbstractSerotonin (5-HT) is an important regulator of numerous aspects of flatworm biology, ranging from neuromuscular function to sexual maturation and egg laying. In the parasitic blood fluke Schistosoma mansoni, 5-HT targets several G-protein coupled receptors (GPCRs), one of which has been demonstrated to couple to cAMP and regulate parasite movement. This receptor, Sm.5HTRL, has been successfully co-expressed in mammalian cells along...
Source: International Journal for Parasitology: Drugs and Drug Resistance - October 4, 2018 Category: Parasitology Source Type: research