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Antiparasitic drugs

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https://www.readbyqxmd.com/read/28715108/ivermectin-activates-girk-channels-in-a-pip2-dependent-g%C3%AE-%C3%AE-independent-manner-and-an-amino-acid-residue-at-the-slide-helix-governs-the-activation
#1
I-Shan Chen, Michihiro Tateyama, Yuko Fukata, Motonari Uesugi, Yoshihiro Kubo
Ivermectin (IVM) is a widely used antiparasitic drug in humans and pets which activates glutamate-gated Cl(-) channel in parasites. It is also known that IVM binds to the transmembrane domains (TMs) of several ligand-gated channels, such as Cys-loop receptors and P2X receptors. In this study, we found that the G-protein-gated inwardly rectifying K(+) (GIRK) channel is activated by IVM directly. By electrophysiological recordings in Xenopus oocytes, we observed that IVM activates GIRK channel in a phosphatidylinositol-4,5-biphosphate (PIP2 )-dependent manner, and that the IVM-mediated GIRK activation is independent of Gβγ ...
July 17, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/28679535/small-molecule-based-inhibition-of-mek1-2-proteins-dampens-inflammatory-responses-to-malaria-reduces-parasite-load-and-mitigates-pathogenic-outcomes
#2
Xianzhu Wu, Kiran K Dayanand, Ramesh P Thylur, Christopher C Norbury, D Channe Gowda
Malaria infections cause several systemic and severe single or multi-organ pathologies, killing hundreds of thousands of people annually. Considering the existing widespread resistance of malaria parasites to antiparasitic drugs and their high propensity to develop drug resistance, alternative strategies are required to manage malaria infections. Since malaria is a host immune response-driven disease, one approach is based on gaining a detailed understanding of the molecular and cellular processes that modulate malaria-induced innate and adaptive immune responses...
July 5, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28671059/role-of-polyamines-in-parasite-cell-architecture-and-function
#3
Marcos A Vannier-Santos, Ana M Suarez-Fontes
In the absence of accessible, effective vaccines, the fight against parasitic disease relies mostly on chemotherapy. Nevertheless, the considerable side effects, high costs and growing number of refractory cases comprise substantial drawbacks. Thus, the search for new antiparasitic compounds remains a high priority. The polyamine biosynthesis, conversion and transport pathways offer different targets for selective chemotherapy. Polyamine analogues and other antagonists may provide tools in the search for new lead compounds...
July 3, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28666754/antiparasitic-activity-of-nerolidol-in-a-mouse-model-of-schistosomiasis
#4
Marcos P Silva, Rosimeire N de Oliveira, Ana C Mengarda, Daniel B Roquini, Silmara M Alegretti, Maria C Salvadori, Fernanda S Teixeira, Damião P de Sousa, Pedro L S Pinto, Josué de Moraes
Schistosomiasis is a major public health problem worldwide, especially in poor communities. Since praziquantel is currently the only drug available to treat schistosomiasis, there is an urgent need to identify new antischistosomal drugs. Nerolidol is a sesquiterpene present as an essential oil in several plants, and it has been approved by the US Food and Drug Administration. In this study, we evaluated the in vivo antischistosomal activity of nerolidol in a mouse model of schistosomiasis infected with either adult or juvenile stages of Schistosoma mansoni...
June 27, 2017: International Journal of Antimicrobial Agents
https://www.readbyqxmd.com/read/28641558/bis-2-aminoimidazolines-and-bisguanidines-synthetic-approaches-antiparasitic-activity-and-dna-binding-properties
#5
Christophe Dardonville, J Jonathan Nué Martínez
BACKGROUND: Parasitic diseases caused by protozoan parasites of the genus Trypanosoma and Plasmodium cause some of the deadliest and disabling human infections in tropical and subtropical areas. Diphenyl-based bis(2-phenylimino)imidazolidines and bisguanidines are extremely potent antiparasitic agents against Trypanosoma brucei (etiological agent of African trypanosomiasis) and Plasmodium falciparum (etiological agent of severe malaria). Many of these compounds are also curative in mouse models of stage 1 African trypanosomiasis representing promising leads for the development of antitrypanosomal drugs...
June 22, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28624508/epidemiological-profile-of-cutaneous-larva-migrans-in-travelers-returning-to-france-between-2003-and-2015
#6
Doudou Sow, Ferelaha Soro, Emilie Javelle, Fabrice Simon, Philippe Parola, Philippe Gautret
BACKGROUND: Cutaneous larva migrans (CLM) is caused by the penetration and migration of canine or feline hookworm larvae into the skin, and frequently affects travelers from high-income countries returning from tropical and sub-tropical areas. Unfortunately, this pathology is neglected due to poor understanding among both physicians and travelers. This study describes the profile of cases reported in Marseille, France. PATIENTS AND METHODS: A retrospective study was performed in two specialized hospitals between 2003 and 2015...
June 15, 2017: Travel Medicine and Infectious Disease
https://www.readbyqxmd.com/read/28612332/cocaine-levamisole-induced-vasculitis-vasculopathy-syndrome
#7
REVIEW
Javier Marquez, Lina Aguirre, Carolina Muñoz, Andres Echeverri, Mauricio Restrepo, Luis F Pinto
PURPOSE OF REVIEW: To understand the clinical spectrum of cocaine-levamisole-induced vasculitis. Worldwide recreational drug consumption is high among the adult population from various social strata. The use of cocaine with levamisole, a frequently added antiparasitic diluent, favors the manifestations of vasculitic lesions, especially in the skin. RECENT FINDINGS: New insights into immunological mechanisms involved in the pathogenesis of the disease. There are still many unknown aspects in the pathogenesis of this disease, such as the immune system interaction with p-ANCAs and the release of inflammatory NETs (neutrophil extracellular traps), which are the origin of auto-antigens and tissue damage, manifesting as vasculitic purpura on the skin...
June 2017: Current Rheumatology Reports
https://www.readbyqxmd.com/read/28610952/structural-diversity-of-marine-cyclic-peptides-and-their-molecular-mechanisms-for-anticancer-antibacterial-antifungal-and-other-clinical-applications
#8
REVIEW
Yeji Lee, Chanvorleak Phat, Soon-Cheol Hong
Many cyclic peptides and analogues derived from marine sources are known to possess biological properties, including anticancer, antitumor, antibacterial, antifungal, antiparasitic, anti-inflammation, anti-proliferative, anti-hypertensive, cytotoxic, and antibiotic properties. These compounds demonstrate different activities and modes of action according to their structure such as cyclic oligopeptide, cyclic lipopeptide, cyclic glycopeptide and cyclic depsipeptide. The recent advances in application of the above-mentioned cyclic peptides were reported in dolastatins, soblidotin, didemnin B, aplidine, salinosporamide A, kahalalide F and bryostatin 1 and they are currently in clinical trials...
June 10, 2017: Peptides
https://www.readbyqxmd.com/read/28606429/mebendazole-an-antiparasitic-drug-inhibits-drug-transporters-expression-in-preclinical-model-of-gastric-peritoneal-carcinomatosis
#9
Laine Celestino Pinto, Caroline de Fátima Aquino Moreira-Nunes, Bruno Moreira Soares, Rommel Mário Rodriguez Burbano, José Alexandre Rodrigues de Lemos, Raquel Carvalho Montenegro
The present study aimed to investigate whether MBZ down-regulates drug transporter expression (ABCB1, ABCC1, SLC47A1). mRNA expression level of ABCB1, ABCC1 and SLC47A1 was evaluated by qPCR and protein expression levels MDR-1 was performed by western blotting in malignant ascites cells (AGP-01) treated with MBZ for 24h. The mRNA expression level of ABCB1 and ABCC1 significantly decreased at a 1.0μM of MBZ compared to negative control, while SLC47A1 extremely decreased at all tested concentrations of MBZ. Protein expression levels MDR-1 significantly decreased at a 1...
June 9, 2017: Toxicology in Vitro: An International Journal Published in Association with BIBRA
https://www.readbyqxmd.com/read/28606053/protein-kinase-inhibitors-as-potential-antimicrobial-drugs-against-tuberculosis-malaria-and-hiv
#10
Yong Cheng, Jeffrey S Schorey, Cheng-Cai Zhang, Xuejuan Tan
Infectious diseases that are caused by pathogenic microbes such as bacteria, viruses, parasites or fungi remain the top major cause of death across the world, particularly in low income countries, and may be transmitted from person to person, or from insects or animals. In general, infectious diseases may be treated with antimicrobial agents including antibiotics, antiviral, antifungal or antiparasitic medications. The therapeutic application of antimicrobial drugs in the 20th century substantially contributed to the global control of infectious diseases worldwide...
June 12, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28605319/medicinal-mushrooms-in-human-clinical-studies-part-i-anticancer-oncoimmunological-and-immunomodulatory-activities-a-review
#11
Solomon P Wasser
More than 130 medicinal functions are thought to be produced by medicinal mushrooms (MMs) and fungi, including antitumor, immunomodulating, antioxidant, radical scavenging, cardiovascular, antihypercholesterolemic, antiviral, antibacterial, antiparasitic, antifungal, detoxification, hepatoprotective, antidiabetic, and other effects. Many, if not all, higher Basidiomycetes mushrooms contain biologically active compounds in fruit bodies, cultured mycelia, and cultured broth. Special attention has been paid to mushroom polysaccharides...
2017: International Journal of Medicinal Mushrooms
https://www.readbyqxmd.com/read/28595532/pharmacological-and-toxicological-profile-of-harmane-%C3%AE-carboline-alkaloid-friend-or-foe
#12
Haroon Khan, Seema Patel, Mohammad A Kamal
The plant secondary metabolites have an outstanding therapeutic potential and success over the years. In fact, it is the foundation of numerous clinically used drugs. Similarly, there is a general perception that these products usually have safe option. However, such products might have toxic/unwanted lethal effects therefore, along with biological relevance, toxicological evaluation is equally important for clinical applications. Harmane-β-carboline alkaloid has shown several pharmacological activities such as antianxiety, antidepressant, antiplatelet, antidiabetic, acetylcholinesterase and myeloperoxidase inhibition, antioxidant, antiparasitic, hypotensive, morphine withdrawal syndrome alleviation, and antinociceptive effects...
June 6, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/28572816/ergosterol-isolated-from-the-basidiomycete-pleurotus-salmoneostramineus-affects-trypanosoma-cruzi-plasma-membrane-and-mitochondria
#13
Tatiana Rodrigues Alexandre, Marta Lopes Lima, Mariana Kolos Galuppo, Juliana Tonini Mesquita, Matilia Ana do Nascimento, Augusto Leonardo Dos Santos, Patricia Sartorelli, Daniel Carvalho Pimenta, Andre Gustavo Tempone
BACKGROUND: Major drawbacks of the available treatment against Chagas disease (American trypanosomiasis) include its toxicity and therapeutic inefficiency in the chronic phase of the infection, which makes it a concern among neglected diseases. Therefore, the discovery of alternative drugs for treating chronic Chagas disease requires immediate action. In this work, we evaluated the mushroom Pleurotus salmoneostramineus in the search for potential antiparasitic compounds. METHODS: Fruit bodies of the basidiomycete Pleurotus salmoneostramineus were triturated and submitted to organic solvent extraction...
2017: Journal of Venomous Animals and Toxins Including Tropical Diseases
https://www.readbyqxmd.com/read/28552793/artichoke-leaf-extract-protects-liver-of-schistosoma-mansoni-infected-mice-through-modulation-of-hepatic-stellate-cells-recruitment
#14
Shaimaa Ahmed Sharaf El-Deen, Reham Mustafa Brakat, Asmaa Shams El Dein Mohamed
Schistosomiasis is the second most common human parasitic disease worldwide. It is responsible for 300000 deaths per year. Liver fibrosis is the main pathology of schistosomiasis and its complications are the major cause of death in infected cases. Unfortunately, the therapeutic dose of praziquantel (PZQ) - the main drug treatment - doesn't markedly affect fibrosis. In the present study, antiparasitic and hepatoprotective properties of artichoke leaf extract (ALE) were tested on mice experimentally infected with Schistosoma mansoni (S...
July 2017: Experimental Parasitology
https://www.readbyqxmd.com/read/28508166/toxoplasma-gondii-and-schizophrenia-a-review-of-published-rcts
#15
REVIEW
Sam D Chorlton
Over the last 60 years, accumulating evidence has suggested that acute, chronic, and maternal Toxoplasma gondii infections predispose to schizophrenia. More recent evidence suggests that chronically infected patients with schizophrenia present with more severe disease. After acute infection, parasites form walled cysts in the brain, leading to lifelong chronic infection and drug resistance to commonly used antiparasitics. Chronic infection is the most studied and closely linked with development and severity of schizophrenia...
July 2017: Parasitology Research
https://www.readbyqxmd.com/read/28503051/an-update-review-on-the-anthelmintic-activity-of-bitter-gourd-momordica-charantia
#16
REVIEW
Sutthaya Poolperm, Wannee Jiraungkoorskul
Momordica charantia (Family: Cucurbitales), as known as bitter melon or gourd, is a daily consumption as food and traditional medicinal plant in Southeast Asia and Indo-China. It has been shown to possess anticancer, antidepressant, antidiabetic, anti-inflammatory, antimicrobial, antiobesity, antioxidant, and antiulcer properties. Its common phytochemical components include alkaloids, charantin, flavonoids, glycosides, phenolics, tannins, and terpenoids. This plant is rich in various saponins including momordicin, momordin, momordicoside, karavilagenin, karaviloside, and kuguacin, all of which have been reported to contribute to its remedial properties including antibacterial, antifungal, antiviral, and antiparasitic infections...
January 2017: Pharmacognosy Reviews
https://www.readbyqxmd.com/read/28502250/antiplasmodial-dihetarylthioethers-target-the-coenzyme-a-synthesis-pathway-in-plasmodium-falciparum-erythrocytic-stages
#17
Thomas Weidner, Leonardo Lucantoni, Abed Nasereddin, Lutz Preu, Peter G Jones, Ron Dzikowski, Vicky M Avery, Conrad Kunick
BACKGROUND: Malaria is a widespread infectious disease that threatens a large proportion of the population in tropical and subtropical areas. Given the emerging resistance against the current standard anti-malaria chemotherapeutics, the development of alternative drugs is urgently needed. New anti-malarials representing chemotypes unrelated to currently used drugs have an increased potential for displaying novel mechanisms of action and thus exhibit low risk of cross-resistance against established drugs...
May 15, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28479228/design-strategies-of-oxidosqualene-cyclase-inhibitors-targeting-the-sterol-biosynthetic-pathway
#18
REVIEW
Vitor Won-Held Rabelo, Nelilma Correia Romeiro, Paula Alvarez Abreu
Targeting the sterol biosynthesis pathway has been explored for the development of new bioactive compounds. Among the enzymes of this pathway, oxidosqualene cyclase (OSC) which catalyzes lanosterol cyclization from 2,3-oxidosqualene has emerged as an attractive target. In this work, we reviewed the most promising OSC inhibitors from different organisms and their potential for the development of new antiparasitic, antifungal, hypocholesterolemic and anticancer drugs. Different strategies have been adopted for the discovery of new OSC inhibitors, such as structural modifications of the natural substrate or the reaction intermediates, the use of the enzyme's structural information to discover compounds with novel chemotypes, modifications of known inhibitors and the use of molecular modeling techniques such as docking and virtual screening to search for new inhibitors...
July 2017: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/28453841/the-use-of-quinacrine-in-nitroimidazole-resistant-giardia-duodenalis-an-old-drug-for-an-emerging-problem
#19
MULTICENTER STUDY
Ana Requena-Méndez, Pilar Goñi, Encarnación Rubio, Diana Pou, Victoria Fumadó, Silvia Lóbez, Edelweiss Aldasoro, Juan Cabezos, Maria Eugenia Valls, Begoña Treviño, Antonio Federico Martínez Montseny, Antonio Clavel, Joaquim Gascon, José Muñoz
Background.: There is little evidence regarding the management of refractory giardiasis after treatment with nitroimidazoles. This study estimates the proportion of persistent giardiasis in 3 hospitals in Barcelona, describes associated risk factors and genotype, and evaluates the efficacy rate of quinacrine in those with persistent giardiasis. Methods.: A clinical, prospective, observational study was conducted in patients with giardiasis treated with nitroimidazoles...
March 15, 2017: Journal of Infectious Diseases
https://www.readbyqxmd.com/read/28446445/susceptibility-testing-of-medically-important-parasites
#20
REVIEW
Abebe Genetu Bayih, Anjan Debnath, Edward Mitre, Christopher D Huston, Benoît Laleu, Didier Leroy, Benjamin Blasco, Brice Campo, Timothy N C Wells, Paul A Willis, Peter Sjö, Wesley C Van Voorhis, Dylan R Pillai
In the last 2 decades, renewed attention to neglected tropical diseases (NTDs) has spurred the development of antiparasitic agents, especially in light of emerging drug resistance. The need for new drugs has required in vitro screening methods using parasite culture. Furthermore, clinical laboratories sought to correlate in vitro susceptibility methods with treatment outcomes, most notably with malaria. Parasites with their various life cycles present greater complexity than bacteria, for which standardized susceptibility methods exist...
July 2017: Clinical Microbiology Reviews
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