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Antiparasitic drugs

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https://www.readbyqxmd.com/read/29442007/development-and-analytical-characterization-of-a-new-antiparasitic-fenbendazole-compound-tablet-and-pharmacokinetic-investigations-after-its-oral-administration-to-dogs
#1
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
https://www.readbyqxmd.com/read/29435139/quantitative-high-throughput-phenotypic-screening-of-pediatric-cancer-cell-lines-identifies-multiple-opportunities-for-drug-repurposing
#2
Min Shen, Rosita Asawa, Ya-Qin Zhang, Elizabeth Cunningham, Hongmao Sun, Alexander Tropsha, William P Janzen, Eugene N Muratov, Stephen J Capuzzi, Sherif Farag, Ajit Jadhav, Julie Blatt, Anton Simeonov, Natalia J Martinez
Drug repurposing approaches have the potential advantage of facilitating rapid and cost-effective development of new therapies. Particularly, the repurposing of drugs with known safety profiles in children could bypass or streamline toxicity studies. We employed a phenotypic screening paradigm on a panel of well-characterized cell lines derived from pediatric solid tumors against a collection of ∼3,800 compounds spanning approved drugs and investigational agents. Specifically, we employed titration-based screening where compounds were tested at multiple concentrations for their effect on cell viability...
January 12, 2018: Oncotarget
https://www.readbyqxmd.com/read/29427703/safety-and-clinical-efficacy-of-tenvermectin-a-novel-antiparasitic-16-membered-macrocyclic-lactone-antibiotics
#3
Chenzhong Fei, Rufeng She, Guiyu Li, Lifang Zhang, Wushun Fan, Suhan Xia, Feiqun Xue
Tenvermectin (TVM) is a novel 16-membered macrocyclic lactone antibiotics, which contains component TVM A and TVM B. However there is not any report on safety and clinical efficacy of TVM for developing as a potential drug. In order to understand the part of safety and clinical efficacy of TVM, we conducted the acute toxicity test, the standard bacterial reverse mutation (Ames) test and the clinical deworming test. In the acute toxicity studies, TVM, TVM A and ivermectin (IVM) were administrated once by oral gavage to mice and rats...
February 7, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29415440/revisiting-the-therapeutic-potential-of-bothrops-jararaca-venom-screening-for-novel-activities-using-connectivity-mapping
#4
Carolina Alves Nicolau, Alyson Prorock, Yongde Bao, Ana Gisele da Costa Neves-Ferreira, Richard Hemmi Valente, Jay William Fox
Snake venoms are sources of molecules with proven and potential therapeutic applications. However, most activities assayed in venoms (or their components) are of hemorrhagic, hypotensive, edematogenic, neurotoxic or myotoxic natures. Thus, other relevant activities might remain unknown. Using functional genomics coupled to the connectivity map (C-map) approach, we undertook a wide range indirect search for biological activities within the venom of the South American pit viper Bothrops jararaca . For that effect, venom was incubated with human breast adenocarcinoma cell line (MCF7) followed by RNA extraction and gene expression analysis...
February 6, 2018: Toxins
https://www.readbyqxmd.com/read/29411605/investigation-of-agonist-recognition-and-channel-properties-in-a-flatworm-glutamate-gated-chloride-channel
#5
Daniel Callau-Vázquez, Stephan A Pless, Timothy Lynagh
Glutamate-gated chloride channels (GluCls) are neurotransmitter receptors that mediate crucial inhibitory signaling in invertebrate neuromuscular systems. Their role in invertebrate physiology and their absence from vertebrates make GluCls a prime target for antiparasitic drugs. GluCls from flatworm parasites are substantially different from and are much less understood than those from roundworm and insect parasites, hindering the development of potential therapeutics targeting GluCls in flatworm-related diseases such as schistosomiasis...
February 7, 2018: Biochemistry
https://www.readbyqxmd.com/read/29393084/clinical-course-and-outcome-of-childhood-acquired-platelet-dysfunction-with-eosinophilia
#6
Thirachit Chotsampancharoen, Pornpun Sripornsawan, Sarapee Duangchu, Edward McNeil
Acquired platelet dysfunction with eosinophilia (APDE) is a syndrome which manifests as a transient state of platelet dysfunction in the presence of eosinophilia. The aim of this work was to study the clinical course and outcomes of children diagnosed with APDE. The hospital records of children with APDE were retrospectively reviewed and a total of 69 children were included. The mean (standard deviation) age at diagnosis was 6.9 (3.1) years. All of the patients presented with ecchymoses on the extremities, body, and face...
January 11, 2018: Acta Haematologica
https://www.readbyqxmd.com/read/29392954/heparin-and-heparan-sulfate-binding-of-the-antiparasitic-drug-imidocarb-circular-dichroism-spectroscopy-isothermal-titration-calorimetry-and-computational-studies
#7
Ferenc Zsila, Tünde Juhász, Gergely Kohut, Tamás Beke-Somfai
This study is aimed to assess the binding interaction between the antiparasitic cationic drug imidocarb (IMD) and sulfated glycosaminoglycans (GAGs), the ubiquitious nonprotein macromolecules of living organisms. These complex, heterogeneous polyanions are the integral constituents of cell membranes and the extracellular matrix and display affinity toward basic compounds, the binding of which may affect their biological functions. Exciton-type circular dichroism (CD) spectroscopic features measured at low salt concentration verify the heparin and heparan sulfate binding of IMD, which occurs in a cooperative manner by association of several drug molecules to a disaccharide unit...
February 2, 2018: Journal of Physical Chemistry. B
https://www.readbyqxmd.com/read/29390009/chemical-composition-immunostimulatory-cytotoxic-and-antiparasitic-activities-of-the-essential-oil-from-brazilian-red-propolis
#8
Ângela Sena-Lopes, Francisco Silvestre Brilhante Bezerra, Raquel Nascimento das Neves, Rodrigo Barros de Pinho, Mara Thais de Oliveira Silva, Lucielli Savegnago, Tiago Collares, Fabiana Seixas, Karine Begnini, João Antonio Pêgas Henriques, Mariana Roesch Ely, Luciane C Rufatto, Sidnei Moura, Thiago Barcellos, Francine Padilha, Odir Dellagostin, Sibele Borsuk
Most studies of Brazilian red propolis have explored the composition and biological properties of its ethanolic extracts. In this work, we chemically extracted and characterized the essential oil of Brazilian red propolis (EOP) and assessed its adjuvant, antiparasitic and cytotoxic activities. The chemical composition of EOP was analyzed using gas chromatography with mass spectrometry (GC-MS). EOP was tested for in vitro activity against Trichomonas vaginalis (ATCC 30236 isolate); trophozoites were treated with different concentrations of EOP (ranging from 25 to 500 μg/mL) in order to establish the MIC and IC50 values...
2018: PloS One
https://www.readbyqxmd.com/read/29376495/anti-inflammatory-anti-allergy-agents-in-medicinal-chemistry-formerly-current-medicinal-chemistry-anti-inflammator
#9
Ashwani Kumar Dhingra, Bhawna Chopra, Jagdeep Singh Dua, Deo N Parsad
The search of novel anti-inflammatory agent is not considered as an ending process, since most of the clinically used anti-inflammatory drugs such as NSAIDs, Coxibs and GCs are allied with considerable toxicity. However, numerous approaches were used to overcome the toxicity level such as co-administration with suitable agent/substance which provides protection against toxicity as well to synthesise new potent and safe anti-inflammatory drug. Although the drug treatment has been improved steadily but yet, it is still a challenge for the medicinal chemists to identify more potent therapeutic agents to treat or reduce the symptoms of inflammatory diseases...
January 26, 2018: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29359192/targeted-phenotypic-screening-in-plasmodium-falciparum-and-toxoplasma-gondii-reveals-novel-modes-of-action-of-medicines-for-malaria-venture-malaria-box-molecules
#10
Gowtham Subramanian, Meenakshi A Belekar, Anurag Shukla, Jie Xin Tong, Ameya Sinha, Trang T T Chu, Akshay S Kulkarni, Peter R Preiser, D Srinivasa Reddy, Kevin S W Tan, Dhanasekaran Shanmugam, Rajesh Chandramohanadas
The Malaria Box collection includes 400 chemically diverse small molecules with documented potency against malaria parasite growth, but the underlying modes of action are largely unknown. Using complementary phenotypic screens against Plasmodium falciparum and Toxoplasma gondii, we report phenotype-specific hits based on inhibition of overall parasite growth, apicoplast segregation, and egress or host invasion, providing hitherto unavailable insights into the possible mechanisms affected. First, the Malaria Box library was screened against tachyzoite stage T...
January 2018: MSphere
https://www.readbyqxmd.com/read/29351667/what-to-expect-and-when-benznidazole-toxicity-in-chronic-chagas-disease-treatment
#11
E Aldasoro, E Posada, A Requena-Méndez, A Calvo-Cano, N Serret, A Casellas, S Sanz, D Soy, M J Pinazo, J Gascon
Background: Benznidazole is one of the two most effective antiparasitic drugs for Chagas' disease treatment. However, knowledge about its toxicity profile is mostly based on post-marketing observational studies. Objectives: Our study combines data from two prospective clinical trials designed to assess the safety of the drug newly produced by ELEA Laboratories (Abarax®). Methods: Eligible participants were selected using a consecutive sampling strategy in the CINEBENZ and BIOMARCHA studies between 2013 and 2016 (EUDRACT 2011-002900-34 and 2012-002645-38, respectively, and clinicaltrials...
January 16, 2018: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/29349663/ibandronate-metal-complexes-solution-behavior-and-antiparasitic-activity
#12
Bruno Demoro, Santiago Rostán, Mauricio Moncada, Zhu-Hong Li, Roberto Docampo, Claudio Olea Azar, Juan Diego Maya, Julia Torres, Dinorah Gambino, Lucía Otero
To face the high costs of developing new drugs, researchers in both industry and academy are looking for ways to repurpose old drugs for new uses. In this sense, bisphosphonates that are clinically used for bone diseases have been studied as agents against Trypanosoma cruzi, causative parasite of Chagas disease. In this work, the development of first row transition metal complexes (M = Co2+, Mn2+, Ni2+) with the bisphosphonate ibandronate (iba, H4iba representing the neutral form) is presented. The in-solution behavior of the systems containing iba and the selected 3d metal ions was studied by potentiometry...
January 18, 2018: Journal of Biological Inorganic Chemistry: JBIC
https://www.readbyqxmd.com/read/29346035/determination-of-105-antibiotic-anti-inflammatory-antiparasitic-agents-and-tranquilizers-by-lc-ms-ms-based-on-an-acidic-quechers-like-extraction
#13
Aurélien Desmarchelier, Kaïli Fan, Mai Minh Tien, Marie-Claude Savoy, Adrienne Tarres, Denis Fuger, Alexandre Goyon, Thomas Bessaire, Pascal Mottier
A procedure for screening 105 veterinary drugs in foods by liquid chromatography tandem mass-spectrometry (LC-MS/MS) is presented. Its scope encompasses raw materials of animal origin (milk, meat, fish, egg and fat) but also related processed ingredients and finished products commonly used and manufactured by food business operators. Due to the complexity of the matrices considered and to efficiently deal with losses during extraction and matrix effects during MS source ionisation, each sample was analyzed twice, that is "unspiked" and "spiked at the screening target concentration" using a QuEChERS-like extraction...
January 18, 2018: Food Additives & Contaminants. Part A, Chemistry, Analysis, Control, Exposure & Risk Assessment
https://www.readbyqxmd.com/read/29337988/l-arginine-supplementation-reduces-mortality-and-improves-disease-outcome-in-mice-infected-with-trypanosoma-cruzi
#14
Sofía Carbajosa, Héctor O Rodríguez-Angulo, Susana Gea, Carlos Chillón-Marinas, Cristina Poveda, María C Maza, Diana Colombet, Manuel Fresno, Núria Gironès
Chagas disease caused by Trypanosoma cruzi is a neglected disease that affects about 7 million people in Latin America, recently emerging on other continents due to migration. As infection in mice is characterized by depletion of plasma L-arginine, the effect on infection outcome was tested in mice with or without L-arginine supplementation and treatment with 1400W, a specific inhibitor of inducible nitric oxide synthase (iNOS). We found that levels of L-arginine and citrulline were reduced in the heart and plasma of infected mice, whereas levels of asymmetric dimethylarginine, an endogenous iNOS inhibitor, were higher...
January 2018: PLoS Neglected Tropical Diseases
https://www.readbyqxmd.com/read/29329071/synthesis-anticancer-activity-and-mechanism-of-action-of-new-thiazole-derivatives
#15
Temístocles Italo de Santana, Miria de Oliveira Barbosa, Paulo André Teixeira de Moraes Gomes, Anne Cecília Nascimento da Cruz, Teresinha Gonçalves da Silva, Ana Cristina Lima Leite
Thiazole derivatives are recognized to possess various biological activities as antiparasitic, antifungal, antimicrobial and antiproliferative. The present work reports the synthesis of 22 new substances belonging to two classes of compounds: thiosemicarbazones and thiazoles, with the purpose of developing new drugs that present high specificity for tumor cells and low toxicity to the organism. A cytotoxic screening was performed to evaluate the performance of the new derivatives in five tumor cell lines. Eight compounds were shown to be promising in at least three tumor cell lines...
December 14, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29327961/tracheal-resection-in-a-secretary-bird-sagittarius-serpentarius-with-granulomatous-foreign-body-induced-tracheitis
#16
Carsten Ludwig, Imke Lueders, Volker Schmidt, Hermann Kempf
A 24-year-old female secretary bird ( Sagittarius serpentarius) was presented with acute, mild dyspnea occurring only during feeding times. Despite initial conservative therapy consisting of antibiotics and antifungal, antiparasitic, and anti-inflammatory drugs, the dyspnea worsened progressively, resulting in severe respiratory distress. Radiographs of the trachea suggested stenosis in the caudal one-third of the trachea. Tracheal endoscopy revealed an obstruction of approximately 90% of the tracheal lumen, in addition to mild suspected aspergillosis of the air sacs...
December 2017: Journal of Avian Medicine and Surgery
https://www.readbyqxmd.com/read/29324075/screening-of-veterinary-drug-residues-in-food-by-lc-ms-ms-background-and-challenges
#17
Thierry Delatour, Lucie Racault, Thomas Bessaire, Aurélien Desmarchelier
Regulatory agencies and government authorities have established maximum residue limits (MRL) in various food matrices of animal origin for supporting governments and food operators in the monitoring of veterinary drug residues in the food chain, and ultimately in the consumer's plate. Today, about 200 veterinary drug residues from several families, mainly with antibiotic, antiparasitic or anti-inflammatory activities, are regulated in a variety of food matrices such as milk, meat or egg. The current article provides a review of the regulatory framework in milk and muscle including data from Codex Alimentarius, Europe, USA, Canada and China for about 220 veterinary drugs...
January 11, 2018: Food Additives & Contaminants. Part A, Chemistry, Analysis, Control, Exposure & Risk Assessment
https://www.readbyqxmd.com/read/29317890/enterobius-vermicularis-in-the-endometrium-of-the-uterus-a-case-report
#18
Biserka Pigac, Silvija Mašić, Valentina Mašić
Enterobius vermicularis is an intestinal nematode of humans and the most common helminth infection. Main transmission path is direct contact between infected and uninfected person meaning ingestion of the eggs. Human infections are usually asymptomatic or manifest as perianal itching. Although ectopic locations are uncommon, Enterobius can occasionally be detected in appendix, kidney, male urinary tract and female genital tract. We present a case from Varaždin General Hospital, Varaždin, Croatia in 2012, involving a 90-yr-old female patient who underwent hysterectomy leading to accidental finding of E...
October 2017: Iranian Journal of Parasitology
https://www.readbyqxmd.com/read/29317871/perspective-on-the-genetic-response-to-antiparasitics-a-review-article
#19
REVIEW
Patricia Alarcon-Valdes, Mariana Ortiz-Reynoso, Jonnathan Santillan-Benitez
Background: Drugs' pharmacokinetics and pharmacodynamics can be affected by diverse genetic variations, within which simple nucleotide polymorphisms (SNPs) are the most common. Genetic variability is one of the factors that could explain questions like why a given drug does not have the desired effect or why do adverse drug reactions arise. Methods: In this retrospective observational study, literature search limits were set within PubMed database as well as the epidemiological bulletins published by the Mexican Ministry of Health, from Jan 1st 2001 to Mar 31st 2017 (16 years)...
October 2017: Iranian Journal of Parasitology
https://www.readbyqxmd.com/read/29317800/leishmaniasis-in-humans-drug-or-vaccine-therapy
#20
REVIEW
Masoud Ghorbani, Ramin Farhoudi
Leishmania is an obligate intracellular pathogen that invades phagocytic host cells. Approximately 30 different species of Phlebotomine sand flies can transmit this parasite either anthroponotically or zoonotically through their bites. Leishmaniasis affects poor people living around the Mediterranean Basin, East Africa, the Americas, and Southeast Asia. Affected regions are often remote and unstable, with limited resources for treating this disease. Leishmaniasis has been reported as one of the most dangerous neglected tropical diseases, second only to malaria in parasitic causes of death...
2018: Drug Design, Development and Therapy
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