antimalarial

Not Open Access | The Antimalarial Natural Product Salinipostin A Identifies Essential α/β Serine Hydrolases Involved in Lipid Metabolism in P. falciparum Parasites

Tags:

antimalarial, salinipostin A, serine hydrolase, lipid metabolism, p. falciparum, parasites

Author(s):

Yoo E, Schulze CJ, Stokes BH, Onguka O, Yeo T, Mok S, Gnädig NF, Zhou Y, Kurita K, Foe IT, Terrell SM, Boucher MJ, Cieplak P, Kumpornsin K, Lee MCS, Linington RG, Long JZ, Uhlemann AC, Weerapana E, Fidock DA, Bogyo M

Reference:

Cell Chem Biol. 2020 Feb 20;27(2):143-157.e5

Salinipostin A (Sal A) is a potent antiplasmodial marine natural product with an undefined mechanism of action. Using a Sal A-derived activity-based probe, we identify its targets in the Plasmodium falciparum parasite. All of the identified proteins contain α/β serine hydrolase domains and several are essential for parasite growth. One of the essential targets displays a high degree of homology to human monoacylglycerol lipase (MAGL) and is able to process lipid esters including a MAGL acylglyceride substrate.

NOT Open Access | Potential antimalarial activity of Coccinia barteri leaf extract and solvent fractions against Plasmodium berghei infected mice

Tags:

antimalarial, coccinia barteri, leaf extract, solvent fractions, plasmodium berghei, infected mice

Author(s):

Orabueze CI, Obi E, Adesegun SA, Coker HA

Reference:

Journal of Ethnopharmacology, Volume 248, 10 February 2020, 112334

Coccinia barteri (Hook. F.) is traditional used in Southeast of Nigeria in management of fever. This study aimed to evaluate the antimalarial activities of hydro-methanol crude extract and solvent fractions of Coccinia barteri leaf.

Not Open Access | Schistosoma haematobium infection modulates Plasmodium falciparum parasite density and antimalarial antibody responses

Tags:

schistosoma haematobium infection, plasmodium falciparum, parasite density, antimalarial, antibody responses

Author(s):

Tokplonou L, Nouatin O, Courtin D, et al.

Reference:

Parasite Immunol. 2020 Feb 5:e12702

Schistosomiasis and malaria are endemic in sub‐Saharan Africa where Schistosoma haematobium (Sh) and Plasmodium falciparum (Pf) coinfections are thus frequent. We explored the effect of Sh infection on antibody responses directed to Pf merozoite antigens and on malaria susceptibility in Beninese children.

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

Tags:

Flavonoid Compounds, Citrus Species, antimalarial

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

Tags:

antimalarial, Hydromethanolic, Crude Extract, solvent fractions, Nuxia congesta, Ex Fresen, Buddlejaceae, plasmodium berghei, infected mice

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

Tags:

Current progress, antimalarial, pharmacotherapy, drug discovery

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

Tags:

2-Aminomethylphenol, antimalarial, JPC-3210, aotus monkey, human, model

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

Tags:

antimalarial, cell penetrating, Peptide TP10, Primaquine, chloroquine, Hemolytic Conjugates

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

Tags:

antimalarial, malaria, asymptomatic, diagnosis, elimination, reservoir, clinical disease

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

Tags:

malaria artemisinin, antimalarial, kelch13, proteomics, silac, protein turnover, cytostome

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.

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