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Paula Viviani, Adrian Lifschitz, Jorge García, María Laura Maté, Miguel Angel Quiroga, Carlos Lanusse, Guillermo Virkel
1. Precision-cut liver slices (PCLS) from food-producing animals have not been extensively used to study xenobiotic metabolism, and thus information on this field of research is sparse. 2. The aims of the present work were to further validate the technique of production and culture of bovine PCLS and to characterize the metabolic interaction between the anthelmintic albendazole (ABZ) and the flavin-monooxygenase (FMO) inhibitor methimazole (MTZ). 3. Nine (9) steers were used as donors. PCLS were produced and incubated under two methods, a dynamic organ culture (DOC) incubator and a well-plate (WP) system...
October 21, 2016: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
Zongze Zhang, Robin B Gasser, Xin Yang, Fangyuan Yin, Guanghui Zhao, Min Bao, Baoliang Pan, Weiyi Huang, Chunren Wang, Fengcai Zou, Yanqin Zhou, Junlong Zhao, Rui Fang, Min Hu
Haemonchus contortus is one of the most important parasitic nematodes of small ruminants around the world, particularly in tropical and subtropical regions. The control of haemonchosis relies mainly on anthelmintics, but the excessive and prolonged use of anthelmintics is causing serious drug resistance issues in many countries. As benzimidazole (BZ) anthelmintics have been broadly used in China, we hypothesized that resistance is widespread. Given the link between three known single nucleotide polymorphisms (SNPs, designated F167Y, E198A and F200Y) in the isotype-1 β-tubulin gene and BZ resistance, our goal here was to explore the presence of these mutations in H...
October 5, 2016: International Journal for Parasitology, Drugs and Drug Resistance
Shyamalima Gogoi, Arun K Yadav
BACKGROUND: Leaves of Caesalpinia bonducella (L.) Roxb. have been traditionally used as an herbal remedy to treat the intestinal helminthic infections in traditional medicine of India. AIM: This study was undertaken to evaluate the potential in vitro and in vivo anthelmintic effects of C. bonducella leaf extract against Syphacia obvelata (Nematoda) and Hymenolepis diminuta (Cestoda). MATERIALS AND METHODS: The in vitro anthelmintic activity of the extract was investigated on adult worms of S...
September 2016: Journal of Intercultural Ethnopharmacology
Purobi Nath, Arun K Yadav
BACKGROUND: The rhizomes of a herb Acorus calamus Linn. (Acoraceae) have been widely used as a traditional medicine to cure intestinal-helminthic infections in India and South Africa. AIM: This study was undertaken to investigate the in vivo anthelmintic activity of a standardized methanolic extract obtained from the rhizomes A. calamus in a rodent model. MATERIALS AND METHODS: A methanolic extract obtained from rhizomes of A. calamus was characterized for active principle using nuclear magnetic resonance (1)H NMR, (13)C NMR, mass and infrared spectroscopy...
September 2016: Journal of Intercultural Ethnopharmacology
Ananta Swargiary, Abhijita Daimari, Manita Daimari, Noymi Basumatary, Ezekiel Narzary
OBJECTIVE: Clerodendrum viscosum, Eryngium foetidum, Lippia javanica, and Murraya koenigii are one among the common wild edible plants in Northeast India which are also used as antidiabetic, stomach-ache relieving drugs, etc., The present study was aimed to reveal the phytochemical, antioxidant, and anthelmintic activity of the plants. MATERIALS AND METHODS: The antioxidant capacity of methanolic extract of plants was studied by 1,1-diphenyl-2-picrylhydrazyl (DPPH), ferric reducing antioxidant power, TBARS, and total antioxidant activity (TAA)...
July 2016: Indian Journal of Pharmacology
Mark D Mathew, Neal D Mathew, Angela Miller, Mike Simpson, Vinci Au, Stephanie Garland, Marie Gestin, Mark L Edgley, Stephane Flibotte, Aruna Balgi, Jennifer Chiang, Guri Giaever, Pamela Dean, Audrey Tung, Michel Roberge, Calvin Roskelley, Tom Forge, Corey Nislow, Donald Moerman
BACKGROUND: The lack of new anthelmintic agents is of growing concern because it affects human health and our food supply, as both livestock and plants are affected. Two principal factors contribute to this problem. First, nematode resistance to anthelmintic drugs is increasing worldwide and second, many effective nematicides pose environmental hazards. In this paper we address this problem by deploying a high throughput screening platform for anthelmintic drug discovery using the nematode Caenorhabditis elegans as a surrogate for infectious nematodes...
October 2016: PLoS Neglected Tropical Diseases
Janis C Weeks, William M Roberts, Kristin J Robinson, Melissa Keaney, Jon J Vermeire, Joseph F Urban, Shawn R Lockery, John M Hawdon
The screening of candidate compounds and natural products for anthelmintic activity is important for discovering new drugs against human and animal parasites. We previously validated in Caenorhabditis elegans a microfluidic device ('chip') that records non-invasively the tiny electrophysiological signals generated by rhythmic contraction (pumping) of the worm's pharynx. These electropharyngeograms (EPGs) are recorded simultaneously from multiple worms per chip, providing a medium-throughput readout of muscular and neural activity that is especially useful for compounds targeting neurotransmitter receptors and ion channels...
September 15, 2016: International Journal for Parasitology, Drugs and Drug Resistance
C Bingham, A Hodge, B Mariadass
AIM: To determine if there was a benefit from treating ewes with a low body condition score (BCS) with long acting anthelmintic products pre-lambing and to compare the effects of two commonly used treatment options. METHODS: The study was conducted on a single commercial hill country sheep and beef property in the central North Island of New Zealand. Mixed age twin-bearing ewes were preselected by the farmer as being in poor condition 4 weeks before the planned start of lambing, and were sequentially drafted into three equal groups identified with coloured ear tags...
October 17, 2016: New Zealand Veterinary Journal
Jeannine Hess, Malay Patra, Abdul Jabbar, Vanessa Pierroz, Sandro Konatschnig, Bernhard Spingler, Stefano Ferrari, Robin B Gasser, Gilles Gasser
In this study, we present the design, synthesis, characterization and biological evaluation of structurally new ferrocenyl and ruthenocenyl derivatives of the organic anthelmintic monepantel (Zolvix(®)). All seven metallocenyl derivatives prepared (4a/b, 5a/b, 6a/b and 7) were isolated as racemates and characterized by (1)H, (13)C and (19)F NMR spectroscopies, mass spectrometry, IR spectroscopy and elemental microanalysis. The molecular structures of four compounds (4a/b, 6a and 7) were further confirmed by X-ray crystallography...
October 17, 2016: Dalton Transactions: An International Journal of Inorganic Chemistry
Marion A David, Stéphane Orlowski, Roger K Prichard, Shaima Hashem, François André, Anne Lespine
Macrocyclic lactones (ML) are important anthelmintics used in animals and humans against parasite nematodes, but their therapeutic success is compromised by the spread of ML resistance. Some ABC transporters, such as p-glycoproteins (Pgps), are selected and overexpressed in ML-resistant nematodes, supporting a role for some drug efflux proteins in ML resistance. However, the role of such proteins in ML transport remains to be clarified at the molecular level. Recently, Caenorhabditis elegans Pgp-1 (Cel-Pgp-1) has been crystallized, and its drug-modulated ATPase function characterized in vitro revealed Cel-Pgp-1 as a multidrug transporter...
September 15, 2016: International Journal for Parasitology, Drugs and Drug Resistance
Maeghan O'Neill, Cristina Ballesteros, Lucienne Tritten, Erica Burkman, Weam I Zaky, Jianguo Xia, Andrew Moorhead, Steven A Williams, Timothy G Geary
The use of microfilaricidal drugs for the control of onchocerciasis and lymphatic filariasis (LF) necessitates prolonged yearly dosing. Prospects for elimination or eradication of these diseases would be enhanced by the availability of a macrofilaricidal drug. Flubendazole (FLBZ), a benzimidazole anthelmintic, is an appealing candidate. FLBZ has demonstrated potent macrofilaricidal effects in a number of experimental rodent models and in one human trial. Unfortunately, FLBZ was deemed unsatisfactory for use in mass drug administration campaigns due to its limited oral bioavailability...
October 1, 2016: International Journal for Parasitology, Drugs and Drug Resistance
Humera Ishaq
Present study was planned to search for neuropharmacological properties of methanolic extracts of different parts of Melia azedarach Linn. because conventional medicine shows adverse effects. Recently natural products are studied worldwide, as safer alternatives, which are not duly supported with scientifically proved data. Melia azedarach (Bakayan, China berry tree) is medium sized tree belonging to family Meliaceae. Traditional use of plant is as anthelmintic, antilithic and diuretic. Topical application of oil for cramps and rheumatism is beneficial...
September 2016: Pakistan Journal of Pharmaceutical Sciences
J B Matthews, P Geldhof, T Tzelos, E Claerebout
The global increase in anthelmintic resistant nematodes of ruminants, together with consumer concerns about chemicals in food, necessitates the development of alternative methods of control for these pathogens. Sub-unit recombinant vaccines are ideally placed to fill this gap. Indeed, they are probably the only valid option for the long term control of ruminant parasitic nematodes given the increasing ubiquity of multi-drug resistance in a range of worm species across the world. The development of a sub-unit multicellular parasite vaccine to the point of practical application would be a ground-breaking step in the control of these important endemic infections of livestock...
October 11, 2016: Parasite Immunology
Masahiro Hirama
Our chemical syntheses and related scientific investigations of natural products with complex architectures and powerful biological activities are described, focusing on the very large 3 nm-long polycyclic ethers called the ciguatoxins, highly strained and labile chromoprotein antitumor antibiotics featuring nine-membered enediyne cores, and extremely potent anthelmintic macrolides called the avermectins.
2016: Proceedings of the Japan Academy. Series B, Physical and Biological Sciences
J Ventura-Cordero, P G González-Pech, P R Jaimez-Rodriguez, G I Ortíz-Ocampo, C A Sandoval-Castro, J F J Torres-Acosta
It is important to determine whether gastrointestinal nematodes (GINs) affect foliage choice of goats leading to confirm the expression of a self-medication behavior. This study investigated the effect of GIN infection on tropical foliage selection by goats. During experimental stage 1 (10 days), goats had a natural mixed GIN infection, and at stage 2 (10 days), goats were treated with effective anthelmintics to maintain them free of GIN infection. During stage 1 the twelve adult goats (32 ± 2.3 kg live weight [LW]) were assigned to three groups (n = 4) according to their initial GIN infection status: HI group, with fecal egg count (FEC) between 1450 and 2150 eggs per g/feces (EPG); MI group, medium FEC (592-1167 EPG); and the NI group, free from GIN infection...
October 9, 2016: Tropical Animal Health and Production
Rolf Nijsse, Lapo Mughini-Gras, Jaap A Wagenaar, Harm W Ploeger
BACKGROUND: To reduce environmental contamination with Toxocara canis eggs, the current general advice is to deworm all dogs older than six months on average four times a year. However, only a small proportion of non-juvenile household dogs actually shed T. canis eggs, and some dogs shed eggs more frequently than others. The identification of these frequent shedders and the associated risk factors is an important cornerstone for constructing evidence-based deworming regimens. The purpose of this study is to identify risk factors associated with recurrence of periods of shedding Toxocara eggs in a cohort of household dogs older than six months...
October 4, 2016: Parasites & Vectors
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
Paolo E Crisi, Giovanni Aste, Donato Traversa, Angela Di Cesare, Elettra Febo, Massimo Vignoli, Domenico Santori, Alessia Luciani, Andrea Boari
OBJECTIVES: The aim of this study was to retrospectively describe clinical, radiographic and therapeutic features of feline lungworm infection. METHODS: Medical records of cats with lungworm diagnosis, thoracic radiography and without concurrent diseases between 2013 and 2015 were reviewed. Collection of data included physical examination, haematology, serum biochemistry, therapy with a variety of anthelmintics and outcomes. RESULTS: Thirty-seven records were recovered and 26 were included in the study...
September 30, 2016: Journal of Feline Medicine and Surgery
Luis E Ferreira, Bruno I Benincasa, Ana L Fachin, Suzelei C França, Silvia S H T Contini, Ana C S Chagas, Rene O Beleboni
Haemonchus contortus is an important gastrointestinal parasite on sheep farms in tropical regions. The resistance of the parasite against most anthelmintic drugs represents a great economic problem to sheep farming and is a major challenge that needs to be overcome. The searches for new anthelmintic agents that act on different stages of the parasite's life cycle are necessary for the development of new therapeutic options. The aim of this study was to evaluate the in vitro and in vivo anthelmintic activity of Thymus vulgaris essential oil against H...
September 15, 2016: Veterinary Parasitology
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