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antimalarial

NOT Open Access | Multiple-targets Directed Screening of Flavonoid Compounds from Citrus Species to find out Antimalarial Lead with Predicted Mode of Action: An In Silico and Whole Cell-based In vitro Approach

January 15, 2020 - 08:03 -- NOT Open Access
Author(s): 
Gogoi N, Chetia D, Gogoi B, Das A
Reference: 
Current Computer-Aided Drug Design, 2019 Dec 25

In this study, 44 flavonoids found mainly in the fruit juice of Citrus species having traditional use in malaria-associated fever were selected for in silico multiple-target directed screening against three vital targets of the parasite namely dihydrooroate dehydrogenase (PfDHODH), dihydrofolate reductase thymidine synthase (PfDHFR-TS) and plasma membrane P-type cation translocating ATPase (PfATP4) to find out new lead molecule(s).

Evaluation of Antimalarial Activity of Hydromethanolic Crude Extract and Solvent Fractions of the Leaves of Nuxia congesta R. Br. Ex Fresen (Buddlejaceae) in Plasmodium berghei Infected Mice

January 14, 2020 - 12:17 -- Open Access
Author(s): 
Fenta M, Kahaliw W
Reference: 
Journal of Experimental Pharmacology, 16 December 2019 Volume: 11 Pages 121—134

In Ethiopia, malaria control has been complicated due to resistance of the parasite and its vectors to the current drugs. Therefore, new drugs are required to avert the problem posed by drug-resistant Plasmodium strains. There is need to investigate alternative sources of antimalarial agents and plants are potential source of antimalarial drugs. This study aimed to investigate the antimalarial activity of the leaves of N. congesta crude extract (hydromethanolic extract) and solvent fractions (n-hexane, chloroform, and aqueous fractions of crude extract) traditionally used to treat malaria in many parts of Ethiopia.

NOT Open Access | Current progress in antimalarial pharmacotherapy and multi-target drug discovery

January 14, 2020 - 12:04 -- NOT Open Access
Author(s): 
Tibon NS, Ng CH, Cheong SL
Reference: 
European Journal of Medicinal Chemistry, Volume 188, 15 February 2020, 111983

Discovery and development of antimalarial drugs have long been dominated by single-target therapy. Continuous effort has been made to explore and identify different targets in malaria parasite crucial for the malaria treatment. The single-target drug therapy was initially successful, but it was later supplanted by combination therapy with multiple drugs to overcome drug resistance.

NOT Open Access | In Vivo Efficacy and Pharmacokinetics of the 2-Aminomethylphenol Antimalarial, JPC-3210, in the Aotus Monkey-Human Malaria Model

December 23, 2019 - 15:10 -- NOT Open Access
Author(s): 
McCallum F, Birrell GW, Chavchich M, Harris I, Obaldia N 3rd, Van Breda K, Heffernan GD, Jacobus DP, Shanks D, Edstein MD
Reference: 
Antimicrob Agents Chemother. 2019 Dec 16. pii: AAC.01538-19

Nonimmune Aotus monkeys infected with Plasmodium falciparum and Plasmodium vivax were cured of their infections when treated with a single oral dose of 5 mg/kg and 10 mg/kg of the 2-aminomethylphenol, JPC-3210, respectively.

Coupling the Antimalarial Cell Penetrating Peptide TP10 to Classical Antimalarial Drugs Primaquine and Chloroquine Produces Strongly Hemolytic Conjugates

December 23, 2019 - 14:59 -- Open Access
Author(s): 
Aguiar L, Biosca A, Lantero E, Gut J, Vale N, Rosenthal PJ, Nogueira F, Andreu D, Fernàndez-Busquets X, Gomes P
Reference: 
Molecules 2019, 24(24), 4559

Recently, we disclosed primaquine cell penetrating peptide conjugates that were more potent than parent primaquine against liver stage Plasmodium parasites and non-toxic to hepatocytes. The same strategy was now applied to the blood-stage antimalarial chloroquine, using a wide set of peptides, including TP10, a cell penetrating peptide with intrinsic antiplasmodial activity. Chloroquine-TP10 conjugates displaying higher antiplasmodial activity than the parent TP10 peptide were identified, at the cost of an increased hemolytic activity, which was further confirmed for their primaquine analogues.

Not Open Access | Asymptomatic malaria in the clinical and public health context

December 2, 2019 - 17:45 -- NOT Open Access
Author(s): 
Cheaveau J, Mogollon DC, Mohon MAN, Golassa L, Yewhalaw D, Pillai DR
Reference: 
Expert Rev Anti Infect Ther. 2019 Nov 21:1-14.

Historically, the global community has focused on the control of symptomatic malaria. However, interest in asymptomatic malaria has been growing, particularly in the context of malaria elimination.

Decreased K13 Abundance Reduces Hemoglobin Catabolism and Proteotoxic Stress, Underpinning Artemisinin Resistance

December 2, 2019 - 14:43 -- Open Access
Author(s): 
Yang T, Yeoh LM, Cobbold SA, et al.
Reference: 
Cell Rep. 2019 Nov 26;29(9):2917-2928.e5

Increased tolerance of Plasmodium falciparum to front-line artemisinin antimalarials (ARTs) is associated with mutations in Kelch13 (K13), although the precise role of K13 remains unclear. Here, we show that K13 mutations result in decreased expression of this protein, while mislocalization of K13 mimics resistance-conferring mutations, pinpointing partial loss of function of K13 as the relevant molecular event.

Repurposing the antimalarial pyronaridine tetraphosphate to protect against Ebola virus infection

November 30, 2019 - 20:12 -- Open Access
Author(s): 
Lane TR, Massey C, Comer JE, Anantpadma M, Freundlich JS, Davey RA, Madrid PB, Ekins S
Reference: 
PLoS Negl Trop Dis. 2019 Nov 21;13(11):e0007890.

Recent outbreaks of the Ebola virus (EBOV) have focused attention on the dire need for antivirals to treat these patients. We identified pyronaridine tetraphosphate as a potential candidate as it is an approved drug in the European Union which is currently used in combination with artesunate as a treatment for malaria (EC50 between 420 nM-1.14 μM against EBOV in HeLa cells).

NOT Open Access | Antimalarial herbal remedies of Bukavu and Uvira areas in DR Congo: An ethnobotanical survey

November 28, 2019 - 06:32 -- NOT Open Access
Author(s): 
Mboni Henry Manya, Flore Keymeulen, Jérémie Ngezahayoc, Amuri Salvius Bakaria, Mutombo Emery Kalonda, Byanga Joh Kahumba, Pierre Duez, Caroline Stévigny, Simbi Jean-Baptiste Lumbu
Reference: 
Journal of Ethnopharmacology, 22 November 2019, 112422

The main objective of the present study was to collect and gather information on herbal remedies traditionally used for the treatment of malaria in Bukavu and Uvira, two towns of the South Kivu province in DRC.

Country: 

The genomic architecture of antimalarial drug resistance

November 26, 2019 - 20:17 -- Open Access
Author(s): 
Annie N Cowell, Elizabeth A Winzeler
Reference: 
Briefings in Functional Genomics, Volume 18, Issue 5, September 2019, Pages 314–328

Plasmodium falciparum and Plasmodium vivax, the two protozoan parasite species that cause the majority of cases of human malaria, have developed resistance to nearly all known antimalarials. The ability of malaria parasites to develop resistance is primarily due to the high numbers of parasites in the infected person’s bloodstream during the asexual blood stage of infection in conjunction with the mutability of their genomes.

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