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Antiparasitic drugs

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https://www.readbyqxmd.com/read/29227923/in-vitro-leishmanicidal-and-trypanocidal-evaluation-and-magnetic-properties-of-7-amino-1-2-4-triazolo-1-5-a-pyrimidine-cu-ii-complexes
#1
J M Méndez-Arriaga, I Oyarzabal, G Escolano, A Rodríguez-Diéguez, M Sánchez-Moreno, J M Salas
Two triazolopyrimidine complexes have been obtained from reaction between 7-amino-1,2,4-triazolo[1,5-a]pyrimidine (7atp) and Cu (II) salts. Crystal structures of [Cu2(μ-7atp)4Cl2]Cl2·4H2O (1) and [Cu2(μ-7atp)4(H2O)2](NO3)4·H2O (2) have been studied by X-ray diffraction methods and characterized by spectroscopic and thermal analysis. Magnetic studies of these dinuclear complexes have revealed the existence of moderate antiferromagnetic interactions between the copper ions, with J values of -91.2 and -96...
December 2, 2017: Journal of Inorganic Biochemistry
https://www.readbyqxmd.com/read/29219244/-click-on-plga-peg-and-hyaluronic-acid-gaining-access-to-anti-leishmanial-pentamidine-bioconjugates
#2
Angela Scala, Anna Piperno, Nicola Micale, Placido G Mineo, Antonio Abbadessa, Roberta Risoluti, Germano Castelli, Federica Bruno, Fabrizio Vitale, Antonio Cascio, Giovanni Grassi
Pentamidine (Pent), an antiparasitic drug used for the treatment of visceral leishmaniasis, has been modified with terminal azide groups and conjugated to two different polymer backbones (PLGA-PEG [PP] copolymer and hyaluronic acid [HA]) armed with alkyne end-groups. The conjugation has been performed by Copper Catalyzed Azido Alkyne Cycloaddition (CuAAC) using CuSO4 /sodium ascorbate as metal source. The novel PP-Pent and HA-Pent bioconjugates are proposed, respectively, as non-targeted and targeted drug delivery systems against Leishmania infections...
December 8, 2017: Journal of Biomedical Materials Research. Part B, Applied Biomaterials
https://www.readbyqxmd.com/read/29208358/effect-of-epicatechin-a-flavonoid-on-the-no-and-nos-activity-of-raillietina-echinobothrida
#3
Mitali Chetia, Robin Das
(-)-Epicatechin, a natural flavonoid reportedly has huge pharmacological properties. In this study the cestocide effect of (-)-epicatechin is demonstrated in Raillietina echinobothrida. Although the antiparasitic activity of (-)-epicatechin has been demonstrated against protozoa, helminthes and ectoparasites, in the present study the cestocide activity of (-)-epicatechin is shown to be related to a decrease in nitric oxide synthase (NOS) activity and nitric oxide (NO) production. On exposure to 0.53mg/ml each of epicatechin, reference drug praziquantel and Ѡ Nitro-L- Arginine Methyl Ester (NOS inhibitor), the parasites attained paralysis at 10...
December 2, 2017: Acta Tropica
https://www.readbyqxmd.com/read/29190292/tnf-%C3%AE-blockade-suppresses-pericystic-inflammation-following-anthelmintic-treatment-in-porcine-neurocysticercosis
#4
Siddhartha Mahanty, Miguel A Orrego, Carla Cangalaya, M Paz Adrianzen, Gianfranco Arroyo, Juan Calcina, Armando E Gonzalez, Héctor H García, Cristina Guerra-Giraldez, Theodore E Nash
BACKGROUND: Neurocysticercosis (NCC) is an infection of the brain with the larval cyst of the tapeworm, Taenia solium. Cysticidal treatment induces parasite killing resulting in a post inflammatory response and seizures, which generally requires corticosteroid treatment to control inflammation. The nature of this response and how to best control it is unclear. We investigated the anti-inflammatory effects of pretreatment with etanercept (ETN), an anti-tumor necrosis factor agent, or dexamethasone (DEX), a high potency corticosteroid, on the post treatment inflammatory response in naturally infected pigs with neurocysticercosis after a single dose of the cysticidal drug praziquantel (PZQ)...
November 2017: PLoS Neglected Tropical Diseases
https://www.readbyqxmd.com/read/29170085/the-modelling-studies-determing-the-mode-of-action-of-anthelmintics-inhibiting-in-vitro-tpp-of-anisakis-simplex-s-l
#5
Elżbieta Łopieńska-Biernat, Tomasz Molcan, Łukasz Paukszto, Jan Paweł Jastrzębski, Kamil Myszczyński
The trehalose-6-phosphate phosphatase (TPP) enzyme is involved in the synthesis of trehalose, the main sugar in the energy metabolism of nematodes. TPP is a member of the HAD-like hydrolase superfamily and shows a robust and specific phosphatase activity for the substrate trehalose-6-phosphate. The presence of conserved active sites of TPP in closely related nematodes and its absence in humans makes it a promising target for antiparasitic drugs. In the present study, homology modeling, molecular docking and MD simulation techniques were used to explore the structure and dynamics of TPP...
November 20, 2017: Experimental Parasitology
https://www.readbyqxmd.com/read/29167671/immune-checkpoint-targets-for-host-directed-therapy-to-prevent-and-treat-leishmaniasis
#6
REVIEW
Rajiv Kumar, Shashi Bhushan Chauhan, Susanna S Ng, Shyam Sundar, Christian R Engwerda
Leishmaniasis encompasses a group of diseases caused by protozoan parasites belonging to the genus Leishmania. These diseases range from life threatening visceral forms to self-healing cutaneous lesions, and each disease manifestations can progress to complications involving dissemination of parasites to skin or mucosal tissue. A feature of leishmaniasis is the key role host immune responses play in disease outcome. T cells are critical for controlling parasite growth. However, they can also contribute to disease onset and progression...
2017: Frontiers in Immunology
https://www.readbyqxmd.com/read/29165511/-cystoisospora-belli-infection-in-hiv-patients-analysis-of-cases-with-different-clinical-evolution
#7
Heber Silva-Díaz, Darwin Fernández-Valverde, Gustavo Hernández-Córdova, Virgilio E Failoc-Rojas
INTRODUCTION: Cystoisospora belli infection is one of the most important causes of watery diarrhea in patients with HIV and causes high rates of morbidity and mortality. METHODS: A retrospective study was conducted in patients with HIV and diarrhea by C. belli. Clinical and laboratory characteristics were collected by analyzing clinical records. RESULTS: Four had recurrent diarrhea despite receiving secondary prophylaxis with cotrimoxazole and specific treatment, two of which had a good viral and immunological response to highly active antiretroviral therapy (HAART) at the time of diagnosis and antiparasitic treatment...
August 2017: Revista Chilena de Infectología: órgano Oficial de la Sociedad Chilena de Infectología
https://www.readbyqxmd.com/read/29165211/case-report-myiasis-due-to-cochliomyia-hominivorax-and-dermatobia-hominis-clinical-and-pathological-differences-between-two-species-in-northern-peru
#8
Virgilio E Failoc-Rojas, Carolina Molina-Ayasta, Jaime Salazar-Zuloeta, Abel Samamé, Heber Silva-Díaz
Infestations caused by fly larvae (Myiasis) have been observed in patients with risk factors and in tropical zones. The aim of our study was to describe the clinical and epidemiological aspects and the risk factors associated with the occurrence of obligatory myiasis, as well as the therapeutic approach to patients. We identified the cases of myiasis diagnosed in two referral hospitals in northern Peru from January 2012 to December 2015 and included patients in whom larval development and a compatible clinical profile were observed...
November 20, 2017: American Journal of Tropical Medicine and Hygiene
https://www.readbyqxmd.com/read/29163920/harnessing-fungal-nonribosomal-cyclodepsipeptide-synthetases-for-mechanistic-insights-and-tailored-engineering
#9
Charlotte Steiniger, Sylvester Hoffmann, Andi Mainz, Marcel Kaiser, Kerstin Voigt, Vera Meyer, Roderich D Süssmuth
Nonribosomal peptide synthetases represent potential platforms for the design and engineering of structurally complex peptides. While previous focus has been centred mainly on bacterial systems, fungal synthetases assembling drugs like the antifungal echinocandins, the antibacterial cephalosporins or the anthelmintic cyclodepsipeptide (CDP) PF1022 await in-depth exploitation. As various mechanistic features of fungal CDP biosynthesis are only partly understood, effective engineering of NRPSs has been severely hampered...
November 1, 2017: Chemical Science
https://www.readbyqxmd.com/read/29160352/genital-myiasis-associated-with-genital-piercing-case-report
#10
Daniel Melecchi Freitas, Flavio Aranovich, José Nicolau Olijnyk, Renan Lemos
CONTEXT: Myiasis is caused by larval infestation that usually occurs in exposed wounds. Dermatobia hominis is the most common fly species responsible for this parasitic infection. Genital piercing is an ornamental practice used in certain social circles. At placement, it transverses the skin surface and, as such, may be related to complications. CASE REPORT: We report a case of a 31-year-old man with a history of wound infection secondary to genital piercing who was exposed to an environment with flies, leading to myiasis...
November 9, 2017: São Paulo Medical Journal, Revista Paulista de Medicina
https://www.readbyqxmd.com/read/29152541/missing-the-mark-a-two-time-point-cohort-study-estimating-intestinal-parasite-prevalence-in-informal-settlements-in-lima-peru
#11
Michael Townsend Cooper, Rapha A Searing, David M Thompson, David Bard, Hélène Carabin, Carlos Gonzales, Carmen Zavala, Kyle Woodson, Monique Naifeh
Objectives: The World Health Organization's (WHO) recommendations list Peru as potentially needing prevention of soil-transmitted helminthiasis (STH). Prevalence of STH varies regionally and remains understudied in the newest informal settlements of the capital city, Lima. The purpose of this study was to evaluate the need for Mass Drug Administration (MDA) of antiparasitic drugs in the newest informal settlements of Lima. The aim of this study was to estimate the season-specific prevalence of STH to determine if these prevalence estimates met the WHO threshold for MDA in 3 informal settlements...
2017: Global Pediatric Health
https://www.readbyqxmd.com/read/29131471/the-toxicological-effects-of-some-avermectins-on-goat-liver-carbonic-anhydrase-enzyme
#12
Cuneyt Caglayan, İlhami Gulcin
Avermectins are used worldwide as antiparasitic drugs in the field of veterinary medicine and as agricultural pesticides and insecticides. Carbonic anhydrase (CA, E.C. 4.2.1.1) is a zinc-containing metalloenzyme that catalyzes the reversible hydration of carbon dioxide (CO2 ) to yield protons (H(+) ) and bicarbonate (HCO3(-) ). In this study, some avermectins, including abamectin, doramectin, eprinomectin, and moxidectin, were investigated for in vitro inhibitory effects on the CA enzyme purified from goat liver, which was purified (125...
November 13, 2017: Journal of Biochemical and Molecular Toxicology
https://www.readbyqxmd.com/read/29127083/ntz-increases-%C3%AE-catenin-citrullination-to-suppress-wnt-signaling
#13
(no author information available yet)
The antiparasitic drug NTZ inhibits WNT signaling and APC-mutant colorectal cancer cell growth.
November 10, 2017: Cancer Discovery
https://www.readbyqxmd.com/read/29122715/nematicidal-activity-of-a-water-soluble-lectin-from-seeds-of-moringa-oleifera
#14
Mário Luan Silva de Medeiros, Maiara Celine de Moura, Thiago Henrique Napoleão, Patrícia Maria Guedes Paiva, Luana Cassandra Breitenbach Barroso Coelho, Ana Carla Diógenes Suassuna Bezerra, Michele Dalvina Correia da Silva
Gastrointestinal nematodes are the major cause of animal diseases, and the indiscriminate use of synthetic anthelmintic contributes to the development of drug resistance. Natural bioproducts are noteworthy since they have proved to be promising for alternative antiparasitic therapies. This study evaluated the in vitro effect of WSMoL (water soluble Moringa oleifera lectin) on hatching of eggs and on the development of early-stage larvae of gastrointestinal nematodes from naturally infected goats. In addition, the interference of WSMoL on activity of proteases was determined and the affinity of the lectin for glycosylated molecules of these parasites was investigated using fluorescein isothiocyanate (FITC)-labeled WSMoL...
November 6, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29107437/selenium-containing-analogues-of-wc-9-are-extremely-potent-inhibitors-of-trypanosoma-cruzi-proliferation
#15
María N Chao, Melissa Storey, Catherine Li, Maricel G Rodríguez, Florencia Di Salvo, Sergio H Szajnman, Silvia N J Moreno, Roberto Docampo, Juan B Rodriguez
The obligate intracellular parasite, Trypanosoma cruzi is the etiologic agent of Chagas disease or American trypanosomiasis, which is the most prevalent parasitic disease in the Americas. The present chemotherapy to control this illness is still deficient particularly in the chronic stage of the disease. The ergosterol biosynthesis pathway has received much attention as a molecular target for the development of new drugs for Chagas disease. Especially, inhibitors of the enzymatic activity of squalene synthase were shown to be effective compounds on T...
October 16, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29107428/pt-ii-pd-ii-and-au-iii-complexes-with-a-thiosemicarbazone-derived-from-diacethylmonooxime-structural-analysis-trypanocidal-activity-cytotoxicity-and-first-insight-into-the-antiparasitic-mechanism-of-action
#16
Ana C R Gonçalves, Zumira A Carneiro, Carolina G Oliveira, Amanda Danuello, Wendell Guerra, Ronaldo J Oliveira, Francis B Ferreira, Laudimir L W Veloso-Silva, Fernanda A H Batista, Júlio C Borges, Sérgio de Albuquerque, Victor M Deflon, Pedro I S Maia
New complexes of composition [MX(HL1)] (M = Pt(II), Pd(II), X = Cl(-) or I(-)) and [MX(L1)] (M = Au(III), X = Cl(-); M = Pt(II), Pd(II), X = PPh3) have been synthesized using a potentially tridentate thiosemicarbazone (H2L1) containing an additional oxime binding site. Among other analytical methods, all the seven complexes have been structurally characterized by single crystal X-ray diffractometry. Interesting structural features such as the influence of the halide ligands on hydrogen bonds and the formation of supramolecular structures for the phosphine derivatives are discussed...
December 1, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29102680/ammoides-pusilla-apiaceae-essential-oil-activity-against-acanthamoeba-castellanii-neff
#17
Najet Souhaiel, Ines Sifaoui, Dorsaf Ben Hassine, Jean Bleton, Myriam Bonose, Fathi Moussa, José E Piñero, Jacob Lorenzo-Morales, Manef Abderrabba
Acanthamoeba is a free-living amoeba genus that causes several diseases namely, amoebic keratitis which is a painful sight threatening eyes disease. Its treatment is difficult and the exploration for new drugs is very important. The main objective of the present study was to evaluate the chemical composition of the Essential Oils (EO) obtained from leaves and flowers and aerial parts of Ammoides pusilla by an alternative method "Hydrodistillation''. Identification and quantification were realized by Gas Chromatography-Mass Spectrometry (GC-MS) and Gas Chromatography with Flame Ionization Detection (GC-FID)...
November 2, 2017: Experimental Parasitology
https://www.readbyqxmd.com/read/29097304/laser-responsive-liposome-for-selective-tumor-targeting-of-nitazoxanide-nanoparticles
#18
Wael M Darwish, Noha A Bayoumi, Mohamed T El-Kolaly
Nitazoxanide [2-(Acetyloxy)-N-(5-nitro-2-thiazolyl)benzamide], usually referred as NTZ, is an antiparasites drug with a potential anti-cancer reactivity. However, the bioavailability of nitazoxanide is limited due to its poor water solubility. In this study, nitazoxanide could be successfully incorporated in a stable biocompatible liposome (NTZ-LP) using a modified thin film hydration technique. Further, a novel lipophilic phthalocyanine star polymer R4PcZn was prepared as photosensitizer and in situ incorporated with NTZ in the liposome formulation affording a laser-responsive liposome (NTZ-ZnPc-LP)...
October 31, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29092797/gold-nanoparticles-against-parasites-and-insect-vectors
#19
REVIEW
Giovanni Benelli
Nanomaterials are currently considered for many biological, biomedical and environmental purposes, due to their outstanding physical and chemical properties. The synthesis of gold nanoparticles (Au NPs) is of high interest for research in parasitology and entomology, since these nanomaterials showed promising applications, ranging from detection techniques to drug development, against a rather wide range of parasites of public health relevance, as well as on insect vectors. Here, I reviewed current knowledge about the bioactivity of Au NPs on selected insect species of public health relevance, including major mosquito vectors, such as Aedes aegypti, Anopheles stephensi and Culex quinquefasciatus...
October 29, 2017: Acta Tropica
https://www.readbyqxmd.com/read/29083417/small-molecule-promotes-%C3%AE-catenin-citrullination-and-inhibits-wnt-signaling-in-cancer
#20
Yi Qu, Jan Roger Olsen, Xing Yuan, Phil F Cheng, Mitchell P Levesque, Karl A Brokstad, Paul S Hoffman, Anne Margrete Oyan, Weidong Zhang, Karl-Henning Kalland, Xisong Ke
Wnt (wingless)/β-catenin signaling is critical for tumor progression and is frequently activated in colorectal cancer as a result of the mutation of adenomatous polyposis coli (APC); however, therapeutic agents targeting this pathway for clinical use are lacking. Here we report that nitazoxanide (NTZ), a clinically approved antiparasitic drug, efficiently inhibits Wnt signaling independent of APC. Using chemoproteomic approaches, we have identified peptidyl arginine deiminase 2 (PAD2) as the functional target of NTZ in Wnt inhibition...
October 30, 2017: Nature Chemical Biology
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