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Jack Carson, Charlotte M Thomas, Aaron McGinty, Gustavo Takata, David J Timson
Schistosoma mansoni, like other trematodes, expresses a number of unusual calcium binding proteins which consist of an EF-hand domain joined to a dynein light chain-like (DLC-like) domain by a flexible linker. These proteins have been implicated in host immune responses and drug binding. Three members of this protein family from S. mansoni (SmTAL1, SmTAL2 and SmTAL3) have been well characterised biochemically. Here we characterise the remaining family members from this species (SmTAL4-13). All of these proteins form homodimers and all except SmTAL5 bind to calcium and manganese ions...
February 14, 2018: Molecular and Biochemical Parasitology
Yanyan Liu, Tianzi Wang, Wenya Ding, Chunliu Dong, Xiaoting Wang, Jianqing Chen, Yanhua Li
The aim of the present investigation was to enhance the solubility, dissolution, and oral bioavailability of praziquantel (PZQ), a poorly water-soluble BCS II drug (Biopharmaceutical Classification System), using a solid dispersion (SD) technique involving hydrophilic copolymers. The SD formulations were prepared by a solvent evaporation method with PZQ and PEG 4000 (polyethylene glycol 4000), PEG 6000, or P 188 polymers at various weight ratios or a combination of PEG 4000/P 188. The optimized SD formulation, which had the highest solubility in distilled water, was further characterized by its surface morphology, crystallinity, and dissolution in 0...
February 15, 2018: Drug Delivery and Translational Research
Cunchun Dai, Shaoqi Qu, Ruili Zhang, Li Zhao, Yuwen Li, Jiajia Zhu, Chunmei Wang, Hui Guo, Zhihui Hao
The objective of this study was to prepare a new compound fenbendazole tablet containing 29.7 % fenbendazole, 1.50 % praziquantel and 0.059 % ivermectin for oral administration. The tablets were successfully prepared using mannitol as filler agent, polyvinyl polypyrrolidone as disintegrant, 5 % povidone (PVAK30) as a binder agent and magnesium stearate as lubricant. The appearance, hardness, fragility, time limit of disintegration and fenbendazole dissolution at 45 min all met the technical standards of the Ministry of Agriculture for the People's Republic of China...
February 1, 2018: Die Pharmazie
Tim A Day, Michael J Kimber
Chan et al. recently demonstrated that the antischistosomal drug praziquantel has a potent and specific interaction with human 5-HT 2B receptors, and that the drug also elicits contraction of mouse mesenteric vasculature apparently mediated by the same receptor subtype We consider what this might mean about the drug's molecular therapeutic targets in both the worm and the host.
February 9, 2018: Trends in Parasitology
Natan R G Assis, Anderson J Caires, Bárbara C Figueiredo, Suellen B Morais, Fábio S Mambelli, Fábio V Marinho, Luís O Ladeira, Sergio C Oliveira
Schistosomiasis is an important parasitic disease affecting >207 million people in 76 countries around the world and causing approximately 250,000 deaths per year. At present, the main strategy adopted for the control of schistosomiasis is the use of safe chemotherapy, such as praziquantel. However, the high rates of reinfection after treatment restrict the use of this treatment approach and assume the need for other forms of control such as vaccination. Sm29 is a protein that is localized in the Schistosoma mansoni tegument of adult worms and schistosomula and is considered a powerful vaccine candidate...
February 8, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
A Raffetin, F Bruneel, C Roussel, M Thellier, P Buffet, E Caumes, S Jauréguiberry
INTRODUCTION: Artesunate and other artemisinin derivatives are used in various infectious and non-infectious diseases. We aimed to analyze available data on artesunate and artemisinin derivatives activity in humans and their potential clinical benefits in non-malarial indications. MATERIAL AND METHODS: Literature review performed on PubMed and the Cochrane Library databases using the PRISMA method. We analyzed studies published in English from January 2008 to August 2017 using the same indicators of drug efficacy...
February 5, 2018: Médecine et Maladies Infectieuses
Fatma M Dardir, Aya S Mohamed, Mostafa R Abukhadra, Ezzat A Ahmed, Mamdouh F Soliman
The aim of this paper is to characterize and evaluate newly discovered bentonite deposits in Egypt for pharmaceutical and cosmetic applications as well as its suitability as carrier for Praziquantel drug. The study was performed for the raw bentonite sample, purified bentonite sample and alkali activated purified bentonite sample. The raw bentonite sample composed mainly of montmorillonite contaminated by little amounts of quartz and calcite, while the purified sample composed of montmorillonite without detected mineral impurities and matches the mineralogical properties of Wyoming bentonite as an international standard...
January 29, 2018: European Journal of Pharmaceutical Sciences
Jana Kovač, Gordana Panic, Anna Neodo, Isabel Meister, Jean T Coulibaly, Jessica D Schulz, Jennifer Keiser
Pharmacokinetic (PK) studies with paediatric populations are increasing in importance for drug development. However, conventional PK sampling methods are characterised by invasiveness and low patient adherence, unsuitable for use with sensitive population, such as children. Mitra™ is a novel volumetric absorptive micro-sampling device, which offers an alternative to the dried blood spotting (DBS) technique, a current popular sampling technique within PK studies. We tested Mitra™ for the first time in the framework of a randomised controlled trial in rural Côte d'Ivoire...
January 26, 2018: Journal of Pharmaceutical and Biomedical Analysis
Debora Zanolla, Beatrice Perissutti, Nadia Passerini, Michele R Chierotti, Dritan Hasa, Dario Voinovich, Lara Gigli, Nicola Demitri, Silvano Geremia, Jennifer Keiser, Paolo Cerreia Vioglio, Beatrice Albertini
Praziquantel is the only available drug to treat Schistosomiasis. However, its utilization is limited by many drawbacks, including the high therapeutic dose needed, resulting in large tablets and capsules difficult to be swallowed, especially from pediatric patients. In this study, an alternative option to overcome these disadvantages is proposed: to switch to a novel crystalline polymorph of racemic compound praziquantel. The preparation of the crystalline polymorph was realized via a neat grinding process in a vibrational mill...
January 30, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Shu-Hua Xiao, Jun Sun, Ming-Gang Chen
BACKGROUND: Chemotherapy for schistosomiasis has been around for 100 years. During the past century, great efforts have been made to develop new antischistosomal drugs from antimonials to nonantimonials, and some of these have been used extensively in clinical treatment. With the exception of a few drugs, such as oxamniquine and metrifonate, most of the antischistosomals developed in the pre-praziquantel period have variable limitations with respect to safety and efficacy. Although oxamniquine and metrifonate have been used for schistosomiasis control, they are only effective against Schistosoma mansoni and S...
February 7, 2018: Infectious Diseases of Poverty
Kumar Saurabh, Shilpi Ranjan
PURPOSE: To describe the clinical and sociodemographic profile of fasciolopsiasis in children. MATERIALS AND METHODS: A chart review of 56 children presenting with the passage of adult Fasciolopsis buski per stool from February 2015 to January 2016 was done for their clinical profile and risk factors for acquiring fasciolopsiasis in the Paediatric Unit of a medical college of Northern India. RESULTS: The mean age of presentation was 8.2 years (2-14 years age group)...
October 2017: Indian Journal of Medical Microbiology
Soledad Colombe, Myung Hee Lee, Peter J Masikini, Lisette van Lieshout, Claudia J de Dood, Pytsje T Hoekstra, Paul L A M Corstjens, Julius Mngara, Govert J van Dam, Jennifer A Downs
It has been postulated that impaired host immunity due to HIV infection reduces parasite egg excretion. Schistosoma/HIV interactions have also been shown to differ by sex. We hypothesized that egg excretion would vary based on both HIV status and sex. We examined data from more than 1,700 participants in eight studies conducted in northwest Tanzania between 2010 and 2016. Schistosoma infection was defined by circulating anodic antigen (CAA) serum levels ≥ 30 pg/mL and/or egg positivity in either stool by Kato Katz method or urine by filtration...
February 5, 2018: American Journal of Tropical Medicine and Hygiene
Jennifer F Friedman, Remigio M Olveda, Mark H Mirochnick, Amaya L Bustinduy, Alison M Elliott
In 2014, an estimated 40 million women of reproductive age were infected with Schistosoma haematobium, S. japonicum and/or S. mansoni. In both 2003 and 2006, the World Health Organization (WHO) recommended that all schistosome-infected pregnant and breastfeeding women be offered treatment, with praziquantel, either individually or during treatment campaigns. In 2006, WHO also stated the need for randomized controlled trials to assess the safety and efficacy of such treatment. Some countries have yet to follow the recommendation on treatment and many programme managers and pregnant women in other countries remain reluctant to follow the recommended approach...
January 1, 2018: Bulletin of the World Health Organization
Maria João Gouveia, Paul J Brindley, Fátima Gärtner, José M Correia da Costa, Nuno Vale
Schistosomiasis is a major neglected tropical disease. Control of schistosomiasis currently relies on a single drug, praziquantel, and despite its efficacy against the all schistosome species that parasitize humans, it displays some problematic drawbacks and alone is ineffective in counteracting adverse pathologies associated with infection. Moreover, due to the development of the potential emergence of PZQ-resistant strains, the search for additional or alternative antischistosomal drugs have become a public health priority...
February 5, 2018: Pharmaceuticals
Yves-Nathan T Tian-Bi, Mamadou Ouattara, Stefanie Knopp, Jean T Coulibaly, Eveline Hürlimann, Bonnie Webster, Fiona Allan, David Rollinson, Aboulaye Meïté, Nana R Diakité, Cyrille K Konan, Eliézer K N'Goran, Jürg Utzinger
BACKGROUND: To achieve a world free of schistosomiasis, the objective is to scale up control and elimination efforts in all endemic countries. Where interruption of transmission is considered feasible, countries are encouraged to implement a comprehensive intervention package, including preventive chemotherapy, information, education and communication (IEC), water, sanitation and hygiene (WASH), and snail control. In northern and central Côte d'Ivoire, transmission of Schistosoma haematobium is seasonal and elimination might be achieved...
January 29, 2018: BMC Public Health
Wassana Jamnongkan, Malinee Thanee, Puangrat Yongvanit, Watcharin Loilome, Raynoo Thanan, Phongsaran Kimawaha, Tidarat Boonmars, Runglawan Silakit, Nisana Namwat, Anchalee Techasen
Cholangiocarcinoma (CCA) caused by infection of the liver fluke Opisthorchis viverrini, (Ov) is the major public health problem in northeast Thailand. Following Ov infection the subsequent molecular changes can be associated by reactive oxygen species (ROS) induced chronic inflammation, advanced periductal fibrosis, and cholangiocarcinogenesis. Notably, resistance to an activation of cell death in prolonged oxidative stress conditions can occur but some damaged/mutated cells could survive and enable clonal expansion...
2018: PeerJ
Luana Maria Mariz Gomes da Silva, Jamerson Ferreira de Oliveira, Willams Leal Silva, Anekecia Lauro da Silva, Antônio Sérgio Alves de Almeida Junior, Victor Hugo Barbosa Dos Santos, Luiz Carlos Alves, Fábio André Brayner Dos Santos, Vlaudia Maria Assis Costa, André de Lima Aires, Maria do Carmo Alves de Lima, Monica Camelo Pessoa de Azevedo Albuquerque
Schistosomiasis is considered a serious public health problem in 78 countries and territories located in Africa, Asia and America and it is estimated in more than 249 million people infected by any of the species of Schistosoma. The exclusive use of praziquantel (PZQ), effective drug against all species of Schistosoma, has been the basis of the development of a possible resistance against the strains of this parasite. In addition, PZQ is not effective against young forms of worms. Thus, there is a need for the development of new drugs with schistosomicidal activity...
January 20, 2018: Chemico-biological Interactions
H E van Munster, L J F Janssen, G J H Bastiaens
An 8-year-old, Senegalese boy presented with a history of painless macroscopic haematuria. The diagnosis schistosomiasis was made, based on the urine sediment that revealed eggs from the trematode parasite Schistosoma haematobium. The patient was treated with praziquantel and made a full recovery.
2018: Nederlands Tijdschrift Voor Geneeskunde
E Zuskova, V Piackova, J Machova, L Chupani, C Steinbach, A Stara, J Velisek
This study evaluated efficacy and toxicity of the pyrazinoisoquinoline anthelmintic praziquantel (PZQ) in barbel infected with metacercariae of Diplostomum spathaceum and adult Pomphorhynchus laevis, and assessed antioxidant biomarkers and the lipid peroxidation response in juvenile barbel post-treatment. The estimated 96-hr LC50 of PZQ was 28.6 mg/L. For evaluation of efficacy, barbel naturally infected with D. spathaceum were exposed to a 10 and 20 mg/L PZQ 4-day bath treatment. Both concentrations were 100% effective against D...
January 19, 2018: Journal of Fish Diseases
Steffen Hahnel, Nic Wheeler, Zhigang Lu, Arporn Wangwiwatsin, Paul McVeigh, Aaron Maule, Matthew Berriman, Timothy Day, Paula Ribeiro, Christoph G Grevelding
Schistosomes are blood-dwelling trematodes with global impact on human and animal health. Because medical treatment is currently based on a single drug, praziquantel, there is urgent need for the development of alternative control strategies. The Schistosoma mansoni genome project provides a platform to study and connect the genetic repertoire of schistosomes to specific biological functions essential for successful parasitism. G protein-coupled receptors (GPCRs) form the largest superfamily of transmembrane receptors throughout the Eumetazoan phyla, including platyhelminths...
January 2018: PLoS Pathogens
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