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https://www.readbyqxmd.com/read/28195463/target-elucidation-by-cocrystal-structures-of-nadh-ubiquinone-oxidoreductase-of-plasmodium-falciparum-pfndh2-with-small-molecule-to-eliminate-drug-resistant-malaria
#1
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 antimalarial 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 antimalarial drug development. However, the absence of structural information on 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 22, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28188731/design-in-silico-and-in%C3%A2-vitro-evaluation-of-curcumin-analogues-against-plasmodium-falciparum
#2
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/28183299/avidity-of-anti-malarial-antibodies-inversely-related-to-transmission-intensity-at-three-sites-in-uganda
#3
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/28152649/anti-inflammatory-anti-cholinergic-and-cytotoxic-effects-of-sida-rhombifolia
#4
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/28146103/role-of-quinone-reductase-2-in-the-antimalarial-properties-of-indolone-type-derivatives
#5
Laure-Estelle Cassagnes, Nambinina Rakotoarivelo, Serena Sirigu, Pierre Pério, Ennaji Najahi, Léonard M G Chavas, Andrew Thompson, Régis Gayon, Gilles Ferry, Jean A Boutin, Alexis Valentin, Karine Reybier, Françoise Nepveu
Indolone-N-oxides have antiplasmodial properties against Plasmodium falciparum at the erythrocytic stage, with IC50 values in the nanomolar range. The mechanism of action of indolone derivatives involves the production of free radicals, which follows their bioreduction by an unknown mechanism. In this study, we hypothesized that human quinone reductase 2 (hQR2), known to act as a flavin redox switch upon binding to the broadly used antimalarial chloroquine, could be involved in the activity of the redox-active indolone derivatives...
January 30, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28076793/chloroquine-inducible-par-4-secretion-is-essential-for-tumor-cell-apoptosis-and-inhibition-of-metastasis
#6
Ravshan Burikhanov, Nikhil Hebbar, Sunil K Noothi, Nidhi Shukla, James Sledziona, Nathália Araujo, Meghana Kudrimoti, Qing Jun Wang, David S Watt, Danny R Welch, Jodi Maranchie, Akihiro Harada, Vivek M Rangnekar
The induction of tumor suppressor proteins capable of cancer cell apoptosis represents an attractive option for the re-purposing of existing drugs. We report that the anti-malarial drug, chloroquine (CQ), is a robust inducer of Par-4 secretion from normal cells in mice and cancer patients in a clinical trial. CQ-inducible Par-4 secretion triggers paracrine apoptosis of cancer cells and also inhibits metastatic tumor growth. CQ induces Par-4 secretion via the classical secretory pathway that requires the activation of p53...
January 10, 2017: Cell Reports
https://www.readbyqxmd.com/read/28036313/pretreatment-elevated-erythrocyte-sedimentation-rate-and-c-reactive-protein-as-a-predictor-of-malarial-complications
#7
Sachin Vemula, Vidyalakshmi Katara, Unnikrishnan Bhaskaran, Sushma Adappa, Mahabala Chakrapani
INTRODUCTION: Complications of malaria can develop suddenly and unexpectedly. Although various parameters have been associated with severity of malaria, they have not been studied as predictors of these events. Many of the malarial complications are inflammatory in nature, and C-reactive protein (CRP) and elevated erythrocyte sedimentation rate (ESR) could be early markers of these complications and might precede and predict the development of complications. METHODOLOGY: A total of 122 inpatients with uncomplicated newly diagnosed malaria were studied...
December 30, 2016: Journal of Infection in Developing Countries
https://www.readbyqxmd.com/read/28031457/force-spectroscopy-of-the-plasmodium-falciparum-vaccine-candidate-circumsporozoite-protein-suggests-a-mechanically-pliable-repeat-region
#8
Aditya Prasad Patra, Shobhona Sharma, Sri Rama Koti Ainavarapu
The most effective vaccine candidate of malaria is based on the Plasmodium falciparum circumsporozoite protein (CSP), a major surface protein implicated in the structural strength, motility, and immune evasion properties of the infective sporozoites. It is suspected that reversible conformational changes of CSP are required for infection of the mammalian host, but the detailed structure and dynamic properties of CSP remain incompletely understood, limiting our understanding of its function in the infection...
February 10, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28012440/nrf2-inhibition-reverses-the-resistance-of-cisplatin-resistant-head-and-neck-cancer-cells-to-artesunate-induced-ferroptosis
#9
Jong-Lyel Roh, Eun Hye Kim, Hyejin Jang, Daiha Shin
: Artesunate, an anti-malarial drug, has been repurposed as an anticancer drug due to its induction of cell death via reactive oxygen species (ROS) production. However, the molecular mechanisms regulating cancer cell death and the resistance of cells to artesunate remain unclear. We investigated the molecular mechanisms behind the antitumor effects of artesunate and an approach to overcome artesunate resistance in head and neck cancer (HNC). The effects of artesunate and trigonelline were tested in different HNC cell lines, including three cisplatin-resistant HNC cell lines...
December 18, 2016: Redox Biology
https://www.readbyqxmd.com/read/28000518/artemisinin-inhibits-inflammatory-response-via-regulating-nf-%C3%AE%C2%BAb-and-mapk-signaling-pathways
#10
Ke Si Wang, Junbo Li, Zhe Wang, Chunliu Mi, Juan Ma, Lian Xun Piao, Guang Hua Xu, Xuezheng Li, Xuejun Jin
Artemisinin, isolated from the Chinese plant Artemisia annua, has been used for many years to treat different forms of malarial parasites. In this study, we explored the anti-inflammatory activity of artemisinin and the underlying mechanism of this action. We demonstrated that the anti-inflammatory effects of artemisinin in TPA-induced skin inflammation in mice. Then the artemisinin significantly inhibited the expression of NF-κB reporter gene induced by TNF-α in a dose-dependent manner. Artemisinin also inhibited TNF-α induced phosphorylation and degradation of IκBα, p65 nuclear translocation...
December 21, 2016: Immunopharmacology and Immunotoxicology
https://www.readbyqxmd.com/read/27941926/dihydroartemisinin-inhibits-catabolism-in-rat-chondrocytes-by-activating-autophagy-via-inhibition-of-the-nf-%C3%AE%C2%BAb-pathway
#11
Li-Bo Jiang, De-Hua Meng, Soo-Min Lee, Shu-Hao Liu, Qin-Tong Xu, Yang Wang, Jian Zhang
Osteoarthritis is a disease with inflammatory and catabolic imbalance in cartilage. Dihydroartemisinin (DHA), a natural and safe anti-malarial agent, has been reported to inhibit inflammation, but its effects on chondrocytes have yet to be elucidated. We investigated the effects of DHA on catabolism in chondrocytes. Viability of SD rats chondrocytes was analyzed. Autophagy levels were determined via expression of autophagic markers LC3 and ATG5, GFP-LC3 analysis, acridine orange staining, and electron microscopy...
December 12, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27936446/design-synthesis-and-evaluation-of-4-aminoquinoline-purine-hybrids-as-potential-antiplasmodial-agents
#12
P Linga Reddy, Shabana I Khan, Prija Ponnan, Mohit Tripathi, Diwan S Rawat
A novel series of 4-aminoquinoline-purine hybrids were synthesized and assessed for their antiplasmodial activity against CQ-sensitive and CQ-resistant strains of P. falciparum. It was envisaged that linking of the 4-aminoquinoline pharmacophore (targeting heme-detoxification pathway of malarial parasite) with the purine functionality (targeting plasmodial HG(X)PRT enzyme) will produce a hybrid antiplasmodial agent with increased potency. The synthesized hybrids displayed good antiplasmodial activities against both the sensitive and resistant strains of P...
January 27, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27923179/structural-dynamics-of-casein-kinase-i-cki-from-malarial-parasite-plasmodium-falciparum-isolate-3d7-insights-from-theoretical-modelling-and-molecular-simulations
#13
Budheswar Dehury, Santosh Kumar Behera, Namita Mahapatra
The protein kinases (PKs), belonging to serine/threonine kinase (STKs), are important drug targets for a wide spectrum of diseases in human. Among protein kinases, the Casein Kinases (CKs) are vastly expanded in various organisms, where, the malarial parasite Plasmodium falciparum possesses a single member i.e., PfCKI, which can phosphorylate various proteins in parasite extracts in vitro condition. But, the structure-function relationship of PfCKI and dynamics of ATP binding is yet to be understood. Henceforth, an attempt was made to study the dynamics, stability, and ATP binding mechanisms of PfCKI through computational modelling, docking, molecular dynamics (MD) simulations, and MM/PBSA binding free energy estimation...
January 2017: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/27912758/emerging-polymorphisms-in-falciparum-kelch-13-gene-in-northeastern-region-of-india
#14
Neelima Mishra, Ram Suresh Bharti, Prashant Mallick, Om Prakash Singh, Bina Srivastava, Roma Rana, Sobhan Phookan, Hardev Prasad Gupta, Pascal Ringwald, Neena Valecha
BACKGROUND: Recent reports of emergence and spread of artemisinin resistance in the Southeast Asia region, including Myanmar, pose a greater threat to malaria control and elimination in India. Whole genome sequencing studies have associated mutations in the K13 propeller gene (k13), PF3D7_1343700 with artemisinin resistance both in vitro and in vivo. The aim of the present study was to find the k13 gene polymorphisms in Plasmodium falciparum parasites from the three sites in the Northeast region of India, bordering Bangladesh and Myanmar...
December 3, 2016: Malaria Journal
https://www.readbyqxmd.com/read/27903279/in-vitro-and-in-vivo-anti-malarial-activity-of-novel-harmine-analog-heat-shock-protein-90-inhibitors-a-possible-partner-for-artemisinin
#15
Abebe Genetu Bayih, Asongna Folefoc, Abu Naser Mohon, Scott Eagon, Marc Anderson, Dylan R Pillai
BACKGROUND: The emergence of artemisinin-resistant Plasmodium falciparum strains poses a serious challenge to the control of malaria. This necessitates the development of new anti-malarial drugs. Previous studies have shown that the natural beta-carboline alkaloid harmine is a promising anti-malarial agent targeting the P. falciparum heat-shock protein 90 (PfHsp90). The aim of this study was to test the anti-malarial activity of harmine analogues. METHODS: Forty-two harmine analogues were synthesized and the binding of these analogues to P...
December 1, 2016: Malaria Journal
https://www.readbyqxmd.com/read/27873143/regulation-of-rac1-gtpase-activity-by-quinine-through-g-protein-and-bitter-taste-receptor-t2r4
#16
Crystal Sidhu, Appalaraju Jaggupilli, Prashen Chelikani, Rajinder P Bhullar
Rac1 belongs to the Rho family of small GTPases and regulates actin cytoskeleton reorganization. T2R4 is a bitter taste receptor belonging to the G protein-coupled receptor family of proteins. In addition to mediating bitter taste perception from the tongue, T2R4s are found in extra-oral tissues, e.g., nasal epithelium, airways, brain, testis suggesting a much broader physiological function for these receptors. Anti-malarial drug and a bitter tasting compound, quinine, is a known agonist for T2R4, whereas BCML (Nα,Nα-Bis(carboxymethyl)-L-lysine) acts as an inverse agonist...
February 2017: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/27814577/identification-of-natural-peptides-as-a-new-class-of-antimalarial-drugs-by-in-silico-approaches
#17
Ramar Perumal Samy, Sok Lin Foo, Octavio L Franco, Bradley G Stiles, Alan P Kumar, Gautam Sethi, Lina Hk Lim
Malaria is one of the most widespread and serious parasitic diseases worldwide. Currently available antimalarial drugs have side effects, and many strains of Plasmodia have developed resistance to such drugs. The present review examines the use of annexins and of natural peptides from snake venom as a new class of anti-malarial agents, with the key property of reducing inflammation. Severe cases of malaria manifest elevated serum levels of liver enzymes, inflammation, fibrin deposition, apoptosis, and reduction in peripheral CD8(+) T cells...
January 1, 2017: Frontiers in Bioscience (Scholar Edition)
https://www.readbyqxmd.com/read/27806730/comparative-physiological-plasticity-to-desiccation-in-distinct-populations-of-the-malarial-mosquito-anopheles-coluzzii
#18
K Hidalgo, D Siaussat, V Braman, K R Dabiré, F Simard, K Mouline, D Renault
BACKGROUND: In West Africa, populations of the malaria vector mosquito, Anopheles coluzzii, are seasonally exposed to strong desiccating conditions during the dry season. Their dynamics strictly follows the pace of the availability of suitable larval development sites (water collections). Accordingly, mosquitoes can reproduce all year long where permanent breeding is possible, or stop reproduction and virtually disappear at the onset of the dry season when surface water dries up, like observed in temporary habitats of dry savannah areas...
November 2, 2016: Parasites & Vectors
https://www.readbyqxmd.com/read/27806725/the-effect-of-malaria-and-anti-malarial-drugs-on-skeletal-and-cardiac-muscles
#19
REVIEW
Mauro Toledo Marrelli, Marco Brotto
Malaria remains one of the most important infectious diseases in the world, being a significant public health problem associated with poverty and it is one of the main obstacles to the economy of an endemic country. Among the several complications, the effects of malaria seem to target the skeletal muscle system, leading to symptoms, such as muscle aches, muscle contractures, muscle fatigue, muscle pain, and muscle weakness. Malaria cause also parasitic coronary artery occlusion. This article reviews the current knowledge regarding the effect of malaria disease and the anti-malarial drugs on skeletal and cardiac muscles...
November 2, 2016: Malaria Journal
https://www.readbyqxmd.com/read/27799332/ph-alkalinization-by-chloroquine-suppresses-pathogenic-burkholderia-type-6-secretion-system-1-and-multinucleated-giant-cells
#20
Jennifer Chua, Jeffrey L Senft, Stephen J Lockett, Paul J Brett, Mary N Burtnick, David DeShazer, Arthur M Friedlander
Burkholderia mallei and B. pseudomallei cause glanders and melioidosis, respectively, in humans and animals. A hallmark of pathogenesis is the formation of granulomas containing multinucleated giant cells (MNGCs) and cell death. These processes depend on type 6 secretion system 1 (T6SS-1), which is required for virulence in animals. We examined the cell biology of MNGC formation and cell death. We found that chloroquine diphosphate (CLQ), an antimalarial drug, inhibits Burkholderia growth, phagosomal escape, and subsequent MNGC formation...
January 2017: Infection and Immunity
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