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https://www.readbyqxmd.com/read/28214869/effects-of-antimalarial-tafenoquine-on-blood-platelet-activity-and-survival
#1
Hang Cao, Rosi Bissinger, Anja T Umbach, Abdulla Al Mamun Bhuyan, Florian Lang, Meinrad Gawaz
BACKGROUND/AIMS: The 8-aminoquinoline tafenoquine has been shown to be effective against Plasmodia, Leishmania and Trypanosoma. The substance is at least in part effective by triggering apoptosis of the parasites. Moreover, tafenoquine has been shown to trigger eryptosis, the suicidal erythrocyte death characterized by cell shrinkage and cell membrane scrambling with phosphatidylserine translocation to the erythrocyte surface. The effect of tafenoquine on eryptosis is in part due to stimulation of Ca2+ entry and oxidative stress...
January 26, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28211535/arylmethylamino-steroids-as-antiparasitic-agents
#2
Reimar Krieg, Esther Jortzik, Alice-Anne Goetz, Stéphanie Blandin, Sergio Wittlin, Mourad Elhabiri, Mahsa Rahbari, Selbi Nuryyeva, Kerstin Voigt, Hans-Martin Dahse, Axel Brakhage, Svenja Beckmann, Thomas Quack, Christoph G Grevelding, Anthony B Pinkerton, Bruno Schönecker, Jeremy Burrows, Elisabeth Davioud-Charvet, Stefan Rahlfs, Katja Becker
In search of antiparasitic agents, we here identify arylmethylamino steroids as potent compounds and characterize more than 60 derivatives. The lead compound 1o is fast acting and highly active against intraerythrocytic stages of chloroquine-sensitive and resistant Plasmodium falciparum parasites (IC50 1-5 nM) as well as against gametocytes. In P. berghei-infected mice, oral administration of 1o drastically reduces parasitaemia and cures the animals. Furthermore, 1o efficiently blocks parasite transmission from mice to mosquitoes...
February 17, 2017: Nature Communications
https://www.readbyqxmd.com/read/28207781/absence-of-genotoxic-effects-of-the-chalcone-e-1-2-hydroxyphenyl-3-4-methylphenyl-prop-2-en-1-one-and-its-potential-chemoprevention-against-dna-damage-using-in-vitro-and-in-vivo-assays
#3
Débora Cristina da Silva Lima, Camila Regina do Vale, Jefferson Hollanda Véras, Aline Bernardes, Caridad Noda Pérez, Lee Chen-Chen
The chalcone (E)-1-(2-hydroxyphenyl)-3-(4-methylphenyl)-prop-2-en-1-one), or 2HMC, displays antileishmanial, antimalarial, and antioxidant activities. The aim of this study was to investigate the cytotoxic, genotoxic, mutagenic, and protective effects of 2HMC using the Ames mutagenicity test, the mouse bone marrow micronucleus test, and the comet assay in mice. In the assessment using the Ames test, 2HMC did not increase the number of His+ revertants in Salmonella typhimurium strains, demonstrating lack of mutagenicity...
2017: PloS One
https://www.readbyqxmd.com/read/28197691/the-medicinal-and-pharmaceutical-importance-of-dendrobium-species
#4
REVIEW
Jaime A Teixeira da Silva, Tzi Bun Ng
Plants of the Dendrobium genus, one of the largest in the Orchidaceae, manifest a diversity of medicinal effects encompassing antiangiogenic, immunomodulating, antidiabetic, cataractogenesis-inhibiting, neuroprotective, hepatoprotective, anti-inflammatory, antiplatelet aggregation, antifungal, antibacterial, antiherpetic, antimalarial, aquaporin-5 stimulating, and hemagglutininating activities and also exert beneficial actions on colonic health and alleviate symptoms of hyperthyroidism. The active principles include a wide range of proteinaceous and non-proteinaceous molecules...
February 14, 2017: Applied Microbiology and Biotechnology
https://www.readbyqxmd.com/read/28193646/simplified-reversed-chloroquines-to-overcome-malaria-resistance-to-quinoline-based-drugs
#5
Bornface Gunsaru, Steven J Burgess, Westin Morrill, Jane X Kelly, Shawheen Shomloo, Martin J Smilkstein, Katherine Liebmann, David H Peyton
Building on our earlier work of attaching a chemosensitizer (reversal agent) to a known drug pharmacophore, we have now expanded the structure-activity relationship study to include simplified versions of the chemosensitizer. The change from two aromatic rings in this head group to a single ring, in fact, does not appear to detrimentally affect the antimalarial activity of the compounds. Data from in vitro heme binding and β-hematin inhibition assays suggest that the single aromatic RCQ compounds retain similar activities against P...
February 13, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28192202/ethnomedicinal-uses-of-plants-for-the-treatment-of-malaria-in-soon-valley-khushab-pakistan
#6
Amin Shah, Sarvat Rahim
ETHNOPHARMACOLOGICAL RELEVANCE: To best of our knowledge this is the first quantitative ethno-medicinal study with the aim of documenting the indigenous knowledge and practices of using plants for malarial therapy in Soon Valley, Khushab, Pakistan. In this Valley, malaria is among the major public health problems but, until now, the population still mostly relies on herbal medicine for treatment. MATERIALS AND METHODS: Ethno-medicinal data were documented from 63 informants by using semi-structured questionnaires and interviewing the informants about their knowledge of plants regarding malaria and related symptoms...
February 10, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28188731/design-in-silico-and-in-vitro-evaluation-of-curcumin-analogues-against-plasmodium-falciparum
#7
Chandrajit Dohutia, Dipak Chetia, Kabita Gogoi, Kishore Sarma
The polyphenolic compound curcumin has been reported for its antimalarial properties in various scientific studies. Plasmodium falciparum ATP6, the parasite orthologue of mammalian sarcoplasmic Ca(2+) ATPase (SERCA) has been identified as a key molecular target of both artemisinin and curcumin. The work was thereby undertaken to study the anti-malarial properties of two different series of curcumin analogues based on their docking interactions with PfATP6 and correlating the results with their anti-malarial activity...
February 7, 2017: Experimental Parasitology
https://www.readbyqxmd.com/read/28183236/antimalarial-antiplasmodial-and-analgesic-activities-of-root-extract-of-alchornea-laxiflora
#8
Jude E Okokon, Nkemnele Bensella Augustine, Dinesh Mohanakrishnan
CONTEXT: Alchornea laxiflora (Benth.) Pax. & Hoffman (Euphorbiaceae) root decoctions are traditionally used in the treatment of malaria and pain in Nigeria. OBJECTIVE: To assess the antimalarial, antiplasmodial and analgesic potentials of root extract and fractions against malarial infections and chemically-induced pains. MATERIAL AND METHODS: The root extract and fractions of Alchornea laxiflora were investigated for antimalarial activity against Plasmodium berghei infection in mice, antiplasmodial activity against chloroquine sensitive (Pf 3D7) and resistant (Pf INDO) strains of Plasmodium falciparum using SYBR green assay method and analgesic activity against experimentally-induced pain models...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/28183182/a-redox-active-fluorescent-ph-indicator-for-detecting-plasmodium-falciparum-strains-with-reduced-responsiveness-to-quinoline-antimalarial-drugs
#9
Mouhamad Jida, Cecilia P Sanchez, Karène Urgin, Katharina Ehrhardt, Saravanan Mounien, Aurelia Geyer, Mourad Elhabiri, Michael Lanzer, Elisabeth Davioud-Charvet
Mutational changes in the Plasmodium falciparum chloroquine resistance transporter (PfCRT) have been associated with differential responses to a wide spectrum of biologically active compounds including current and former quinoline and quinoline-like antimalarial drugs. PfCRT confers altered drug responsiveness by acting as a transport system, expelling drugs from the parasite's digestive vacuole where these drugs exert, at least part of, their antiplasmodial activity. To preserve the efficacy of these invaluable drugs, novel functional tools are required for epidemiological surveys of parasite strains carrying mutant PfCRT variants and for drug development programs aimed at inhibiting or circumventing the action of PfCRT...
February 10, 2017: ACS Infectious Diseases
https://www.readbyqxmd.com/read/28181563/the-antimicrobial-molecule-trappin-2-elafin-has-anti-parasitic-properties-and-is-protective-in-vivo-in-a-murine-model-of-cerebral-malaria
#10
Christian Roussilhon, Gilles Bang, Fabien Bastaert, Brigitte Solhonne, Ignacio Garcia-Verdugo, Roger Peronet, Pierre Druilhe, Anavaj Sakuntabhai, Salaheddine Mecheri, Jean-Michel Sallenave
According to the WHO, and despite reduction in mortality rates, there were an estimated 438 000 malaria deaths in 2015. Therefore new antimalarials capable of limiting organ damage are still required. We show that systemic and lung adenovirus (Ad)-mediated over-expression of trappin-2 (T-2) an antibacterial molecule with anti-inflammatory activity, increased mice survival following infection with the cerebral malaria-inducing Plasmodium berghei ANKA (PbANKA) strain. Systemically, T-2 reduced PbANKA sequestration in spleen, lung, liver and brain, associated with a decrease in pro-inflammatory cytokines (eg TNF-α in spleen and lung) and an increase in IL-10 production in the lung...
February 9, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28178359/the-malaria-parasite-s-lactate-transporter-pffnt-is-the-target-of-antiplasmodial-compounds-identified-in-whole-cell-phenotypic-screens
#11
Sanduni V Hapuarachchi, Simon A Cobbold, Sarah H Shafik, Adelaide S M Dennis, Malcolm J McConville, Rowena E Martin, Kiaran Kirk, Adele M Lehane
In this study the 'Malaria Box' chemical library comprising 400 compounds with antiplasmodial activity was screened for compounds that perturb the internal pH of the malaria parasite, Plasmodium falciparum. Fifteen compounds induced an acidification of the parasite cytosol. Two of these did so by inhibiting the parasite's formate nitrite transporter (PfFNT), which mediates the H+-coupled efflux from the parasite of lactate generated by glycolysis. Both compounds were shown to inhibit lactate transport across the parasite plasma membrane, and the transport of lactate by PfFNT expressed in Xenopus laevis oocytes...
February 2017: PLoS Pathogens
https://www.readbyqxmd.com/read/28178358/substrate-analogous-inhibitors-exert-antimalarial-action-by-targeting-the-plasmodium-lactate-transporter-pffnt-at-nanomolar-scale
#12
André Golldack, Björn Henke, Bärbel Bergmann, Marie Wiechert, Holger Erler, Alexandra Blancke Soares, Tobias Spielmann, Eric Beitz
Resistance against all available antimalarial drugs calls for novel compounds that hit unexploited targets in the parasite. Here, we show that the recently discovered Plasmodium falciparum lactate/proton symporter, PfFNT, is a valid druggable target, and describe a new class of fluoroalkyl vinylogous acids that potently block PfFNT and kill cultured parasites. The original compound, MMV007839, is derived from the malaria box collection of potent antimalarials with unknown targets and contains a unique internal prodrug principle that reversibly switches between a lipophilic transport form and a polar, substrate-analogous active form...
February 2017: PLoS Pathogens
https://www.readbyqxmd.com/read/28178218/intramolecular-hydrogen-bonds-in-conformers-of-quinine-and-quinidine-an-hf-mp2-and-dft-study
#13
Mireille K Bilonda, Liliana Mammino
Quinine is an alkaloid with powerful antimalarial activity, isolated from the bark of Peru's cinchona trees. Quinidine is an erythro diastereoisomer of quinine also exhibiting antimalarial activity. Conformational studies performed so far had never identified conformers with intramolecular hydrogen bonds (IHB). The current study shows the possibility of conformers with an IHB between the quinuclidine and quinoline moieties of these molecules. The study was performed at different levels of theory: Hartree Fock (HF) with the 6-31G(d,p) basis set, Density Functional Theory (DFT) with the B3LYP functional and the 6-31+G(d,p) basis set and Møller-Plesset Perturbation Theory (MP2) with the 6-31+G(d,p) basis set, to confirm the results...
February 7, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28176804/griseofulvin-impairs-intraerythrocytic-growth-of-plasmodium-falciparum-through-ferrochelatase-inhibition-but-lacks-activity-in-an-experimental-human-infection-study
#14
Clare M Smith, Ante Jerkovic, Thy Thuc Truong, Simon J Foote, James S McCarthy, Brendan J McMorran
Griseofulvin, an orally active antifungal drug used to treat dermatophyte infections, has a secondary effect of inducing cytochrome P450-mediated production of N-methyl protoporphyrin IX (N-MPP). N-MPP is a potent competitive inhibitor of the heme biosynthetic-enzyme ferrochelatase, and inhibits the growth of cultured erythrocyte stage Plasmodium falciparum. Novel drugs against Plasmodium are needed to achieve malaria elimination. Thus, we investigated whether griseofulvin shows anti-plasmodial activity. We observed that the intraerythrocytic growth of P...
February 8, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28173854/anti-influenza-virus-activity-of-extracts-from-the-stems-of-jatropha-multifida-linn-collected-in-myanmar
#15
Masaki Shoji, So-Yeun Woo, Aki Masuda, Nwet Nwet Win, Hla Ngwe, Etsuhisa Takahashi, Hiroshi Kido, Hiroyuki Morita, Takuya Ito, Takashi Kuzuhara
BACKGROUND: To contribute to the development of novel anti-influenza drugs, we investigated the anti-influenza activity of crude extracts from 118 medicinal plants collected in Myanmar. We discovered that extract from the stems of Jatropha multifida Linn. showed anti-influenza activity. J. multifida has been used in traditional medicine for the treatment of various diseases, and the stem has been reported to possess antimicrobial, antimalarial, and antitumor activities. However, the anti-influenza activity of this extract has not yet been investigated...
February 7, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28171830/a-review-on-antioxidant-potential-of-bioactive-heterocycle-benzofuran-natural-and-synthetic-derivatives
#16
REVIEW
Karam Chand, Rajeshwari, Asha Hiremathad, Mahak Singh, M Amelia Santos, Rangappa S Keri
The majority of heterocycle compounds and typically common heterocycle fragments present in most pharmaceuticals currently marketed, alongside with their intrinsic versatility and unique physicochemical properties, have poised them as true cornerstones of medicinal chemistry. In this context, oxygen heterocycles exhibit diverse biological and pharmacological activities due in part to the similarities with many natural and synthetic molecules with known biological activity. Among oxygen containing heterocycles, benzofuran (synthetic and natural isolated) and its derivatives have attracted medicinal chemists and pharmacologists due to their pronounced biological activities and their potential applications as pharmacological agents such as antioxidant, antitumor, antiplatelet, antimalarial, antiinflammatory, antidepressant and anticonvulsant properties...
November 18, 2016: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28167052/heme-binding-activity-of-methoxyflavones-from-pentzia-monodiana-maire-asteraceae
#17
Sergio Ortiz, Kamel Dali-Yahia, Pedro Vasquez-Ocmin, Raphaël Grougnet, Philippe Grellier, Sylvie Michel, Alexandre Maciuk, Sabrina Boutefnouchet
A heme-binding assay based on mass spectrometry was performed on P. monodiana Maire (Asteraceae) extracts to identify metabolites able to form adducts with heminic part of haemoglobin, as potential antimalarial drugs. Main adducts were characterized and their stability was measured. Isolation of main constituents of P. monodiana Maire lead to identification of the two methoxyflavones 3'-O-methyleupatorin (7) and artemetin (8) involved in the adducts formation. Four seco-tanapartholides (1-4), a guaianolide (5), a germacranolide (6) and two other methoxyflavones (9, 10) were also characterized...
February 3, 2017: Fitoterapia
https://www.readbyqxmd.com/read/28160850/in-vitro-and-in-vivo-antimalarial-potential-of-oleoresin-obtained-from-copaifera-reticulata-ducke-fabaceae-in-the-brazilian-amazon-rainforest
#18
Giovana A G de Souza, Nazaré C da Silva, Juarez de Souza, Karen R M de Oliveira, Amanda L da Fonseca, Leopoldo C Baratto, Elaine C P de Oliveira, Fernando de Pilla Varotti, Waldiney P Moraes
BACKGROUND: In view of the wide variety of the flora of the Amazon region, many plants have been studied in the search for new antimalarial agents. Copaifera reticulata is a tree distributed throughout the Amazon region which contains an oleoresin rich in sesquiterpenes and diterpenes with β-caryophyllene as the major compound. The oleoresin has demonstrated antiparasitic activity against Leishmania amazonensis. Because of this previously reported activity, this oleoresin would be expected to also have antimalarial activity...
January 15, 2017: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/28155287/primary-health-workers-knowledge-and-practices-relating-to-neonatal-jaundice-in-ibadan-nigeria
#19
Adebola E Orimadegun, Adeola O Ojebiyi
BACKGROUND: Over half of births and newborn care occur in primary healthcare facilities in Nigeria, but information on activities of personnel working there is scarce. AIM: To assess the knowledge and practices relating to neonatal jaundice (NNJ) among community health workers (CHWs) and community birth attendants (CBAs) in Nigeria. SETTING: We conducted a cross-sectional survey of all 227 CHWs and 193 registered CBAs in Ibadan, Nigeria...
January 30, 2017: African Journal of Primary Health Care & Family Medicine
https://www.readbyqxmd.com/read/28146408/the-antimalarial-effect-of-curcumin-is-mediated-by-the-inhibition-of-glycogen-synthase-kinase-3%C3%AE
#20
Amatul Hamizah Ali, Suhaini Sudi, Rusliza Basir, Noor Embi, Hasidah Mohd Sidek
Curcumin, a bioactive compound in Curcuma longa, exhibits various pharmacological activities, including antimalarial effects. In silico docking simulation studies suggest that curcumin possesses glycogen synthase kinase-3β (GSK3β)-inhibitory properties. The involvement of GSK3 in the antimalarial effects in vivo is yet to be demonstrated. In this study, we aimed to evaluate whether the antimalarial effects of curcumin involve phosphorylation of host GSK3β. Intraperitoneal administration of curcumin into Plasmodium berghei NK65-infected mice resulted in dose-dependent chemosuppression of parasitemia development...
February 2017: Journal of Medicinal Food
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