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antimalarial activity

Abdul Hameed, Mariya Al-Rashida, Maliha Uroos, Syed Ali, Khalid M Khan
Schiff bases are synthetically accessible and structurally diverse compounds, typically obtained by facile condensation between an aldehyde, or a ketone with primary amines. Schiff bases contain an azomethine (-C=N-) linkage that stitches together two or more biologically active aromatic/heterocyclic scaffolds to form various molecular hybrids with interesting biological properties. Schiff bases are versatile metal complexing agents and have been known to coordinate all metals to form stable metal complexes with vast therapeutic applications...
October 24, 2016: Expert Opinion on Therapeutic Patents
Christiana M Adeyemi, Faridoon, Michelle Isaacs, Dumisani Mnkandhla, Heinrich C Hoppe, Rui W M Krause, Perry T Kaye
A series of novel and readily accessible N-benzylated (N-arylcarbamoyl)alkylphosphonate esters and related compounds have been prepared as potential antimalarial agents. Bioassays reveal that some of these compounds exhibit promising activity against Plasmodium falciparum, and exhibit no significant growth inhibition of HeLa cells.
April 9, 2016: Bioorganic & Medicinal Chemistry
Kristina R Kesely, Antonella Pantaleo, Francesco M Turrini, Peter Olupot-Olupot, Philip S Low
With half of the world's population at risk for malaria infection and with drug resistance on the rise, the search for mutation-resistant therapies has intensified. We report here a therapy for Plasmodium falciparum malaria that acts by inhibiting the phosphorylation of erythrocyte membrane band 3 by an erythrocyte tyrosine kinase. Because tyrosine phosphorylation of band 3 causes a destabilization of the erythrocyte membrane required for parasite egress, inhibition of the erythrocyte tyrosine kinase leads to parasite entrapment and termination of the infection...
2016: PloS One
Yuan-Bo Wu, Li Zhang, Wen-Ting Li, Yi Yang, Jiang-Ming Zhao
BACKGROUND: Artesunate (ART) is an antimalarial drug with potential anti-inflammatory effect. This study aimed to explore the potential protective role of ART in hepatic encephalopathy (HE), involving its function against ammonia toxicity. METHODS: HE rats were induced by the administration of thioacetamide (TAA, 300mg/kg/day). Spatial learning ability was tested in both Morris water and eight-arm radial maze. Rat cerebellar granule neurons (CGNs) were prepared for ammonia treatment in vitro, in line with SH-SY5Y and C6 cells...
October 17, 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Aditi A Sidhaye, Kanchan C Bhuran, Sneha Zambare, Munna Abubaker, Niroshini Nirmalan, Kamalinder K Singh
AIM: The intra-erythrocytic development of the malarial parasite is dependent on active uptake of nutrients, including human serum albumin (HSA), into parasitized red blood cells (pRBCs). We have designed HSA-based nanoparticles as a potential drug-delivery option for antimalarials. METHODS: Artemether-loaded nanoparticles (AANs) were designed and antimalarial activity evaluated in vitro/in vivo using Plasmodium falciparum/Plasmodium berghei species, respectively...
October 19, 2016: Nanomedicine
Bishnu Joshi, Sarah Hendrickx, Lila Bahadur Magar, Niranjan Parajuli, Pierre Dorny, Louis Maes
BACKGROUND: Nepal is very rich in biodiversity, and no extensive effort has yet been carried out to screen plants that are used by traditional healers against parasitic diseases. The aim of this study was to evaluate the in vitro antileishmanial and antimalarial activity of crude methanolic or ethanolic extracts of 29 plant species that are currently used by local people of Nepal for treating different ailments. METHODS: Crude extracts of leaves, twigs, aerial parts, and/or roots of the selected plants were evaluated for in vitro inhibitory activity against intracellular amastigotes of Leishmania infantum and against erythrocytic stages of Plasmodium falciparum...
September 2016: Journal of Intercultural Ethnopharmacology
Luís Felipe S P Azeredo, Julia P Coutinho, Valquiria A P Jabor, Patricia R Feliciano, Maria Cristina Nonato, Carlos R Kaiser, Carla Maria S Menezes, Amanda S O Hammes, Ernesto Raul Caffarena, Lucas V B Hoelz, Nicolli B de Souza, Glaécia A N Pereira, Isabela P Cerávolo, Antoniana U Krettli, Nubia Boechat
Malaria remains one of the most serious global infectious diseases. An important target for antimalarial chemotherapy is the enzyme dihydroorotate dehydrogenase from Plasmodium falciparum (PfDHODH), which is responsible for the conversion of dihydroorotate to orotate in the de novo pyrimidine biosynthetic pathway. In this study, we have designed and synthesized fifteen 7-arylpyrazolo[1,5-a]pyrimidine derivatives using ring bioisosteric replacement and molecular hybridization of functional groups based on the highly active 5-methyl-N-(naphthalen-2-yl)-2-(trifluoromethyl)- [1,2,4]triazolo[1,5-a]pyrimidin-7-amine...
September 30, 2016: European Journal of Medicinal Chemistry
Alexandre Y Saito, Adriana A Marin Rodriguez, Danielle S Menchaca Vega, Rodrigo A C Sussmann, Emília A Kimura, Alejandro M Katzin
Malaria, an infectious disease that kills more than 438,000 people per year worldwide, is a major public health problem. The emergence of strains resistant to conventional therapeutic agents necessitates the discovery of new drugs. We previously demonstrated that various substances, including terpenes, have antimalarial activity in vitro and in vivo. Nerolidol is a sesquiterpene present as an essential oil in several plants that is used in scented products and has been approved by the US Food and Drug Administration as a food-flavouring agent...
September 30, 2016: International Journal of Antimicrobial Agents
Dene R Littler, Hayley E Bullen, Katherine L Harvey, Travis Beddoe, Brendan S Crabb, Jamie Rossjohn, Paul R Gilson
The ubiquitous second messenger cAMP mediates signal transduction processes in the malarial parasite that regulate host erythrocyte invasion and the proliferation of merozoites. In Plasmodium falciparum the central receptor for cAMP is the single regulatory subunit (R) of Protein kinase A (PKA). To aid the development of compounds that can selectively dysregulate parasite PKA signalling we solved the structure of the PKA regulatory subunit in complex with cAMP and a related analog that displays antimalarial activity: Sp-2Cl-cAMPS...
October 13, 2016: Journal of Biological Chemistry
Anju Singh, Mudasir Maqbool, Mohammad Mobashir, Nasimul Hoda
Malaria is a critical human disease with extensive exploration yet unestablished due to occurrence of frequent drug resistance. This aspect of malaria pharmacology calls for the introduction of new antimalarial. The drugs reported till date targeted different stages of the parasites in order to stop their growth and proliferation. Beside this, various drugs that could inhibit the imperative enzymes of the parasite have also been reported. Amid them, dihydroorotate dehydrogenase (DHODH) has a key worth. DHODH is involved in the de novo pyrimidine biosynthesis of the malarial parasite which acts as a primary source of energy for its survival...
September 27, 2016: European Journal of Medicinal Chemistry
Tomoyo Sakata-Kato, Dyann F Wirth
Given that resistance to all drugs in clinical use has arisen, discovery of new anti-malarial drug targets is eagerly anticipated. The Plasmodium mitochondrion has been considered a promising drug target largely based on its significant divergence from the host organelle as well as its involvement in ATP production and pyrimidine biosynthesis. However, the functions of Plasmodium mitochondrial protein complexes and associated metabolic pathways are not fully characterized. Here, we report the development of novel and robust bioenergetic assay protocols for Plasmodium falciparum asexual parasites utilizing a Seahorse Bioscience XFe24 Extracellular Flux Analyzer...
October 9, 2016: ACS Infectious Diseases
Miguel Quiliano, Adela Mendoza, Kim Y Fong, Adriana Pabón, Nathan E Goldfarb, Isabelle Fabing, Ariane Vettorazzi, Adela López de Cerain, Ben M Dunn, Giovanny Garavito, David W Wright, Eric Deharo, Silvia Pérez-Silanes, Ignacio Aldana, Silvia Galiano
Synthesis of new 1-aryl-3-substituted propanol derivatives followed by structure-activity relationship, in silico drug-likeness, cytotoxicity, genotoxicity, in silico metabolism, in silico pharmacophore modeling, and in vivo studies led to the identification of compounds 22 and 23 with significant in vitro antiplasmodial activity against drug sensitive (D6 IC50 ≤ 0.19 μM) and multidrug resistant (FCR-3 IC50 ≤ 0.40 μM and C235 IC50 ≤ 0.28 μM) strains of Plasmodium falciparum. Adequate selectivity index and absence of genotoxicity was also observed...
September 28, 2016: International Journal for Parasitology, Drugs and Drug Resistance
Amélie Le Bihan, Ruben de Kanter, Iñigo Angulo-Barturen, Christoph Binkert, Christoph Boss, Reto Brun, Ralf Brunner, Stephan Buchmann, Jeremy Burrows, Koen J Dechering, Michael Delves, Sonja Ewerling, Santiago Ferrer, Christoph Fischli, Francisco Javier Gamo-Benito, Nina F Gnädig, Bibia Heidmann, María Belén Jiménez-Díaz, Didier Leroy, Maria Santos Martínez, Solange Meyer, Joerg J Moehrle, Caroline L Ng, Rintis Noviyanti, Andrea Ruecker, Laura María Sanz, Robert W Sauerwein, Christian Scheurer, Sarah Schleiferboeck, Robert Sinden, Christopher Snyder, Judith Straimer, Grennady Wirjanata, Jutta Marfurt, Ric N Price, Thomas Weller, Walter Fischli, David A Fidock, Martine Clozel, Sergio Wittlin
BACKGROUND: Artemisinin resistance observed in Southeast Asia threatens the continued use of artemisinin-based combination therapy in endemic countries. Additionally, the diversity of chemical mode of action in the global portfolio of marketed antimalarials is extremely limited. Addressing the urgent need for the development of new antimalarials, a chemical class of potent antimalarial compounds with a novel mode of action was recently identified. Herein, the preclinical characterization of one of these compounds, ACT-451840, conducted in partnership with academic and industrial groups is presented...
October 2016: PLoS Medicine
Ari Polachek, Dafna D Gladman, Jiandong Su, Murray B Urowitz
OBJECTIVES: To define and identify a group of SLE patients with low disease activity (LDA) and to examine whether it is similar to patients in remission and different from a high disease activity group (HDA) in short term outcomes. METHODS: LDA group was defined as Systemic Lupus Erythematosus Disease Activity Index (SLEDAI-2K) <3 including only 1 clinical manifestation of: rash, alopecia, mucosal ulcers, pleurisy, pericarditis, fever, thrombocytopenia or leukopenia...
October 1, 2016: Arthritis Care & Research
Uchechukwu M Chukwuocha, Omar Fernández-Rivera, Martha Legorreta-Herrera
ETHNOPHARMACOLOGICAL RELEVANCE: Cymbopogon citratus (lemon grass) has been used in traditional medicine as an herbal infusion to treat fever and malaria. Generally, whole plant extracts possess higher biological activity than purified compounds. However, the antimalarial activity of the whole C. citratus plant has not been experimentally tested. AIM OF THE STUDY: To evaluate the antimalarial activity of an herbal infusion and the whole Cymbopogon citratus plant in two experimental models of malaria...
September 29, 2016: Journal of Ethnopharmacology
Nicolas Chopin, Shinya Iikawa, Julien Bosson, Adeline Lavoignat, Guillaume Bonnot, Anne-Lise Bienvenu, Stéphane Picot, Jean-Philippe Bouillon, Maurice Médebielle
In this Letter we report on an efficient and short 2-3 steps synthesis of γ-hydroxy-γ-lactam derived-tetramates bearing a 7-chloro-4-aminoquinoline skeleton and their evaluation as potent antimalarials. These molecules were obtained through ring opening-ring closure (RORC) process of γ-ylidene-tetronate derivatives in the presence of 7-chloro-4-aminoquinoline-derived amines. In vitro antimalarial activity of these new γ-lactams was evaluated against Plasmodium falciparum clones of variable sensitivity (3D7 and W2) and they were found to be active in the range of 14-827nM with generally good resistance index...
September 15, 2016: Bioorganic & Medicinal Chemistry Letters
M Prieto-Barrios, M Castellanos-González, V Velasco-Tamariz, S Burillo-Martínez, C Morales-Raya, P Ortiz-Romero, Raquel Rivera-Diaz
Psoriasis and lupus erythematosus (LE) are immune-mediated diseases that rarely coexist. In a cohort study of 9420 patients with psoriasis just 0.45% had concomitant LE(1) . In addition to the difficulty of certain clinical overlap, therapeutic dilemmas arise when coming across these patients, as treatments that favor psoriasis can aggravate LE (e.g. ultraviolet light), or viceversa, (e.g. antimalarial drugs)(2) . Traditionally, psoriasis was related to Th1-cell activation whereas LE to Th2-cell-mediated immunity(3) ...
September 29, 2016: Journal of the European Academy of Dermatology and Venereology: JEADV
Oue-Artorn Rajachan, Kwanjai Kanokmedhakul, Wareerat Sanmanoch, Sophon Boonlue, Supa Hannongbua, Patchreenart Saparpakorn, Somdej Kanokmedhakul
Four meroterpenoids, 1-hydroxychevalone C, 1-acetoxychevalone C, 1,11-dihydroxychevalone C, and 11-hydroxychevalone C and two ester epimers, 2S,4S-spinosate and 2S,4R-spinosate, together with seven known compounds, chevalones B, C, and E, tryptoquivaline, nortryptoquivaline, tryptoquivaline L, and quinadoline A were isolated from the fungus Neosartorya spinosa. Their structures were established based on spectroscopic data analyses. The theoretical ECD spectra of epimers, 2S,4S-spinosate and 2S,4R-spinosate were calculated to support the experimental results of their CD spectra...
September 25, 2016: Phytochemistry
Gagandeep S Saggu, Zarna R Pala, Shilpi Garg, Vishal Saxena
The MEP (Methyl Erythritol Phosphate) isoprenoids biosynthesis pathway is an attractive drug target to combat malaria, due to its uniqueness and indispensability for the parasite. It is functional in the apicoplast of Plasmodium and its products get transported to the cytoplasm, where they participate in glycoprotein synthesis, electron transport chain, tRNA modification and several other biological processes. Several compounds have been tested against the enzymes involved in this pathway and amongst them Fosmidomycin, targeted against IspC (DXP reductoisomerase) enzyme and MMV008138 targeted against IspD enzyme have shown good anti-malarial activity in parasite cultures...
2016: Frontiers in Microbiology
Ingy I Abdallah, Magdalena Czepnik, Ronald van Merkerk, Wim J Quax
Amorphadiene synthase (ADS) is known for its vital role as a key enzyme in the biosynthesis of the antimalarial drug artemisinin. Despite the vast research targeting this enzyme, an X-ray crystal structure of the enzyme has not yet been reported. In spite of the remarkable difference in product profile among various sesquiterpene synthases, they all share a common α-helical fold with many highly conserved regions especially the bivalent metal ion binding motifs. Hence, to better understand the structural basis of the mechanism of ADS, a reliable 3D homology model representing the conformation of the ADS enzyme and the position of its substrate, farnesyl diphosphate, in the active site was constructed...
September 27, 2016: Journal of Natural Products
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