Macrocyclic lactone anthelmintic-induced leukocyte binding to Dirofilaria immitis microfilariae: Influence of the drug resistance status of the parasite
Publication date: Available online 26 April 2019Source: International Journal for Parasitology: Drugs and Drug ResistanceAuthor(s): Tessa Berrafato, Ruby Coates, Barbara J. Reaves, Daniel Kulke, Adrian J. WolstenholmeAbstractThe macrocyclic lactone anthelmintics are the only class of drug currently used to prevent heartworm disease. Their extremely high potency in vivo is not mirrored by their activity against Dirofilaria immitis larvae in vitro, leading to suggestions that they may require host immune functions to kill the parasites. We have previously shown that ivermectin stimulates the binding of canine peripheral bloo...
Source: International Journal for Parasitology: Drugs and Drug Resistance - April 27, 2019 Category: Parasitology Source Type: research

In vitro susceptibility of Plasmodium falciparum isolates from the China-Myanmar border area to artemisinins and correlation with K13 mutations
This study followed the dynamics of the K13 polymorphisms in P. falciparum parasites from the China-Myanmar border area obtained in 2007–2016, and their in vitro sensitivities to artesunate (AS) and dihydroartemisinin (DHA). The 50% effective concentration (EC5072h) values of 133 culture-adapted field isolates to AS and DHA, measured by the conventional 72 h SYBR Green I-based assay, varied significantly among the parasites from different years; all were significantly higher than that of the reference strain 3D7. Compared with parasites from 2007 to 2008, ring survival rates almost doubled in parasites obtained in late...
Source: International Journal for Parasitology: Drugs and Drug Resistance - April 10, 2019 Category: Parasitology Source Type: research

Aminoguanidines: New leads for treatment of Giardia duodenalis infection
In conclusion, a class of aminoguanidines, represented by robenidine, has shown antigiardial activity warranting further investigation.Graphical abstract (Source: International Journal for Parasitology: Drugs and Drug Resistance)
Source: International Journal for Parasitology: Drugs and Drug Resistance - April 10, 2019 Category: Parasitology Source Type: research

A high-throughput screen for the identification of compounds that inhibit nematode gene expression by targeting spliced leader trans-splicing
Publication date: Available online 5 April 2019Source: International Journal for Parasitology: Drugs and Drug ResistanceAuthor(s): George Cherian Pandarakalam, Michael Speake, Stuart McElroy, Ammar Alturkistani, Lucas Phillipe, Jonathan Pettitt, Berndt Müller, Bernadette ConnollyAbstractInfections with parasitic nematodes are among the most significant of the neglected tropical diseases affecting about a billion people living mainly in tropical regions with low economic activity.The most effective current strategy to control nematode infections involves large scale treatment programs with anthelmintic drugs. This strategy...
Source: International Journal for Parasitology: Drugs and Drug Resistance - April 7, 2019 Category: Parasitology Source Type: research

Bumped kinase inhibitor 1369 is effective against Cystoisospora suis in vivo and in vitro
Publication date: Available online 2 April 2019Source: International Journal for Parasitology: Drugs and Drug ResistanceAuthor(s): Aruna Shrestha, Kayode K. Ojo, Florian Koston, Bärbel Ruttkowski, Rama S.R. Vidadala, Carlie S. Dorr, Edelmar D. Navaluna, Grant R. Whitman, Kayleigh F. Barrett, Lynn K. Barrett, Matthew A. Hulverson, Ryan Choi, Samantha A. Michaels, Dustin J. Maly, Andrew Hemphill, Wesley C. Van Voorhis, Anja JoachimAbstractCystoisosporosis is a leading diarrheal disease in suckling piglets. With the confirmation of resistance against the only available drug toltrazuril, there is a substantial need for novel ...
Source: International Journal for Parasitology: Drugs and Drug Resistance - April 3, 2019 Category: Parasitology Source Type: research

Insights into Chagas treatment based on the potential of bacteriocin AS-48
Publication date: Available online 29 March 2019Source: International Journal for Parasitology: Drugs and Drug ResistanceAuthor(s): Rubén Martín-Escolano, Rubén Cebrián, Javier Martín-Escolano, Maria J. Rosales, Mercedes Maqueda, Manuel Sánchez-Moreno, Clotilde MarínAbstractChagas disease caused by the protozoan parasite Trypanosoma cruzi represents a significant public health problem in Latin America, affecting around 8 million cases worldwide. Nowadays is urgent the identification of new antichagasic agents as the only therapeutic options available, Nifurtimox and Benznidazole, are in use for>40 years, and present...
Source: International Journal for Parasitology: Drugs and Drug Resistance - March 30, 2019 Category: Parasitology Source Type: research

Resistance formation to nitro drugs in Giardia lamblia: No common markers identified by comparative proteomics
Publication date: Available online 15 March 2019Source: International Journal for Parasitology: Drugs and Drug ResistanceAuthor(s): Joachim Müller, Sophie Braga, Manfred Heller, Norbert MüllerAbstractIn order to elucidate the question whether resistance to nitro drugs in G. lamblia is due to common resistance markers, trophozoites of three resistant G. lamblia strains, namely C4, 1062ID10, and 713M3 were grown in the presence of the two nitro drugs metronidazole and nitazoxanide and compared to their corresponding wild-types WBC6, 106, and 713 by mass spectometry shotgun analysis of their proteomes. Depending on the stra...
Source: International Journal for Parasitology: Drugs and Drug Resistance - March 16, 2019 Category: Parasitology Source Type: research

High-resolution melt (HRM) analysis for detection of SNPs associated with pyrethroid resistance in the southern cattle fever tick, Rhipicephalus (Boophilus) microplus (Acari: Ixodidae)
This study highlights the existence of several mutations in the para-sodium channel gene in different combinations in field populations of R. microplus from Mexico.Graphical abstract (Source: International Journal for Parasitology: Drugs and Drug Resistance)
Source: International Journal for Parasitology: Drugs and Drug Resistance - March 13, 2019 Category: Parasitology Source Type: research

Novel benzoxaborole, nitroimidazole and aminopyrazoles with activity against experimental cutaneous leishmaniasis
ConclusionsThe lead compounds DNDI-0690, DNDI-1047 and DNDI-6148 showed excellent activity across a range of Leishmania species in vitro and against L. major in mice. These compounds offer novel potential drugs for the treatment of CL.Graphical abstract (Source: International Journal for Parasitology: Drugs and Drug Resistance)
Source: International Journal for Parasitology: Drugs and Drug Resistance - February 26, 2019 Category: Parasitology Source Type: research

Investigation of the pathways related to intrinsic miltefosine tolerance in Leishmania (Viannia) braziliensis clinical isolates reveals differences in drug uptake
Publication date: Available online 25 February 2019Source: International Journal for Parasitology: Drugs and Drug ResistanceAuthor(s): Caroline R. Espada, Rubens M. Magalhães, Mario C. Cruz, Paulo R. Machado, Albert Schriefer, Edgar M. Carvalho, Valentín Hornillos, João M. Alves, Angela K. Cruz, Adriano C. Coelho, Silvia R.B. UlianaAbstractIn Brazil, cutaneous leishmaniasis is caused predominantly by L. (V.) braziliensis. The few therapeutic drugs available exhibit several limitations, mainly related to drug toxicity and reduced efficacy in some regions. Miltefosine (MF), the only oral drug available for leishmaniasis t...
Source: International Journal for Parasitology: Drugs and Drug Resistance - February 25, 2019 Category: Parasitology Source Type: research

Plasmodium knowlesi exhibits distinct in vitro drug susceptibility profiles from those of Plasmodium falciparum
Publication date: Available online 22 February 2019Source: International Journal for Parasitology: Drugs and Drug ResistanceAuthor(s): Donelly A. van Schalkwyk, Benjamin Blasco, Rocio Davina Nuñez, Jonathan W.K. Liew, Amirah Amir, Yee L. Lau, Didier Leroy, Robert W. Moon, Colin J. SutherlandAbstractNew antimalarial agents are identified and developed after extensive testing on Plasmodium falciparum parasites that can be grown in vitro. These susceptibility studies are important to inform lead optimisation and support further drug development. Until recently, little was known about the susceptibility of non-falciparum spec...
Source: International Journal for Parasitology: Drugs and Drug Resistance - February 23, 2019 Category: Parasitology Source Type: research

Histone deacetylase enzymes as potential drug targets of Neglected Tropical Diseases caused by cestodes
This report provides the basis for further studies on cestode HDAC enzymes and for discovery of new HDAC inhibitors for the treatment of neglected diseases caused by cestode parasites.Graphical abstract (Source: International Journal for Parasitology: Drugs and Drug Resistance)
Source: International Journal for Parasitology: Drugs and Drug Resistance - February 23, 2019 Category: Parasitology Source Type: research

Development of unstable resistance to diminazene aceturate in Babesia bovis
In this study, we attempted to develop resistance in B. bovis in vitro to DA and clofazimine (CF, a novel antibabesial agent) using short- and long-term drug pressures. In the short term, we found that 6.7 ± 2 (0.54 ± 0.16 μM)-, 12.9 ± 8.6 (1.05 ± 0.7 μM)-, and 14 ± 5.9 (1.14 ± 0.48 μM)-fold increases in the half-maximal inhibitory concentration (IC50) of DA were demonstrated on B. bovis cultivated with 0.04 μM of DA pressure for 4, 8, and 12 days, respectively, as compared to that on parental culture (0.08 ± 0.0065 μM) before drug pressure was initiated. However, in B. bov...
Source: International Journal for Parasitology: Drugs and Drug Resistance - February 14, 2019 Category: Parasitology Source Type: research

Leveraging the medicines for Malaria Venture malaria and pathogen boxes to discover chemical inhibitors of East Coast fever
Publication date: Available online 25 January 2019Source: International Journal for Parasitology: Drugs and Drug ResistanceAuthor(s): James Nyagwange, Elias Awino, Edwin Tijhaar, Nicholas Svitek, Roger Pelle, Vishvanath NeneAbstractChemotherapy of East Coast fever, a lymphoproliferative cancer-like disease of cattle causing significant economic losses in Africa, is largely dependent on the use of buparvaquone, a drug that was developed in the late 1980's. The disease is caused by the tick-borne protozoan pathogen Theileira parva. Buparvaquone can be used prophylactically and it is also active against tropical theileriosis,...
Source: International Journal for Parasitology: Drugs and Drug Resistance - January 26, 2019 Category: Parasitology Source Type: research

The individual components of commercial isometamidium do not possess stronger trypanocidal activity than the mixture, nor bypass isometamidium resistance
Publication date: Available online 21 January 2019Source: International Journal for Parasitology: Drugs and Drug ResistanceAuthor(s): Anthonius A. Eze, John Igoli, Alexander I. Gray, Graham G. Skellern, Harry P. De KoningAbstractThe four components present in the trypanocidal treatment Samorin, the commercially available formulation of isometamidium, were separated and purified by column chromatography. These compounds as well as the Samorin mixture and the other phenanthridine trypanocide, homidium, were tested on Trypanosoma congolense and wild type, diamidine- and isometamidium-resistant Trypanosoma brucei brucei strain...
Source: International Journal for Parasitology: Drugs and Drug Resistance - January 22, 2019 Category: Parasitology Source Type: research