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

January 19, 2021 - 16:04 -- Open Access
Ishiyama A, Hokari R, Nonaka K, Chiba T, Miura H, Otoguro K, Iwatsuki M
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
Reader J, van der Watt ME, Birkholtz LM, et al.
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
Kumarihamy M, Rosa LH, Techen N, Ferreira D, Croom EM Jr, Duke SO, Tekwani BL, Khan S, Nanayakkara NPD
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
Jiang T, Huang Y, Cheng W, Sun Y, Wei W, Wu K, Shen C, Fu X, Dong H, Li J.
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
Wang X, Xie Y, Jiang N, Wang J, Liang H, Liu D, Yang N, Sang X, Feng Y, Chen R, Chen Q
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
Sirignano C, Hammami S, El Mokni R, Blagborough AM, Luciano P, Rigano D, Scafati OT
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
Kifle ZD, Atnafie SA
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.

NOT Open Access | Cyclic peptide engineered from phytocystatin inhibitory hairpin loop as an effective modulator of falcipains and potent antimalarial

December 10, 2020 - 09:50 -- NOT Open Access
Mishra M, Singh V, Tellis MB, Joshi RS, Pandey KC, Singh S
J Biomol Struct Dyn. 2020 Dec 9:1-13

Cystatins are classical competitive inhibitors of C1 family cysteine proteases (papain family). Phytocystatin superfamily shares high sequence homology and typical tertiary structure with conserved glutamine-valine-glycine (Q-X-V-X-G) loop blocking the active site of C1 proteases. Here, we develop a cysteine-bounded cyclic peptide (CYS-cIHL) and linear peptide (CYS-IHL), using the conserved inhibitory hairpin loop amino acid sequence.

Molecular surveillance of antimalarial partner drug resistance in sub-Saharan Africa: a spatial-temporal evidence mapping study

November 18, 2020 - 12:27 -- Open Access
Hanna Y Ehrlich, Justin Jones, Sunil Parikh
Lancet Microbe. 2020 Sep;1(5):e209-e217.

Molecular markers for antimalarial drug resistance can be used to rapidly monitor the emergence and spatial distribution of resistance to artemisinin-based combination therapies (ACTs). Little has been done to analyse molecular surveillance efforts or to assess surveillance coverage. This study aimed to develop an evidence map to characterise the spatial-temporal distribution and sampling methodologies of drug resistance surveillance in sub-Saharan Africa, specifically focusing on markers associated with ACT partner drugs.

Defining the antimalarial activity of cipargamin in healthy volunteers experimentally infected with blood stage Plasmodium falciparum

November 18, 2020 - 12:18 -- Open Access
McCarthy JS, Abd-Rahman AN, Collins KA, Marquart L, Griffin P, Kümmel A, Fuchs A, Winnips C, Mishra V, Csermak-Renner K, Jain JP, Gandhi P
Antimicrob Agents Chemother. 2020 Nov 16:AAC.01423-20

The spiroindolone cipargamin, a new antimalarial compound that inhibits Plasmodium ATP4, is currently in clinical development. This study aimed to characterize the antimalarial activity of cipargamin in healthy volunteers experimentally infected with blood-stage Plasmodium falciparum Eight subjects were intravenously inoculated with parasite-infected erythrocytes and received a single oral dose of 10 mg cipargamin 7 days later. Blood samples were collected to monitor the development and clearance of parasitemia, and plasma cipargamin concentrations.


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