Antiechinococcal assessment of atovaquone —an in silico and in vitro analysis

AbstractCystic echinococcosis (CE), a hydatid disease, caused by larval form of dog tapewormEchiconoccus granulosus, is responsible for considerable human morbidity and mortality. The currently available drugs have to be applied in high doses for prolonged periods for treatment of CE, and have several side effects. Atovaquone, a naphthoquinone, has previously been shown to possess a very promising antiparasitic potential against malaria, toxoplasmosis, babesiasis, etc. by inhibiting parasite ’s electron transport chain, cytochrome bc1 complex. Thus, the present study was aimed to investigate the antiechinococcal potency of atovaquone. The mode of binding of atovaquone to cytochrome bc1 complex ofE. granulosus was also predicted using in silico approach. The 3D model of cytbc1 complex ofE. granulosus was prepared using I-Tasser server and was docked with atovaquone. The docking results predicted the binding of atovaquone to Thr-371 amino acid of Ubiquinol region of cyt b. The protoscolicidal efficacy of atovaquone was further investigated by in vitro experiments. Dose-dependent death of protoscolesces was observed within a few time intervals after treatment with atovaquone, thereby indicating its potential in treatment of CE. The 100% protoscolicidal activity of atovaquone was achieved at a concentration of 20  μg/mL within 60 h of treatment. It is probably the first study to investigate the effect of atovaquone on protoscolesces ofE. granulosus. The results...
Source: Comparative Clinical Pathology - Category: Pathology Source Type: research

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We reported three cases of possible parasite resistance to artemether-lumefantrine therapy. All subjects had complete parasite clearance when treated with other antimalarial drugs. This observation necessitates the urgent need to re-evaluate artemether-lumefantrine medication in Nigeria since it is one of the most commonly used ACT drug.
Source: Revista da Sociedade Brasileira de Medicina Tropical - Category: Tropical Medicine Source Type: research
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 aga...
Source: International Journal for Parasitology: Drugs and Drug Resistance - Category: Parasitology Source Type: research
In conclusion, African medicinal plants are a potential source of lead compounds for drug discovery and the production of phytopharmaceuticals in the management of devastating parasitic diseases. There is a need to apply traditional medicine knowledge in clinical applications via value addition.
Source: Journal of Herbal Medicine - Category: Complementary Medicine Source Type: research
Publication date: August 2018Source: International Journal for Parasitology: Drugs and Drug Resistance, Volume 8, Issue 2Author(s): Reto Rufener, Dominic Ritler, Jana Zielinski, Luca Dick, Emerson Teixeira da Silva, Adriele da Silva Araujo, Deborah Elisabeth Joekel, David Czock, Christine Goepfert, Adriana Marques Moraes, Marcus Vinicius Nora de Souza, Joachim Müller, Meike Mevissen, Andrew Hemphill, Britta Lundström-StadelmannAbstractThe cestode E. multilocularis causes the disease alveolar echinococcosis (AE) in humans. The continuously proliferating metacestode (larval stage) of the parasite infects mostly the...
Source: International Journal for Parasitology: Drugs and Drug Resistance - Category: Parasitology Source Type: research
In conclusion, African medicinal plants are a potential source of lead compounds for drug discovery and the production of phytopharmaceuticals in the management of devastating parasitic diseases. There is a need to apply traditional medicine knowledge in clinical applications via value addition.
Source: Journal of Herbal Medicine - Category: Complementary Medicine Source Type: research
Publication date: August 2018Source: International Journal for Parasitology: Drugs and Drug Resistance, Volume 8, Issue 2Author(s): Reto Rufener, Dominic Ritler, Jana Zielinski, Luca Dick, Emerson Teixeira da Silva, Adriele da Silva Araujo, Deborah Elisabeth Joekel, David Czock, Christine Goepfert, Adriana Marques Moraes, Marcus Vinicius Nora de Souza, Joachim Müller, Meike Mevissen, Andrew Hemphill, Britta Lundström-StadelmannAbstractThe cestode E. multilocularis causes the disease alveolar echinococcosis (AE) in humans. The continuously proliferating metacestode (larval stage) of the parasite infects mostly the...
Source: International Journal for Parasitology: Drugs and Drug Resistance - Category: Parasitology Source Type: research
Little attention has been devoted to the role of HLA‐G gene and molecule on parasitic disorders, and the available studies have focused on malaria, African and American trypanosomiasis, leishmaniosis, toxoplasmosis and echinococcosis. After reporting a brief description regarding the role of the cells of innate and adaptive immune system against parasites, we reviewed the major features of the HLA‐G gene and molecule and the role of HLA‐G on the major cells of immune system. Increased levels of soluble HLA‐G (sHLA‐G) have been observed in patients presenting toxoplasmosis and in the active phase of echinococcosis...
Source: Tissue Antigens - Category: Allergy & Immunology Authors: Tags: REVIEW ARTICLE Source Type: research
In conclusion, African medicinal plants are a potential source of lead compounds for drug discovery and the production of phytopharmaceuticals in the management of devastating parasitic diseases. There is a need to apply traditional medicine knowledge in clinical applications via value addition.
Source: Journal of Herbal Medicine - Category: Complementary Medicine Source Type: research
This article reviews and summarises the imaging findings of some of the most important and frequent human parasitic diseases, including information about the parasite ’s life cycle, pathophysiology, clinical findings, diagnosis, and treatment. We include malaria, amoebiasis, toxoplasmosis, trypanosomiasis, leishmaniasis, echinococcosis, cysticercosis, clonorchiasis, schistosomiasis, fascioliasis, ascariasis, anisakiasis, dracunculiasis, and strongyloidiasis. Th e aim of this review is to help radiologists when dealing with these diseases or in cases where they are suspected.Teaching Points•Incidence of parasitic...
Source: Insights into Imaging - Category: Radiology Source Type: research
The metacestode (larval) stage of the tapeworm Echinococcus multilocularis causes alveolar echinococcosis (AE), a very severe and in many cases incurable disease. To date, benzimidazoles such as albendazole and mebendazole are the only approved chemotherapeutical treatment options. Benzimidazoles inhibit metacestode proliferation, but do not act parasiticidal. Thus, benzimidazoles have to be taken a lifelong, can cause adverse side effects such as hepatotoxicity, and are ineffective in some patients. We here describe a newly developed screening cascade for the evaluation of the in vitro efficacy of new compounds that inclu...
Source: PLoS Neglected Tropical Diseases - Category: Tropical Medicine Authors: Source Type: research
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