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https://www.readbyqxmd.com/read/28212631/anti-malarial-effect-of-novel-chloroquine-derivatives-as-agents-for-the-treatment-of-malaria
#1
Seon-Ju Yeo, Dong-Xu Liu, Hak Sung Kim, Hyun Park
BACKGROUND: The widespread emergence of anti-malarial drug resistance has necessitated the discovery of novel anti-malarial drug candidates. In this study, chloroquine derivatives were evaluated for the improved anti-malarial activity. RESULTS: Novel two derivatives (SKM13 and SKM14) were synthesized based on the chloroquine (CQ) template containing modified side chains such as α,β-unsaturated amides and phenylmethyl group. The selective index indicated that SKM13 was 1...
February 17, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28207974/aamyb1-and-its-orthologue-atmyb61-affect-terpene-metabolism-and-trichome-development-in-artemisia-annua-and-arabidopsis-thaliana
#2
Luis Matías-Hernández, Weimin Jiang, Ke Yang, Kexuan Tang, Peter E Brodelius, Soraya Pelaz
The effective anti-malarial drug artemisinin (AN) isolated from Artemisia annua is relatively expensive due to the low content in the plant as it is only synthesized within the glandular trichomes. Therefore, genetic engineering of A. annua is one of the most promising approaches to improve AN yield. In this work, AaMYB1 transcription factor has been identified and characterized. When AaMYB1 is overexpressed in A. annua, either exclusively in trichomes or in the whole plant, essential AN biosynthetic genes are also overexpressed and consequently AN amount significantly increased...
February 16, 2017: Plant Journal: for Cell and Molecular Biology
https://www.readbyqxmd.com/read/28198460/automated-detection-of-malarial-retinopathy-in-digital-fundus-images-for-improved-diagnosis-in-malawian-children-with-clinically-defined-cerebral-malaria
#3
Vinayak Joshi, Carla Agurto, Simon Barriga, Sheila Nemeth, Peter Soliz, Ian J MacCormick, Susan Lewallen, Terrie E Taylor, Simon P Harding
Cerebral malaria (CM), a complication of malaria infection, is the cause of the majority of malaria-associated deaths in African children. The standard clinical case definition for CM misclassifies ~25% of patients, but when malarial retinopathy (MR) is added to the clinical case definition, the specificity improves from 61% to 95%. Ocular fundoscopy requires expensive equipment and technical expertise not often available in malaria endemic settings, so we developed an automated software system to analyze retinal color images for MR lesions: retinal whitening, vessel discoloration, and white-centered hemorrhages...
February 15, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28196536/community-engagement-and-the-social-context-of-targeted-malaria-treatment-a-qualitative-study-in-kayin-karen-state-myanmar
#4
Kate Sahan, Christopher Pell, Frank Smithuis, Aung Kyaw Phyo, Sai Maung Maung, Chanida Indrasuta, Arjen M Dondorp, Nicholas J White, Nicholas P J Day, Lorenz von Seidlein, Phaik Yeong Cheah
BACKGROUND: The spread of artemisinin-resistance in Plasmodium falciparum is a threat to current global malaria control initiatives. Targeted malaria treatment (TMT), which combines mass anti-malarial administration with conventional malaria prevention and control measures, has been proposed as a strategy to tackle this problem. The effectiveness of TMT depends on high levels of population coverage and is influenced by accompanying community engagement activities and the local social context...
February 14, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28195463/target-elucidation-by-co-crystal-structures-of-nadh-ubiquinone-oxidoreductase-of-plasmodium-falciparum-pfndh2-with-small-molecule-to-eliminate-drug-resistant-malaria
#5
Yiqing Yang, You Yu, Xiaolu Li, Jing Li, Yue Wu, Jie Yu, Jingpeng Ge, Zhenghui Huang, Lubin Jiang, Yu Rao, Maojun Yang
Drug-resistant malarial strains have been continuously emerging recently, which posts a great challenge for the global health. Therefore, new anti-malarial drugs with novel targeting mechanisms are urgently needed for fighting drug-resistant malaria. NADH-ubiquinone oxidoreductase of Plasmodium falciparum (PfNDH2) represents a viable target for anti-malarial drug development. However, the absence of structural information of PfNDH2 limited rational drug design and further development. Herein, we report high resolution crystal structures of the PfNDH2 protein for the first time in Apo-, NADH- and RYL-552 (a new inhibitor)-bound states...
February 14, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28193740/development-of-delayed-hemolytic-anemia-after-treatment-with-oral-artemether-lumefantrine-in-two-patients-with-severe-falciparum-malaria
#6
Yasuhiro Tsuchido, Fukumi Nakamura-Uchiyama, Kasumi Toyoda, Moritoshi Iwagami, Kentaro Tochitani, Koh Shinohara, Naokuni Hishiya, Taku Ogawa, Kenji Uno, Kei Kasahara, Yukiteru Ouji, Shigeyuki Kano, Keiichi Mikasa, Tsunehiro Shimizu, Masahide Yoshikawa, Haruhiko Maruyama
Recently, reports of delayed hemolytic anemia after treatment with artemisinin and its derivatives have emerged. Here we report two cases of delayed hemolytic anemia in a patient with severe falciparum malaria after treatment with oral artemether-lumefantrine (AL). The first patient, a 20-year-old Japanese male student, was diagnosed with falciparum malaria and was administered AL. As having a high parasitemia rate (20.6%) was the only severe malaria criterion met in this case and his general condition was stable, we continued with AL treatment...
February 13, 2017: American Journal of Tropical Medicine and Hygiene
https://www.readbyqxmd.com/read/28192202/ethnomedicinal-uses-of-plants-for-the-treatment-of-malaria-in-soon-valley-khushab-pakistan
#7
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/28189086/pterocarpan-scaffold-a-natural-lead-molecule-with-diverse-pharmacological-properties
#8
REVIEW
Chelliah Selvam, Brian C Jordan, Sandhya Prakash, Daniel Mutisya, Ramasamy Thilagavathi
Phytoalexins are substances produced by plants that act as potent inhibitors of pathogens. Pterocarpans are biologically active isoflavonoids most commonly found in the family Fabaceae that have the ability to act as phytoalexins. It is made up of a tetracyclic ring system possessing benzofuran-benzopyran. A very great number of pterocarpans have been isolated from natural sources and they are proved to have significant biological activities such as anti-microbial, anti-cancerous, anti-inflammatory and anti-malarial activities...
January 17, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28188731/design-in-silico-and-in-vitro-evaluation-of-curcumin-analogues-against-plasmodium-falciparum
#9
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/28185296/a-report-of-cerebral-malaria-treated-with-automated-red-blood-cell-exchange
#10
Waseem Q Anani, Gerald P Smith, Mehraboon Irani, Kathleen E Puca
BACKGROUND: Adjunctive automated whole blood or red blood cell exchange (RBCEx) can rapidly decrease malarial hyperparasitemia. Several case reports and series suggest improvement in clinical symptomatology; however, recent Centers of Disease Control and Prevention (CDC) recommendations concluded that RBCEx has no efficacy as an adjunctive therapy. We present a case of mental status changes secondary to cerebral malaria treated with automated RBCEx resulting in rapid and dramatic neurologic improvement...
February 10, 2017: Transfusion
https://www.readbyqxmd.com/read/28183299/avidity-of-anti-malarial-antibodies-inversely-related-to-transmission-intensity-at-three-sites-in-uganda
#11
Isaac Ssewanyana, Emmanuel Arinaitwe, Joaniter I Nankabirwa, Adoke Yeka, Richard Sullivan, Moses R Kamya, Philip J Rosenthal, Grant Dorsey, Harriet Mayanja-Kizza, Chris Drakeley, Bryan Greenhouse, Kevin K A Tetteh
BACKGROUND: People living in malaria endemic areas acquire protection from severe malaria quickly, but protection from clinical disease and control of parasitaemia is acquired only after many years of repeated infections. Antibodies play a central role in protection from clinical disease; however, protective antibodies are slow to develop. This study sought to investigate the influence of Plasmodium falciparum exposure on the acquisition of high-avidity antibodies to P. falciparum antigens, which may be associated with protection...
February 10, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28183236/antimalarial-antiplasmodial-and-analgesic-activities-of-root-extract-of-alchornea-laxiflora
#12
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/28181499/involvement-of-%C3%AE-defensin-130-defb130-in-the-macrophage-microbicidal-mechanisms-for-killing-plasmodium-falciparum
#13
Mohamad Alaa Terkawi, Ryo Takano, Atsushi Furukawa, Fumi Murakoshi, Kentaro Kato
Understanding the molecular defense mechanism of macrophages and identifying their effector molecules against malarial parasites may provide important clues for the discovery of new therapies. To analyze the immunological responses of malarial parasite-induced macrophages, we used DNA microarray technology to examine the gene profile of differentiated macrophages phagocytizing Plasmodium falciparum-parasitized erythrocytes (iRBC). The transcriptional gene profile of macrophages in response to iRBCs represented 168 down-regulated genes, which were mainly involved in the cellular immune response, and 216 upregulated genes, which were involved in cellular proteolysis, growth, and adhesion...
February 9, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28173853/therapeutic-efficacy-and-effects-of-artemisinin-based-combination-treatments-on-uncomplicated-plasmodium-falciparum%C3%A2-malaria-associated-anaemia-in-nigerian-children-during-seven-years-of-adoption-as-first-line-treatments
#14
Akintunde Sowunmi, Kazeem Akano, Godwin Ntadom, Adejumoke I Ayede, Folasade O Ibironke, Temitope Aderoyeje, Elsie O Adewoye, Bayo Fatunmbi, Stephen Oguche, Henrietta U Okafor, Ismaila Watila, Martin Meremikwu, Philip Agomo, William Ogala, Chimere Agomo, Onikepe A Folarin, Grace O Gbotosho, Christian T Happi
BACKGROUND: Artemisinin-based combination treatments (ACTs) are the first-line treatments of uncomplicated Plasmodium falciparum malaria in many endemic areas but there are few evaluation of their efficacy in anaemic malarious children. METHODS: Therapeutic efficacy of 3-day regimens of artesunate-amodiaquine and artemether-lumefantrine was evaluated in 437 anaemic and 909 non-anaemic malarious children following treatment during a seven-year period (2008-2014)...
February 7, 2017: Infectious Diseases of Poverty
https://www.readbyqxmd.com/read/28166440/malaria-treatment-using-novel-nano-based-drug-delivery-systems
#15
Uday Krishna Baruah, Kuppusamy Gowthamarajan, Ravisankar Vanka, Veera Venkata Satyanarayana Reddy Karri, Kousalya Selvaraj, Gifty M Jojo
We reside in an era of technological innovation and advancement despite which infectious diseases like malaria remain to be one of the greatest threats to the humans. Mortality rate caused by malaria disease is a huge concern in the 21(st) century. Multiple drug resistance and non-specific drug targeting of the most widely used drugs are the main reasons/drawbacks behind the failure in malarial therapy. Dose related toxicity because of high doses is also a major concern. Therefore, to overcome these problems nano based drug delivery systems are being developed to facilitate site specific or target based drug delivery and hence minimising the development of resistance progress and dose dependent toxicity issues...
February 6, 2017: Journal of Drug Targeting
https://www.readbyqxmd.com/read/28163958/a-prospective-comparative-field-study-to-evaluate-the-efficacy-of-a-traditional-plant-based-malaria-prophylaxis
#16
Prakash Bangalore Nagendrappa, Pradeep Annamalai, Muruli Naik, Vinay Mahajan, Ashwini Mathur, Ghosh Susanta, Frederick Gay, Padma Venkatasubramanian
BACKGROUND: An unceasing threat of resistance of malarial parasites to available antimalarial drugs makes the development of new drugs imperative. Natural plant-based products are an alternative source for discovering new antimalarial drugs. AIM: To determine the prophylactic efficacy of a traditionally used plant-based drug on prevention of malaria in endemic villages of Odisha, India. METHODS: A total of 267 healthy human volunteers of both sexes, aged 18-60 years were enrolled in Odisha, India, to receive either minimum 20 doses of aqueous extract of Traditional Plant-based Malaria Prophylactic drug 74, twice a week (experimental group), or no drug (control group) for 14 weeks...
January 2017: Journal of Intercultural Ethnopharmacology
https://www.readbyqxmd.com/read/28153468/anti-malarial-synergy-of-secondary-metabolites-from-morinda-lucida-benth
#17
Bertha Chithambo, Xavier Siwe Noundou, Rui W M Krause
ETHNOPHARMACOLOGICAL RELEVANCE: The roots, stem and leaves of Morinda lucida are used in some African countries as treatment against different types of fevers including yellow fever, malaria, trypanosomiasis and feverish conditions during child birth. AIM OF THE STUDY: To determine the in vitro cell toxicity and anti-malarial activity of the extracts of stem bark of M. lucida and to identify the secondary metabolites in the extract that may be responsible for this activity...
January 30, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28153004/efficacy-of-artemether-lumefantrine-artesunate-amodiaquine-and-dihydroartemisinin-piperaquine-for-treatment-of-uncomplicated-plasmodium-falciparum-malaria-in-angola-2015
#18
Mateusz M Plucinski, Pedro Rafael Dimbu, Aleixo Panzo Macaia, Carolina Miguel Ferreira, Claudete Samutondo, Joltim Quivinja, Marília Afonso, Richard Kiniffo, Eliane Mbounga, Julia S Kelley, Dhruviben S Patel, Yun He, Eldin Talundzic, Denise O Garrett, Eric S Halsey, Venkatachalam Udhayakumar, Pascal Ringwald, Filomeno Fortes
BACKGROUND: Recent anti-malarial resistance monitoring in Angola has shown efficacy of artemether-lumefantrine (AL) in certain sites approaching the key 90% lower limit of efficacy recommended for artemisinin-based combination therapy. In addition, a controversial case of malaria unresponsive to artemisinins was reported in a patient infected in Lunda Sul Province in 2013. METHODS: During January-June 2015, investigators monitored the clinical and parasitological response of children with uncomplicated Plasmodium falciparum infection treated with AL, artesunate-amodiaquine (ASAQ), or dihydroartemisinin-piperaquine (DP)...
February 2, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28152649/anti-inflammatory-anti-cholinergic-and-cytotoxic-effects-of-sida-rhombifolia
#19
Siau Hui Mah, Soek Sin Teh, Gwendoline Cheng Lian Ee
CONTEXT: Sida (Malvaceae) has been used as a traditional remedy for the treatment of diarrhoea, malarial, gastrointestinal dysentery, fevers, asthma and inflammation. OBJECTIVES: This study evaluates the anti-inflammatory, cytotoxic and anti-cholinergic activities of Sida rhombifolia Linn. whole plant for the first time. MATERIALS AND METHODS: S. rhombifolia whole plant was extracted by n-hexane, ethyl acetate and methanol using Soxhlet apparatus...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/28152025/prevalence-of-g6pd-deficiency-in-selected-populations-from-two-previously-high-malaria-endemic-areas-of-sri-lanka
#20
Sharmini Gunawardena, G M G Kapilananda, Dilhani Samarakoon, Sashika Maddevithana, Sulochana Wijesundera, Lallindra V Goonaratne, Nadira D Karunaweera
Glucose-6-Phosphate Dehydrogenase (G6PD) enzyme deficiency is known to offer protection against malaria and an increased selection of mutant genes in malaria endemic regions is expected. However, anti-malarial drugs such as primaquine can cause haemolytic anaemia in persons with G6PD deficiency. We studied the extent of G6PD deficiency in selected persons attending Teaching Hospitals of Anuradhapura and Kurunegala, two previously high malaria endemic districts in Sri Lanka. A total of 2059 filter-paper blood spots collected between November 2013 and June 2014 were analysed for phenotypic G6PD deficiency using the modified WST-8/1-methoxy PMS method...
2017: PloS One
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