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Malaria drug resistance

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https://www.readbyqxmd.com/read/28728898/kbe009-an-antimalarial-bestatin-like-inhibitor-of-the-plasmodium-falciparum-m1-aminopeptidase-discovered-in-an-ugi-multicomponent-reaction-derived-peptidomimetic-library
#1
Jorge González-Bacerio, Sarah El Chamy Maluf, Yanira Méndez, Isel Pascual, Isabelle Florent, Pollyana M S Melo, Alexandre Budu, Juliana C Ferreira, Ernesto Moreno, Adriana K Carmona, Daniel G Rivera, Maday Alonso Del Rivero, Marcos L Gazarini
Malaria is a global human parasitic disease mainly caused by the protozoon Plasmodium falciparum. Increased parasite resistance to current drugs determines the relevance of finding new treatments against new targets. A novel target is the M1 alanyl-aminopeptidase from P. falciparum (PfA-M1), which is essential for parasite development in human erythrocytes and is inhibited by the pseudo-peptide bestatin. In this work, we used a combinatorial multicomponent approach to produce a library of peptidomimetics and screened it for the inhibition of recombinant PfA-M1 (rPfA-M1) and the in vitro growth of P...
July 4, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28724415/identification-and-characterization-of-the-antiplasmodial-activity-of-hsp90-inhibitors
#2
Claribel Murillo-Solano, Chunmin Dong, Cecilia G Sanchez, Juan C Pizarro
BACKGROUND: The recent reduction in mortality due to malaria is being threatened by the appearance of Plasmodium falciparum parasites that are resistant to artemisinin in Southeast Asia. To limit the impact of resistant parasites and their spread across the world, there is a need to validate anti-malarial drug targets and identify new leads that will serve as foundations for future drug development programmes targeting malaria. Towards that end, the antiplasmodial potential of several Hsp90 inhibitors was characterized...
July 19, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28724354/novel-plasmodium-falciparum-metabolic-network-reconstruction-identifies-shifts-associated-with-clinical-antimalarial-resistance
#3
Maureen A Carey, Jason A Papin, Jennifer L Guler
BACKGROUND: Malaria remains a major public health burden and resistance has emerged to every antimalarial on the market, including the frontline drug, artemisinin. Our limited understanding of Plasmodium biology hinders the elucidation of resistance mechanisms. In this regard, systems biology approaches can facilitate the integration of existing experimental knowledge and further understanding of these mechanisms. RESULTS: Here, we developed a novel genome-scale metabolic network reconstruction, iPfal17, of the asexual blood-stage P...
July 19, 2017: BMC Genomics
https://www.readbyqxmd.com/read/28723116/integrated-magnetic-bead-quantum-dot-immunoassay-for-malaria-detection
#4
Chloe Kim, Gwendolyn Hoffmann, Peter C Searson
Malaria persists as a disease of high morbidity and mortality due to improper diagnosis, overuse of drugs, rapidly evolving drug resistant parasites, and poor disease monitoring. The two common tests used in developing countries, microscopic examination of Glemsa slides and rapid diagnostic tests (RDTs), have limitations associated with variability in specificity and sensitivity, and qualitative outcome. Here we report on an immunoassay using magnetic beads for capture and quantum dots for detection of histidine-rich protein 2 (HRP2)...
June 23, 2017: ACS Sensors
https://www.readbyqxmd.com/read/28720134/in-vitro-antioxidant-and-antimalarial-activities-of-leaves-pods-and-bark-extracts-of-acacia-nilotica-l-del
#5
Muhammad Bilal Sadiq, Pattamon Tharaphan, Kesinee Chotivanich, Joel Tarning, Anil Kumar Anal
BACKGROUND: The emergence of drug resistant malaria is threatening our ability to treat and control malaria in the Southeast Asian region. There is an urgent need to develop novel and chemically diverse antimalarial drugs. This study aimed at evaluating the antimalarial and antioxidant potentials of Acacia nilotica plant extracts. METHODS: The antioxidant activities of leaves, pods and bark extracts were determined by standard antioxidant assays; reducing power capacity, % lipid peroxidation inhibition and ferric reducing antioxidant power assay...
July 18, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28711439/updates-on-k13-mutant-alleles-for-artemisinin-resistance-in-plasmodium-falciparum
#6
REVIEW
Myo Thura Zaw, Nor Amalina Emran, Zaw Lin
BACKGROUND: In the fight against malaria caused by Plasmodium falciparum, the successes achieved by artemisinin were endangered by resistance of the parasites to the drug. Whole genome sequencing approach on artemisinin resistant parasite line discovered k13 gene associated with drug resistance. In vitro and in vivo studies indicated mutations in the k13 gene were linked to the artemisinin resistance. METHODOLOGY: The literatures published after April, 2015 up to December, 2016 on k13 mutant alleles for artemisinin resistance in Plasmodium falciparum and relevant literatures were comprehensively reviewed...
June 29, 2017: Journal of Microbiology, Immunology, and Infection, Wei Mian Yu Gan Ran za Zhi
https://www.readbyqxmd.com/read/28710808/the-application-of-physiologically-based-pharmacokinetic-modelling-to-assess-the-impact-of-antiretroviral-mediated-drug-drug-interactions-on-piperaquine-antimalarial-therapy-during-pregnancy
#7
Olusola Olafuyi, Michael Coleman, Raj K S Badhan
Antimalarial therapy during pregnancy poses important safety concerns due to potential teratogenicity and maternal physiological and biochemical changes during gestation. Piperaquine (PQ) has gained interest for use in pregnancy in response to increasing resistance towards sulfadoxine-pyrimethamine in sub-Saharan Africa. Co-infection with HIV is common in many developing countries, however, little is known about the impact of anti-retroviral (ARV) mediated drug-drug interaction (DDI) on PQ pharmacokinetics during pregnancy...
July 14, 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28705249/vector-control-with-driving-y-chromosomes-modelling-the-evolution-of-resistance
#8
Andrea Beaghton, Pantelis John Beaghton, Austin Burt
BACKGROUND: The introduction of new malaria control interventions has often led to the evolution of resistance, both of the parasite to new drugs and of the mosquito vector to new insecticides, compromising the efficacy of the interventions. Recent progress in molecular and population biology raises the possibility of new genetic-based interventions, and the potential for resistance to evolve against these should be considered. Here, population modelling is used to determine the main factors affecting the likelihood that resistance will evolve against a synthetic, nuclease-based driving Y chromosome that produces a male-biased sex ratio...
July 14, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28695570/population-pharmacokinetics-and-electrocardiographic-effects-of-dihydroartemisinin-piperaquine-in-healthy-volunteers
#9
Palang Chotsiri, Thanaporn Wattanakul, Richard Hoglund, Borimas Hanboonkunupakarn, Sasithon Pukrittayakamee, Daniel Blessborn, Podjanee Jittamala, Nicholas J White, Nicholas P J Day, Joel Tarning
AIMS: The aims of the presented study were to evaluate the pharmacokinetic properties of dihydroartemisinin and piperaquine, potential drug-drug interactions with concomitant primaquine treatment, and piperaquine effects on the electrocardiogram in healthy volunteers. METHODS: Population pharmacokinetic properties of dihydroartemisinin and piperaquine were assessed in 16 in healthy Thai adults using an open-label randomized crossover study. Drug concentration-time data and electrocardiographic measurements were evaluated with nonlinear mixed-effects modelling...
July 11, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28693552/chloroquine-efficacy-for-plasmodium-vivax-in-myanmar-in-populations-with-high-genetic-diversity-and-moderate-parasite-gene-flow
#10
Myo Win Htun, Nan Cho Nwe Mon, Khin Myo Aye, Chan Myae Hlaing, Myat Phone Kyaw, Irene Handayuni, Hidayat Trimarsanto, Dorina Bustos, Pascal Ringwald, Ric N Price, Sarah Auburn, Kamala Thriemer
BACKGROUND: Plasmodium vivax malaria remains a major public health burden in Myanmar. Resistance to chloroquine (CQ), the first-line treatment for P. vivax, has been reported in the country and has potential to undermine local control efforts. METHODS: Patients over 6 years of age with uncomplicated P. vivax mono-infection were enrolled into clinical efficacy studies in Myawaddy in 2014 and Kawthoung in 2012. Study participants received a standard dose of CQ (25 mg/kg over 3 days) followed by weekly review until day 28...
July 10, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28693488/donor-support-for-quality-assurance-and-pharmacovigilance-of-anti-malarials-in-malaria-endemic-countries
#11
Stephanie D Kovacs, Brianna M Mills, Andy Stergachis
BACKGROUND: Malaria control efforts have been strengthened by funding from donor groups and government agencies. The Global Fund to Fight AIDS, Tuberculosis and the Malaria (Global Fund), the US President's Malaria Initiative (PMI) account for the majority of donor support for malaria control and prevention efforts. Pharmacovigilance (PV), which encompasses all activities relating to the detection, assessment, understanding, and prevention of adverse effects or any other drug-related problem, is a necessary part of efforts to reduce drug resistance and improve treatment outcomes...
July 11, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28692943/progressive-increase-in-point-mutations-associates-chloroquine-resistance-even-after-withdrawal-of-chloroquine-use-in-india
#12
Sabyasachi Das, Satyajit Tripathy, Sourav Chattopadhayay, Balaram Das, Santanu Kar Mahapatra, Amiya Kumar Hati, Somenath Roy
Chloroquine (CQ) is highly effective against P. vivax, due to the rapid spread of CQ resistance in P. falciparum parasites; it is no longer the drug of choice against P. falciparum. This study elucidates the scenario of chloroquine efficacy at times that coincided with a new drug policy and especially assessed the chloroquine resistant molecular markers after withdrawal of chloroquine in Kolkata and Purulia, two malaria endemic zones of West Bengal, India. In vitro CQ susceptibility was tested in 781 patients with P...
June 29, 2017: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/28690382/qsar-based-predictive-modeling-for-anti-malarial-molecules
#13
Deepak R Bharti, Andrew M Lynn
Malaria is a predominant infectious disease, with a global footprint, but especially severe in developing countries in the African subcontinent. In recent years, drug-resistant malaria has become an alarming factor, and hence the requirement of new and improved drugs is more crucial than ever before. One of the promising locations for antimalarial drug target is the apicoplast, as this organelle does not occur in humans. The apicoplast is associated with many unique and essential pathways in many Apicomplexan pathogens, including Plasmodium...
2017: Bioinformation
https://www.readbyqxmd.com/read/28689867/ex-vivo-activity-of-proveblue-a-methylene-blue-against-field-isolates-of-plasmodium-falciparum-in-dakar-senegal-from-2013-2015
#14
Bécaye Fall, Marylin Madamet, Silman Diawara, Sébastien Briolant, Khalifa Ababacar Wade, Gora Lo, Aminata Nakoulima, Mansour Fall, Raymond Bercion, Mame Bou Kounta, Rémi Amalvict, Nicolas Benoit, Mamadou Wague Gueye, Bakary Diatta, Boubacar Wade, Bruno Pradines
Resistance to most antimalarial drugs has spread from Southeast Asia to Africa. Accordingly, new therapies to use with artemisinin-based combination therapy (triple ACT) are urgently needed. Proveblue, a methylene blue preparation, was found to exhibit antimalarial activity against Plasmodium falciparum strains in vitro. Proveblue has synergistic effects when used in combination with dihydroartemisinin, and has been shown to significantly reduce or prevent cerebral malaria in mice. The objectives of the current study were to evaluate the in vitro baseline susceptibility of clinical field isolates to Proveblue, compare its activity with that of other standard antimalarial drugs and define the patterns of cross-susceptibility between Proveblue and conventional antimalarial drugs...
July 6, 2017: International Journal of Antimicrobial Agents
https://www.readbyqxmd.com/read/28688800/protein-degradation-systems-as-antimalarial-therapeutic-targets
#15
REVIEW
Caroline L Ng, David A Fidock, Matthew Bogyo
Artemisinin (ART)-based combination therapies are the most efficacious treatment of uncomplicated Plasmodium falciparum malaria. Alarmingly, P. falciparum strains have acquired resistance to ART across much of Southeast Asia. ART creates widespread protein and lipid damage inside intraerythrocytic parasites, necessitating macromolecule degradation. The proteasome is the main engine of Plasmodium protein degradation. Indeed, proteasome inhibition and ART have shown synergy in ART-resistant parasites. Moreover, ubiquitin modification is associated with altered parasite susceptibility to multiple antimalarials...
July 5, 2017: Trends in Parasitology
https://www.readbyqxmd.com/read/28687086/ivermectin-susceptibility-and-sporontocidal-effect-in-greater-mekong-subregion-anopheles
#16
Kevin C Kobylinski, Ratawan Ubalee, Alongkot Ponlawat, Chanyapat Nitatsukprasert, Siriporn Phasomkulsolsil, Thanaporn Wattanakul, Joel Tarning, Kesara Na-Bangchang, Patrick W McCardle, Silas A Davidson, Jason H Richardson
BACKGROUND: Novel vector control methods that can directly target outdoor malaria transmission are urgently needed in the Greater Mekong Subregion (GMS) to accelerate malaria elimination and artemisinin resistance containment efforts. Ivermectin mass drug administration (MDA) to humans has been shown to effectively kill wild Anopheles and suppress malaria transmission in West Africa. Preliminary laboratory investigations were performed to determine ivermectin susceptibility and sporontocidal effect in GMS Anopheles malaria vectors coupled with pharmacokinetic models of ivermectin at escalating doses...
July 7, 2017: Malaria Journal
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
#17
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/28673348/anti-malarial-treatment-outcomes-in-ethiopia-a-systematic-review-and-meta-analysis
#18
Eyob Alemayehu Gebreyohannes, Akshaya Srikanth Bhagavathula, Mohammed Assen Seid, Henok Getachew Tegegn
BACKGROUND: Ethiopia is among countries with a high malaria burden. There are several studies that assessed the efficacy of anti-malarial agents in the country and this systematic review and meta-analysis was performed to obtain stronger evidence on treatment outcomes of malaria from the existing literature in Ethiopia. METHODS: A systematic literature search using the preferred reporting items for systematic review and meta-analysis (PRISMA) statement was conducted on studies from Pubmed, Google Scholar, and ScienceDirect databases to identify published and unpublished literature...
July 3, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28673299/efficacy-and-safety-evaluation-of-a-novel-trioxaquine-in-the-management-of-cerebral-malaria-in-a-mouse-model
#19
Onyango C Odhiambo, Hannah N Wamakima, Gabriel N Magoma, Peter G Kirira, Bonface J Malala, Francis T Kimani, Francis W Muregi
BACKGROUND: The emergence of multidrug-resistant strains of Plasmodium falciparum poses a great threat of increased fatalities in cases of cerebral and other forms of severe malaria infections in which parenteral artesunate monotherapy is the current drug of choice. The study aimed to investigate in a mouse model of human cerebral malaria whether a trioxaquine chemically synthesized by covalent linking of a 4,7-dichloroquinoline pharmacophore to artesunate through a recent drug development approach termed 'covalent bitherapy' could improve the curative outcomes in cerebral malaria infections...
July 3, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28669839/optimal-antimalarial-dose-regimens-for-chloroquine-in-pregnancy-based-on-population-pharmacokinetic-modelling
#20
Sam Salman, Francesca Baiwog, Madhu Page-Sharp, Kay Kose, Harin A Karunajeewa, Ivo Mueller, Stephen J Rogerson, Peter M Siba, Kenneth F Ilett, Timothy M E Davis
Despite extensive use and accumulated evidence of safety, there have been few pharmacokinetic studies from which appropriate chloroquine (CQ) dose regimens could be developed specifically for pregnant women. Such optimized CQ-based regimens, used as treatment for acute malaria or as intermittent preventive treatment in pregnancy (IPTp), may have a valuable role if parasite CQ sensitivity returns following reduced drug pressure. In this study, population pharmacokinetic-pharmacodynamic modelling was used to simultaneously analyze plasma concentration-time data for CQ and its active metabolite desethylchloroquine (DCQ) in 44 non-pregnant and 45 pregnant Papua New Guinean women treated with CQ and sulfadoxine-pyrimethamine (SP) or azithromycin (AZI)...
June 29, 2017: International Journal of Antimicrobial Agents
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