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https://www.readbyqxmd.com/read/28441887/chemical-constituents-and-biological-activities-from-branches-of-colubrina-asiatica
#1
Watchara Sangsopha, Kwanjai Kanokmedhakul, Ratsami Lekphrom, Somdej Kanokmedhakul
Sixteen compounds were isolated from a Thai medicinal plant, Colubrina asiatica. The isolated compounds were elucidated on the basis of spectroscopic methods (IR, 1D and 2D NMR) as six triterpene acids (1-6), five steroids (7-11), one benzoic acid derivative (12), two peptides (13 and 14), one sesquiterpenoid (15) and one jujubogenin (16). Compounds 3 and 10 showed antimalarial activity against Plasmodium falciparum. Compound 5 showed antimycobacterial activity. Moreover, compounds 3, 5, 6, 10 and 14 exhibited weak cytotoxicity against cancer cell lines...
April 25, 2017: Natural Product Research
https://www.readbyqxmd.com/read/28440745/primaquine-in-plasma-and-methemoglobinemia-in-patients-with-malaria-due-to-plasmodium-vivax-in-the-brazilian-amazon-basin
#2
José Luiz Vieira, Michelle E S Ferreira, Michelle V D Ferreira, Margarete M Gomes
Primaquine is the only licensed drug available for the elimination of Plasmodium vivax hypnozoites. Methemoglobinemia is currently reported in the course of treatment. There is evidence that metabolites of primaquine formed by the cytochrome pathway are responsible for methemoglobin formation; a genetic polymorphism of cytochrome isoforms; and a potential influence of gender in the activities of these enzymes requiring the establishment of dose × response curves profiles in different population groups. Concentrations of primaquine in plasma and methemoglobin levels were investigated in 54 patients with malaria due to P...
April 3, 2017: American Journal of Tropical Medicine and Hygiene
https://www.readbyqxmd.com/read/28439418/prevention-practices-influencing-frequency-of-occurrence-of-vaso-occlusive-crisis-among-sickle-cell-patients-in-abeokuta-south-local-government-area-of-ogun-state-nigeria
#3
Olorunfemi Emmanuel Amoran, Ahmed Babatunde Jimoh, Omotola Ojo, Temitope Kuponiyi
BACKGROUND: Africa is the most affected continent with 200,000 new born affected by sickle cell anemia annually with of 5% of under five deaths. Nigeria has the largest sickle cell gene pool in the world with about 2% of all babies born to Nigerian parents. This study therefore sets out to assess the prevention practices influencing the frequency of occurrence of vaso-occlusive crisis among patients in Ogun State. METHODS: This study is a descriptive cross-sectional study conducted in Abeokuta South Local Government Area Ogun State...
2017: BMC Hematology
https://www.readbyqxmd.com/read/28435533/discovery-of-antimalarial-azetidine-2-carbonitriles-that-inhibit-p-falciparum-dihydroorotate-dehydrogenase
#4
Micah Maetani, Nobutaka Kato, Valquiria A P Jabor, Felipe A Calil, Maria Cristina Nonato, Christina A Scherer, Stuart L Schreiber
Dihydroorotate dehydrogenase (DHODH) is an enzyme necessary for pyrimidine biosynthesis in protozoan parasites of the genus Plasmodium, the causative agents of malaria. We recently reported the identification of novel compounds derived from diversity-oriented synthesis with activity in multiple stages of the malaria parasite life cycle. Here, we report the optimization of a potent series of antimalarial inhibitors consisting of azetidine-2-carbonitriles, which we had previously shown to target P. falciparum DHODH in a biochemical assay...
April 13, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28433067/chloroquine-and-hydroxychloroquine-inhibit-bladder-cancer-cell-growth-by-targeting-basal-autophagy-and-enhancing-apoptosis
#5
Yi-Chia Lin, Ji-Fan Lin, Sheng-I Wen, Shan-Che Yang, Te-Fu Tsai, Hung-En Chen, Kuang-Yu Chou, Thomas I-Sheng Hwang
Chloroquine (CQ) and hydroxychloroquine (HCQ), two antimalarial drugs, are suggested to have potential anticancer properties. in the present study, we investigated the effects of CQ and HCQ on cell growth of bladder cancer with emphasis on autophagy inhibition and apoptosis induction in vitro. The results showed that CQ and HCQ inhibited the proliferation of multiple human bladder cell lines (including RT4, 5637, and T24) in a time- and dose-dependent fashion, especially in advanced bladder cancer cell lines (5637 and T24) compared to immortalized uroepithelial cells (SV-Huc-1) or other reference cancer cell lines (PC3 and MCF-7)...
May 2017: Kaohsiung Journal of Medical Sciences
https://www.readbyqxmd.com/read/28411684/in-vivo-antimalarial-activity-of-synthetic-hepcidin-against-plasmodium-berghei-in-mice
#6
Ya-Qun Fang, Chuan-Bin Shen, Ning Luan, Hui-Min Yao, Chen-Bo Long, Ren Lai, Xiu-Wen Yan
The present study was designed to investigate the antimalarial activity of synthetic hepcidin and its effect on cytokine secretion in mice infected with Plasmodium berghei. The mice were infected with P. berghei intravenously and treated with hepcidin according to 4-day suppression test and Rane's test. The serum levels of interleukins (IL-1β, IL-2, IL-6, IL-10, IL-12p70, and IL-17A), tumor necrosis factor-α (TNF-α), and interferon-γ (IFN-γ) in the experimental mice were determined using a cytometric bead array (CBA) kit...
March 2017: Chinese Journal of Natural Medicines
https://www.readbyqxmd.com/read/28402391/the-relative-effects-of-artemether-lumefantrine-and-non-artemisinin-antimalarials-on-gametocyte-carriage-and-transmission-of-plasmodium-falciparum-a-systematic-review-and-meta-analysis
#7
Matthew M Ippolito, Julia Johnson, Christopher Mullin, Christopher Mallow, Nadia Morgan, Erika Wallender, Tianjing Li, Philip J Rosenthal
Background.: Artemisinin-based combination therapies (ACTs) have been widely adopted as first-line agents to treat uncomplicated falciparum malaria due to their activity against multidrug resistant parasites. ACTs may also disrupt transmission through a direct antigametocyte effect, but the extent of this effect is uncertain. We assessed the evidence for and estimated the effects of the most widely deployed ACT, artemether-lumefantrine (AL), relative to non-ACTs on gametocyte clearance and transmission interruption...
April 11, 2017: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
https://www.readbyqxmd.com/read/28394230/advanced-mri-techniques-biomarkers-in-neuropsychiatric-lupus
#8
N Sarbu, P Toledano, A Calvo, E Roura, M I Sarbu, G Espinosa, X Lladó, R Cervera, N Bargalló
Objectives The objective of this study was to determine whether advanced MRI could provide biomarkers for diagnosis and prognosis in neuropsychiatric systemic lupus erythematosus (NPSLE). Methods Our prospective study included 28 systemic lupus erythematosus (SLE) patients with primary central NPSLE, 22 patients without NPSLE and 20 healthy controls. We used visual scales to evaluate atrophy and white matter hyperintensities, voxel-based morphometry and Freesurfer to measure brain volume, plus diffusion-tensor imaging (DTI) to assess white matter (WM) and gray matter (GM) damage...
April 2017: Lupus
https://www.readbyqxmd.com/read/28389278/prenylated-flavonoids-from-the-stems-and-roots-of-tripterygium-wilfordii
#9
Yang Chen, Jianping Zhao, Yixing Qiu, Hanwen Yuan, Shabana I Khan, Nusrat Hussain, M Iqbal Choudhary, Feng Zeng, De-An Guo, Ikhlas A Khan, Wei Wang
Phytochemical investigation on the stems and roots of Tripterygium wilfordii led to the isolation and characterization of three new prenylated flavanones, tripteryols A-C (1-3), along with (±)-5,4'-dihydroxy-2'-methoxy-6',6″-dimethypyraro-(2″,3″:7,8)-6-methyflavanone (4), and ((2S)-5,7,4'-trihydroxy-2'-methoxy-8,5'-di(3-methyl-2-butenyl)-6-methylflavanone (5). Structures of the compounds 1-5 were elucidated using spectroscopic techniques, such as UV, IR, NMR (1D and 2D), and HRESI-MS. Tripteryols B (2) was found active in the antimicrobial assay against Cryptococcus neoformans, Pseudomonas aeruginosa, vancomycin-resistant Enterococcus faecalis (VRE) and methicillin-resistant Staphylococcus aureus (MRSA) with IC50 values in the range of 2...
April 5, 2017: Fitoterapia
https://www.readbyqxmd.com/read/28384525/terphenyl-derivatives-and-drimane-phathalide-isoindolinones-from-hypoxylon-fendleri-bcc32408
#10
Chakapong Intaraudom, Nantiya Bunbamrung, Aibrohim Dramae, Nattawut Boonyuen, Palangpon Kongsaeree, Kitlada Srichomthong, Sumalee Supothina, Pattama Pittayakhajonwut
The genus Hypoxylon, a member of the family Xylariaceae, has been known to produce significant secondary metabolites in terms of chemical diversity. Moreover, the compounds isolated can also be used as chemotaxonomic characters for differentiation among the two sections, which are sect. Annulata and sect. Hypoxylon. In our continuing chemical screening programme for novel compounds, the crude extracts of H. fendleri BCC32408 gave significant chemical profiles in HPLC analyses. Thus, the chemical investigation of these crude extracts was then carried out...
April 3, 2017: Phytochemistry
https://www.readbyqxmd.com/read/28383076/the-interaction-of-heme-with-plakortin-and-a-synthetic-endoperoxide-analogue-new-insights-into-the-heme-activated-antimalarial-mechanism
#11
Marco Persico, Roberto Fattorusso, Orazio Taglialatela-Scafati, Giuseppina Chianese, Ivan de Paola, Laura Zaccaro, Francesca Rondinelli, Marco Lombardo, Arianna Quintavalla, Claudio Trombini, Ernesto Fattorusso, Caterina Fattorusso, Biancamaria Farina
In the present work we performed a combined experimental and computational study on the interaction of the natural antimalarial endoperoxide plakortin and its synthetic analogue 4a with heme. Obtained results indicate that the studied compounds produce reactive carbon radical species after being reductively activated by heme. In particular, similarly to artemisinin, the formation of radicals prone to inter-molecular reactions should represent the key event responsible for Plasmodium death. To our knowledge this is the first experimental investigation on the reductive activation of simple antimalarial endoperoxides (1,2-dioxanes) by heme and results were compared to the ones previously obtained from the reaction with FeCl2...
April 6, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28382183/synthesis-of-1-indanones-with-a-broad-range-of-biological-activity
#12
REVIEW
Marika Turek, Dorota Szczęsna, Marek Koprowski, Piotr Bałczewski
This comprehensive review describes methods for the preparation of 1-indanones published in original and patent literature from 1926 to 2017. More than 100 synthetic methods utilizing carboxylic acids, esters, diesters, acid chlorides, ketones, alkynes, alcohols etc. as starting materials, have been performed. This review also covers the most important studies on the biological activity of 1-indanones and their derivatives which are potent antiviral, anti-inflammatory, analgesic, antimalarial, antibacterial and anticancer compounds...
2017: Beilstein Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28377317/dehydroascorbate-derivatized-chitosan-particles-for-targeting-antimalarial-agents-to-infected-erythrocytes
#13
Hasham Shafi, D V Siva Reddy, Tabassum Khan, Rajeev Ranjan, Ashish Srivastava, Suniti Vaishya, Tanuj Sharma, Mohammad Imran Siddiqui, Saman Habib, Amit Misra
The mammalian glucose transporter GLUT-1 and Plasmodium falciparum hexose transporter PfHT1 are overexpressed on human RBC infected with the parasite (iRBC), presumably for enhanced glucose uptake. Dehydroascorbic acid (DHA) competes out glucose in GLUT-1 binding. We prepared particles containing chloroquine phosphate using novel derivatives of chitosan (CSN). CSN was either pre-derivatized with DHA (PRE) or particles made of CSN were derivatized by surface-grafting DHA (POST). The optimized formulations were analyzed for size (170-200nm) drug content (about 40%) entrapment efficiency (50-57%), in vitro drug release (80% in 72h, Higuchi's model), hemolysis on exposure to whole blood or RBC at 5% hematocrit, cytotoxicity towards cultured HEK 293T (kidney) and HepG2 (hepatic) cells, targeting iRBC and in vitro efficacy against P...
April 2, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28374446/superbanone-a-new-2-aryl-3-benzofuranone-and-other-bioactive-constituents-from-the-tube-roots-of-butea-superba
#14
Jutatip Boonsombat, Vilailak Prachyawarakorn, Acharavadee Pansanit, Chulabhorn Mahidol, Somsak Ruchirawat, Sanit Thongnest
Phytochemical investigation from the tube roots of Butea superba, led to the isolation and identification of a new 2-aryl-3-benzofuranone named superbanone (1), one benzoin, 2-hydroxyl-1-(2-hydroxy-4-methoxyphenyl)-2-(4-methoxy-phenyl)ethanone (2), eight pterocarpans (3-10), and eleven isoflavonoids (11-21). Compound 2 was identified for the first time as a natural product. The structure of the isolated compounds was elucidated using spectroscopic methods, mainly 1D and 2D NMR. The isolated compounds and their derivatives were evaluated for α-glucosidase inhibitory and antimalarial activities...
April 4, 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/28374255/qsar-modeling-and-chemical-space-analysis-of-antimalarial-compounds
#15
Pavel Sidorov, Birgit Viira, Elisabeth Davioud-Charvet, Uko Maran, Gilles Marcou, Dragos Horvath, Alexandre Varnek
Generative topographic mapping (GTM) has been used to visualize and analyze the chemical space of antimalarial compounds as well as to build predictive models linking structure of molecules with their antimalarial activity. For this, a database, including ~3000 molecules tested in one or several of 17 anti-Plasmodium activity assessment protocols, has been compiled by assembling experimental data from in-house and ChEMBL databases. GTM classification models built on subsets corresponding to individual bioassays perform similarly to the earlier reported SVM models...
April 3, 2017: Journal of Computer-aided Molecular Design
https://www.readbyqxmd.com/read/28373031/isolation-and-quantification-of-antimalarial-n-alkylamides-from-flower-head-derived-in%C3%A2-vitro-callus-cultures-of-spilanthes-paniculata
#16
Radhika Rajendran, Balaji Sitthu Narashimman, Vishal Trivedi, Rakhi Chaturvedi
This is the pioneer work reporting on simple procedure for synchronized determination and quantification of two biologically active N-alkylamides, (2E,6Z,8E)-N-isobutyl-2,6,8-decatrienamide (spilanthol) and (2E,4Z)-N-isobutyl-2,4-undecadiene-8,10-diynamide (UDA), using in vitro callus cultures from flower-heads of Spilanthes paniculata. The extracts were purified using preparative thin layer chromatography (TLC) and finest separation of compounds was optimized using high performance liquid chromatography (HPLC)...
March 31, 2017: Journal of Bioscience and Bioengineering
https://www.readbyqxmd.com/read/28371168/ama1-and-maebl-are-important-for-plasmodium-falciparum-sporozoite-infection-of-the-liver
#17
Annie S P Yang, Sash Lopaticki, Matthew T O'Neill, Sara M Erickson, Donna N Douglas, Norman M Kneteman, Justin A Boddey
The malaria sporozoite injected by a mosquito migrates to the liver by traversing host cells. The sporozoite also traverses hepatocytes before invading a terminal hepatocyte and developing into exoerythrocytic forms. Hepatocyte infection is critical for parasite development into merozoites that infect erythrocytes, and the sporozoite is thus an important target for antimalarial intervention. Here, we investigated two abundant sporozoite proteins of the most virulent malaria parasite Plasmodium falciparum and show that they play important roles during cell traversal and invasion of human hepatocytes...
March 31, 2017: Cellular Microbiology
https://www.readbyqxmd.com/read/28368118/unguiculin-a-and-ptilomycalins-e-h-antimalarial-guanidine-alkaloids-from-the-marine-sponge-monanchora-unguiculata
#18
Pierre-Eric Campos, Jean-Luc Wolfender, Emerson F Queiroz, Laurence Marcourt, Ali Al-Mourabit, Michel Frederich, Annélise Bordignon, Nicole De Voogd, Bertrand Illien, Anne Gauvin-Bialecki
Chemical study of the CH2Cl2-MeOH (1:1) extract from the sponge Monanchora unguiculata collected in Madagascar highlighted five new compounds, one acyclic guanidine alkaloid, unguiculin A (1) and four pentacyclic alkaloids, ptilomycalins E-H (2-5), along with four known compounds: crambescidin 800 (6) and crambescidin 359 (7), crambescidic acid (8), and fromiamycalin (9). Their structures were elucidated by 1D and 2D NMR spectra and HRESIMS data. All compounds were evaluated for their cytotoxicity against KB cells and their antiplasmodial activity...
April 3, 2017: Journal of Natural Products
https://www.readbyqxmd.com/read/28363637/dsm265-for-plasmodium-falciparum-chemoprophylaxis-a-randomised-double-blinded-phase-1-trial-with-controlled-human-malaria-infection
#19
Mihály Sulyok, Thomas Rückle, Alexandra Roth, Raymund E Mürbeth, Stephan Chalon, Nicola Kerr, Sonia Schnieper Samec, Nathalie Gobeau, Carlos Lamsfus Calle, Javier Ibáñez, Zita Sulyok, Jana Held, Tamirat Gebru, Patricia Granados, Sina Brückner, Christian Nguetse, Juliana Mengue, Albert Lalremruata, Kim Lee Sim, Stephen L Hoffman, Jörg J Möhrle, Peter G Kremsner, Benjamin Mordmüller
BACKGROUND: A drug for causal (ie, pre-erythrocytic) prophylaxis of Plasmodium falciparum malaria with prolonged activity would substantially advance malaria control. DSM265 is an experimental antimalarial that selectively inhibits the parasite dihydroorotate dehydrogenase. DSM265 shows in vitro activity against liver and blood stages of P falciparum. We assessed the prophylactic activity of DSM265 against controlled human malaria infection (CHMI). METHODS: At the Institute of Tropical Medicine, Eberhard Karls University (Tübingen, Germany), healthy, malaria-naive adults were allocated to receive 400 mg DSM265 or placebo either 1 day (cohort 1A) or 7 days (cohort 2) before CHMI by direct venous inoculation (DVI) of 3200 aseptic, purified, cryopreserved P falciparum sporozoites (PfSPZ Challenge; Sanaria Inc, Rockville, MD, USA)...
March 28, 2017: Lancet Infectious Diseases
https://www.readbyqxmd.com/read/28363636/safety-tolerability-pharmacokinetics-and-activity-of-the-novel-long-acting-antimalarial-dsm265-a-two-part-first-in-human-phase-1a-1b-randomised-study
#20
James S McCarthy, Julie Lotharius, Thomas Rückle, Stephan Chalon, Margaret A Phillips, Suzanne Elliott, Silvana Sekuloski, Paul Griffin, Caroline L Ng, David A Fidock, Louise Marquart, Noelle S Williams, Nathalie Gobeau, Lidiya Bebrevska, Maria Rosario, Kennan Marsh, Jörg J Möhrle
BACKGROUND: DSM265 is a novel antimalarial that inhibits plasmodial dihydroorotate dehydrogenase, an enzyme essential for pyrimidine biosynthesis. We investigated the safety, tolerability, and pharmacokinetics of DSM265, and tested its antimalarial activity. METHODS: Healthy participants aged 18-55 years were enrolled in a two-part study: part 1, a single ascending dose (25-1200 mg), double-blind, randomised, placebo-controlled study, and part 2, an open-label, randomised, active-comparator controlled study, in which participants were inoculated with Plasmodium falciparum induced blood-stage malaria (IBSM) and treated with DSM265 (150 mg) or mefloquine (10 mg/kg)...
March 28, 2017: Lancet Infectious Diseases
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