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Antiparasitic drugs

Danielle Oliveira Dos Anjos, Eliomara Sousa Sobral Alves, Vinicius Tomaz Gonçalves, Sheila Suarez Fontes, Mateus Lima Nogueira, Ana Márcia Suarez-Fontes, João Batista Neves da Costa, Fabricio Rios-Santos, Marcos André Vannier-Santos
Natural products comprise valuable sources for new antiparasitic drugs. Here we tested the effects of a novel β-lapachone derivative on Trypanosoma cruzi parasite survival and proliferation and used microscopy and cytometry techniques to approach the mechanism(s) underlying parasite death. The selectivity index determination indicate that the compound trypanocidal activity was over ten-fold more cytotoxic to epimastigotes than to macrophages or splenocytes. Scanning electron microscopy analysis revealed that the R72 β-lapachone derivative affected the T...
October 12, 2016: International Journal for Parasitology, Drugs and Drug Resistance
Juan Guillermo Cárcamo, Marcelo N Aguilar, Constanza F Carreño, Tamara Vera, Luis Arias-Darraz, Jaime E Figueroa, Alex P Romero, Marco Alvarez, Alejandro J Yañez
Rainbow trout (Oncorhynchus mykiss) subjected to three consecutive, alternating treatments with emamectin benzoate (EMB) and deltamethrin (DM) during outbreaks of Caligus rogercresseyi in a farm located in southern Chile (Hornopiren, Chiloé), were studied to determine the effects of these treatments on the protein and enzymatic activity levels of cytochrome P450 1A (CYP1A), flavin-containing monooxygenase (FMO) and glutathione S-transferase (GST) in different tissues. Consecutive and alternating EMB/DM treatments resulted in a 10-fold increase and 3-fold decrease of CYP1A protein levels in the intestine and gills, respectively...
October 17, 2016: Comparative Biochemistry and Physiology. Toxicology & Pharmacology: CBP
Suprabhat Mukherjee, Niladri Mukherjee, Prajna Gayen, Priya Roy, Santi P Sinha Babu
Human diseases caused by the infectious parasites have been one of the major problems throughout the evolutionary journey. Protozoan and metazoan parasitic infections result in a large number of deaths, disabilities and socio-economic loss worldwide to date. Despite our best efforts of developing suitable antiparasitics, these infections take a massive toll on human health. The prevalence of emerging resistance to the existing drugs, lack of efficacy and toxic side effects came out as added complications. Being enlisted under 'neglected' category, serious diseases like leishmaniases, filariases, trypanosomiases etc...
October 4, 2016: Current Drug Metabolism
Heber Silva-Díaz, Lorena Flores-Esqueche, Dunalia Llatas-Cancino, Génesis Guevara Vásquez, Teresa Silva-García
OBJECTIVE: To describe the frequency and antiparasitic in vitro susceptibility of Blastocystis hominis in patients admitted to theHospital Regional Lambayeque, Peru. MATERIAL AND METHODS: A cross-sectional study was conducted from January to August 2015 at 313 patients of all ages. B. hominis detection was performed on serial fecal samples by direct microscopic examination and microculture in modified Locke solution. The in vitro susceptibility testing against the drug metronidazole, nitazoxanide, trimethoprim-sulfamethoxazole and erythromycin was performed in 24 strains of B...
July 2016: Revista de Gastroenterología del Perú: órgano Oficial de la Sociedad de Gastroenterología del Perú
Jeannine Hess, Malay Patra, Loganathan Rangasamy, Sandro Konatschnig, Olivier Blacque, Abdul Jabbar, Patrick Mac, Erik M Jorgensen, Robin B Gasser, Gilles Gasser
The discovery of novel drugs against animal parasites is in high demand due to drug-resistance problems encountered around the world. Herein, the synthesis and characterization of 27 organic and organometallic derivatives of the recently launched nematocidal drug monepantel (Zolvix(®) ) are described. The compounds were isolated as racemates and were characterized by (1) H, (13) C, and (19) F NMR spectroscopy, mass spectrometry, and IR spectroscopy, and their purity was verified by microanalysis. The molecular structures of nine compounds were confirmed by X-ray crystallography...
October 5, 2016: Chemistry: a European Journal
J N Vieira, F S Maia, G F Ferreira, J F Mendes, C L Gonçalves, M M Villela, D I B Pereira, P S Nascente
The fast anthelmintic resistance development has shown a limited efficiency in the control of animal's endoparasitosis and has promoted research using alternative control methods. The use of chemicals in animal anthelmintic treatment, in association with nematophagous fungi used for biological control, is a strategy that has proven to be effective in reducing the nematode population density in farm animals. This study aims to verify the in vitro susceptibility of the nematophagous fungi Arthrobotrys oligospora, Duddingtonia flagrans and Paecilomyces lilacinus against the antiparasitic drugs albendazole, thiabendazole, ivermectin, levamisole and closantel by using the Minimum Inhibitory Concentration (MIC)...
October 3, 2016: Brazilian Journal of Biology, Revista Brasleira de Biologia
Swetalina Pradhan, Bhushan Madke, Poonam Kabra, Adarsh Lata Singh
Antibiotics (antibacterial, antiviral, and antiparasitic) are class of drugs which result in either killing or inhibiting growth and multiplication of infectious organisms. Antibiotics are commonly prescribed by all specialties for treatment of infections. However, antibiotics have hitherto immunomodulatory and anti-inflammatory properties and can be exploited for various noninfectious dermatoses. Dermatologists routinely prescribe antibiotics in treatment of various noninfectious disorders. This study will review anti-inflammatory and immunomodulatory effects of antibiotics and their use in dermatology...
September 2016: Indian Journal of Dermatology
Diana F Florescu, Uriel Sandkovsky
Diarrhea is a common complication in solid organ transplant (SOT) recipients and may be attributed to immunosuppressive drugs or infectious organisms such as bacteria, viruses or parasites. Cryptosporidium usually causes self-limited diarrhea in immunocompetent hosts. Although it is estimated that cryptosporidium is involved in about 12% of cases of infectious diarrhea in developing countries and causes approximately 748000 cases each year in the United States, it is still an under recognized and important cause of infectious diarrhea in SOT recipients...
September 24, 2016: World Journal of Transplantation
Sarah Crunkhorn
No abstract text is available yet for this article.
September 29, 2016: Nature Reviews. Drug Discovery
José Maurício Dos Santos Filho, Diogo Manoel Alves de Queiroz E Silva, Taís Soares Macedo, Helena Mariana Pitangueira Teixeira, Diogo Rodrigo Magalhaes Moreira, Soura Challal, Jean-Luc Wolfender, Emerson Ferreira Queiroz, Milena Botelho Pereira Soares
Malaria, caused by several Plasmodium species, is the major life-threatening parasitic infection worldwide. Due to the parasite resistance to quinoline based drugs, the search for antimalarial agents is necessary. Here, we report the structural design, synthesis and antiparasitic evaluation of two novel series of 1,2,4-oxadiazoles in conjugation to N-acylhydrazones, both groups recognized as privileged structures, as well as the studies on the antimalarial activity of 16 previous described analogues. By varying substituents attached to the phenyl ring, it was possible to retain, enhance or increase the antiparasitic activity in comparison to the nonsubstituted derivatives...
September 9, 2016: Bioorganic & Medicinal Chemistry
Emiliano Felici, Cristian Casado, Chien C Wang, Julio Raba, María R Gomez
Antiparasitic drugs derived from macrocyclic lactones are widely used in livestock activities around the world. An increasing concern for local authorities is the environmental pollution as a consequence of veterinary drugs widely used in rural areas. The purpose of environmental analysis is to monitor low levels of pollutant analytes in a large number of samples. Also, due to the lipophilic characteristic of these lactones, long chain solvents are usually required for performing sample treatment before and during the analysis...
September 20, 2016: Electrophoresis
Medhat Ali, Marwa Abou Eldahab, Hoda Anwer Mansour, Ahmed Nigm
Schistosoma mansoni is one of the parasites causing schistosomiasis, a disease which threatens millions of people all over the world. Traditional chemical drugs are not fully effective against schistosomaisis due to the evolving drug resistant worm strains, so exploring new remedies derived from natural products is a good way to fight schistosomiasis. In the present investigation two natural products, Nigella sativa oil and Chroococcus turgidus extract were used separately or in a combination to explore their effect on S...
September 2016: Acta Biologica Hungarica
Mark R Gillrie, Bernard Renaux, Eleanor Russell-Goldman, Marion Avril, Andrew J Brazier, Koichiro Mihara, Enrico Di Cera, Danny A Milner, Morley D Hollenberg, Joseph D Smith, May Ho
UNLABELLED: Plasmodium falciparum malaria remains one of the most deadly infections worldwide. The pathogenesis of the infection results from the sequestration of infected erythrocytes (IRBC) in vital organs, including the brain, with resulting impairment of blood flow, hypoxia, and lactic acidosis. Sequestration occurs through the adhesion of IRBC to host receptors on microvascular endothelium by Plasmodium falciparum erythrocyte membrane protein 1 (PfEMP1), a large family of variant surface antigens, each with up to seven extracellular domains that can bind to multiple host receptors...
2016: MBio
Alejandro Vallejo, Begoña Monge-Maillo, Carolina Gutiérrez, Francesca F Norman, Rogelio López-Vélez, José A Pérez-Molina
Symptomatic chronic Chagas disease affects up to 40% of patients infected with Trypanosoma cruzi. The lack of reliable early markers of cure after therapy hinders disease management and clinical trials with new drugs. We performed a study with 18 months of follow-up to compare changes in immune parameters and T. cruzi-specific immune responses as surrogate markers of response to therapy between patients treated with benznidazole and untreated patients. This was a pilot, open-label, randomised clinical trial of treatment with benznidazole versus no treatment in patients with indeterminate chronic T...
September 9, 2016: Acta Tropica
Juliana Ide Aoki, Adriano Cappellazzo Coelho, Sandra Marcia Muxel, Ricardo Andrade Zampieri, Eduardo Milton Ramos Sanchez, Audun Helge Nerland, Lucile Maria Floeter-Winter, Paulo Cesar Cotrim
BACKGROUND: Tubercidin (TUB) is a toxic adenosine analog with potential antiparasitic activity against Leishmania, with mechanism of action and resistance that are not completely understood. For understanding the mechanisms of action and identifying the potential metabolic pathways affected by this drug, we employed in this study an overexpression/selection approach using TUB for the identification of potential targets, as well as, drug resistance genes in L. major. Although, TUB is toxic to the mammalian host, these findings can provide evidences for a rational drug design based on purine pathway against leishmaniasis...
September 2016: PLoS Neglected Tropical Diseases
Fatemeh Nouri, Saeid R Nourollahi-Fard, Hamid R Foroodi, Hamid Sharifi
Because of developing resistance to the existing anthelmintic drugs, there is a need for new anthelmintic agents. Tobacco plant has alkaloid materials that have antiparasitic effect. We investigated the in vitro anthelminthic effect of aqueous and alcoholic extract of Tobacco (Nicotiana tabacum) against M. marshalli. For investigating this effect, we prepared three dilutions of aqueous and alcoholic extract of Tobacco (25, 50 and 75 mg/ml). The worms exposed to extracts for 10 h at 25-30 °C. The buffer PBS used as negative control and 50 mg/ml dilution of Levamisole used as standard reference...
September 2016: Journal of Parasitic Diseases: Official Organ of the Indian Society for Parasitology
Reza Zolfaghari Emameh, Harlan R Barker, Leo Syrjänen, Linda Urbański, Claudiu T Supuran, Seppo Parkkila
Carbonic anhydrases (CAs) are metalloenzymes, and classified into the evolutionarily distinct α, β, γ, δ, ζ, and η classes. α-CAs are present in many living organisms. β- and γ-CAs are expressed in most prokaryotes and eukaryotes, except for vertebrates. δ- and ζ-CAs are present in phytoplanktons, and η-CAs have been found in Plasmodium spp. Since the identification of α- and β-CAs in Caenorhabditis elegans, the nematode CAs have been considered as an emerging target in research focused on antiparasitic CA inhibitors...
August 25, 2016: Journal of Enzyme Inhibition and Medicinal Chemistry
Carlos A Méndez-Cuesta, Miguel Ángel Herrera-Rueda, Sergio Hidalgo-Figueroa, Hugo Tlahuext, Rosa Moo-Puc, Juan Bautista Chale-Dzul, Manuel Chan-Bacab, Benjamín Otto Ortega-Morales, Emanuel Hernández-Núñez, Oscar Méndez-Lucio, José L Medina-Franco, Gabriel Navarrete-Vazquez
BACKGROUND: Propamidine, an antiseptic aromatic diamidine is a toxic compound with potential use as antiprotozoal drug. On the other hand, benzimidazole derivatives have shown excellent antiparasitic effects. We designed hybrid molecules between propamidine and benzimidazole in order to retain the antiprotozoal action, but decreasing the toxic effect of the molecule. Objetive: Design and prepare 12 hybrids from propamidine and benzimidazole for testing their antiparasitic effect over three protozoa: Giardia intestinalis, Trichomonas vaginalis and Leishmania Mexicana, as well as conduct several in silico simulations such as toxicological profile, molecular docking and molecular dynamics in order to understand their potential mode of action...
August 11, 2016: Medicinal Chemistry
Ana L Valenciano, Aaron C Ramsey, Webster L Santos, Zachary B Mackey
Human African trypanosomiasis (HAT) is a lethal, vector-borne disease caused by the parasite Trypanosoma brucei. Therapeutic strategies for this neglected tropical disease suffer from disadvantages such as toxicity, high cost, and emerging resistance. Therefore, new drugs with novel modes of action are needed. We screened cultured T. brucei against a focused kinase inhibitor library to identify promising bioactive compounds. Among the ten hits identified from the phenotypic screen, AZ960 emerged as the most promising compound with potent antiparasitic activity (IC50=120nM) and was shown to be a selective inhibitor of an essential gene product, T...
October 1, 2016: Bioorganic & Medicinal Chemistry
(no author information available yet)
This report represents the conclusions of a Joint FAO/WHO Expert Committee convened to evaluate the safety of residues of certain veterinary drugs in food and to recommend maximum levels for such residues in food. The first part of the report considers general principles regarding the evaluation of residues of veterinary drugs within the terms of reference of the Joint FAO/WHO Expert Committee on Food Additives (JECFA), including MRLs for generic fish species, acute reference doses (ARfDs) for veterinary drugs, an approach for dietary exposure assessment of compounds used for multiple purposes (i...
2016: World Health Organization Technical Report Series
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