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antimalarial

Bloodstream infection with Acinetobacter baumanii in a Plasmodium falciparum positive infant: a case report

February 8, 2021 - 10:24 -- Open Access
Author(s): 
Akenten CW, Boahen KG, Marfo KS, Sarpong N, Dekker D, Struck NS, Osei-Tutu L, May J, Amuasi JH, Eibach D
Reference: 
J Med Case Rep. 2021 Feb 5;15(1):46

The increasing incidence of multi-antibiotic-resistant bacterial infections, coupled with the risk of co-infections in malaria-endemic regions, complicates accurate diagnosis and prolongs hospitalization, thereby increasing the total cost of illness. Further, there are challenges in making the correct choice of antibiotic treatment and duration, precipitated by a lack of access to microbial culture facilities in many hospitals in Ghana. The aim of this case report is to highlight the need for blood cultures or alternative rapid tests to be performed routinely in malaria patients, to diagnose co-infections with bacteria, especially when symptoms persist after antimalarial treatment.

Chemoprotective antimalarials identified through quantitative high-throughput screening of Plasmodium blood and liver stage parasites

January 26, 2021 - 15:14 -- Open Access
Author(s): 
Dorjsuren D, Eastman RT, Fidock DA, et al.
Reference: 
Sci Rep. 2021 Jan 22;11(1):2121

The spread of Plasmodium falciparum parasites resistant to most first-line antimalarials creates an imperative to enrich the drug discovery pipeline, preferably with curative compounds that can also act prophylactically. We report a phenotypic quantitative high-throughput screen (qHTS), based on concentration-response curves, which was designed to identify compounds active against Plasmodium liver and asexual blood stage parasites. Our qHTS screened over 450,000 compounds, tested across a range of 5 to 11 concentrations, for activity against Plasmodium falciparum asexual blood stages.

NOT Open Access | Antimalarial application of quinones: A recent update

January 20, 2021 - 08:02 -- NOT Open Access
Author(s): 
Patel OPS, Beteck RM, Legoabe LJ
Reference: 
Eur J Med Chem. 2021 Jan 15;210:113084

Atovaquone belongs to a naphthoquinone class of drugs and is used in combination with proguanil (Malarone) for the treatment of acute, uncomplicated malaria caused by Plasmodium falciparum (including chloroquine-resistant P. falciparum/P. vivax). Numerous quinone-derived compounds have attracted considerable attention in the last few decades due to their potential in antimalarial drug discovery.

Diatretol, an α, α'-dioxo-diketopiperazine, is a potent in vitro and in vivo antimalarial

January 19, 2021 - 16:04 -- Open Access
Author(s): 
Ishiyama A, Hokari R, Nonaka K, Chiba T, Miura H, Otoguro K, Iwatsuki M
Reference: 
J Antibiot (Tokyo). 2021 Jan 14:1-3

A fungal metabolite, diatretol, has shown to be a promising antimalarial agent.

Multistage and transmission-blocking targeted antimalarials discovered from the open-source MMV Pandemic Response Box

January 12, 2021 - 14:50 -- Open Access
Author(s): 
Reader J, van der Watt ME, Birkholtz LM, et al.
Reference: 
Nat Commun. 2021 Jan 11;12(1):269

Chemical matter is needed to target the divergent biology associated with the different life cycle stages of Plasmodium. Here, we report the parallel de novo screening of the Medicines for Malaria Venture (MMV) Pandemic Response Box against Plasmodium asexual and liver stage parasites, stage IV/V gametocytes, gametes, oocysts and as endectocides. Unique chemotypes were identified with both multistage activity or stage-specific activity, including structurally diverse gametocyte-targeted compounds with potent transmission-blocking activity, such as the JmjC inhibitor ML324 and the antitubercular clinical candidate SQ109.

Antimalarials and Phytotoxins from Botryosphaeria dothidea Identified from a Seed of Diseased Torreya taxifolia

January 1, 2021 - 15:58 -- Open Access
Author(s): 
Kumarihamy M, Rosa LH, Techen N, Ferreira D, Croom EM Jr, Duke SO, Tekwani BL, Khan S, Nanayakkara NPD
Reference: 
Molecules. 2020 Dec 24;26(1):E59

The metabolic pathways in the apicoplast organelle of Plasmodium parasites are similar to those in plastids in plant cells and are suitable targets for malaria drug discovery. Some phytotoxins released by plant pathogenic fungi have been known to target metabolic pathways of the plastid; thus, they may also serve as potential antimalarial drug leads. An EtOAc extract of the broth of the endophyte Botryosphaeria dothidea isolated from a seed collected from a Torreya taxifolia plant with disease symptoms, showed in vitro antimalarial and phytotoxic activities.

NOT Open Access | Multiple SNPs detection for antimalarial pyrimethamine resistance via allele-specific PCR coupled with gold nanoparticles-based lateral flow biosensor

December 30, 2020 - 13:45 -- NOT Open Access
Author(s): 
Jiang T, Huang Y, Cheng W, Sun Y, Wei W, Wu K, Shen C, Fu X, Dong H, Li J.
Reference: 
Antimicrob Agents Chemother. 2020 Dec 23:AAC.01063-20

Molecular genotyping holds tremendous potential to detect antimalarial drug resistance (ADR) related to single nucleotide polymorphisms (SNPs). However, it suffers from complicated procedures and expensive instruments. Thus, rapid point-of-care testing (POCT) molecular tools are urgently needed for field survey and clinical use. Herein, a POCT platform consisted of multiple allele-specific PCR (AS-PCR) and gold nanoparticles (AuNPs) based lateral flow biosensor was designed and developed for SNPs detection of Plasmodium falciparum dihydrofolate reductase (pfdhfr) gene related to pyrimethamine resistance.

NOT Open Access | Enhanced Antimalarial Efficacy Obtained by Targeted Delivery of Artemisinin in Heparin-Coated Magnetic Hollow Mesoporous Nanoparticles

December 29, 2020 - 15:29 -- NOT Open Access
Author(s): 
Wang X, Xie Y, Jiang N, Wang J, Liang H, Liu D, Yang N, Sang X, Feng Y, Chen R, Chen Q
Reference: 
ACS Appl Mater Interfaces. 2020 Dec 24

Malaria is one of the deadliest infectious diseases threatening half of the world population. With the deterioration of the parasiticidal effect of the current antimalarials, novel approaches such as screening of more specific inhibitors and targeted delivery of drugs have been under intensive research. Herein, we prepare hollow mesoporous ferrite nanoparticles (HMFNs) of 200 nm with ferromagnetic properties using a one-pot hydrothermal reaction. A magnetically targeted drug-delivery system coloaded with artemisinin in the inner magnetite shell and heparin on the outer mesoporous shell (HMFN@ART@HEP) is developed.

NOT Open Access | Polyoxygenated germacranes from Daucus carota and their antimalarial transmission blocking activity

December 29, 2020 - 15:12 -- NOT Open Access
Author(s): 
Sirignano C, Hammami S, El Mokni R, Blagborough AM, Luciano P, Rigano D, Scafati OT
Reference: 
Phytochemistry. 2020 Dec 23;183:112632

Chemical analysis of the aerial parts obtained from a Tunisian specimen of Daucus carota yielded to the isolation of six undescribed polyoxygenated germacranes and one elemanolide, along with one known metabolite. The stereostructures of the undescribed compounds were determined by extensive spectroscopic analysis including 1D and 2D NMR and HR-ESI-MS analysis.

Anti-Oxidant Potential and Antimalarial Effects of Acanthus polystachyus Delile (Acanthaceae) Against Plasmodium berghei: Evidence for in vivo Antimalarial Activity

December 23, 2020 - 10:32 -- Open Access
Author(s): 
Kifle ZD, Atnafie SA
Reference: 
J Exp Pharmacol. 2020 Dec 11;12:575-587

Malaria is among the most devastating and widespread tropical parasitic diseases which is more prevalent in developing countries. Acanthus polystachyus (Acanthaceae) leaves are traditionally used for the treatment of malaria in Ethiopia. This study aimed to investigate the in vivo antimalarial and in vitro antioxidant activity of the leaves extract of Acanthus polystachyus.

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