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antimalarial

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

November 18, 2020 - 12:27 -- Open Access
Author(s): 
Hanna Y Ehrlich, Justin Jones, Sunil Parikh
Reference: 
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
Author(s): 
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
Reference: 
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.

Not Open Access | Comparative antimalarial, toxicity and mito-protective effects of Diospyros mespiliformis Hochst. ex A. DC. and Mondia whitei (Hook.f.) Skeels on Plasmodium berghei infection in mice

November 18, 2020 - 11:41 -- NOT Open Access
Author(s): 
Olanlokun JO, Bodede O, Prinsloo G, Olorunsogo OO
Reference: 
J Ethnopharmacol. 2020 Nov 12:113585

Diospyros mespiliformis Hochst. ex A. DC. and Mondia whitei (Hook.f.) Skeels are traditionally used in Africa for the treatment of malaria. However, scientific evidence to substantiate this folkloric claim and their effects on liver mitochondria during malaria treatment have not been reported.

Aim of the study

This study investigated the efficacy of D. mespiliformis and M. whitei against chloroquine-sensitive and resistant strains of malarial parasites in mice. It also investigated the toxicity and protection against cellular organelles like mitochondria.

NOT Open Access | Antimalarial properties and preventive effects on mitochondrial dysfunction by extract and fractions of Phyllanthus amarus (Schum. and Thonn) in Plasmodium berghei-infected mice

November 10, 2020 - 14:30 -- NOT Open Access
Author(s): 
Olanlokun JO, Babarinde CO, Olorunsogo OO
Reference: 
J Basic Clin Physiol Pharmacol. 2020 Nov 6, 20200046, eISSN 2191-0286, ISSN 0792-6855

Broad spectrum antimalarial drugs without deleterious effects on mitochondria are scarce. It is in this regard that we investigated the potency of methanol extract and solvent fractions of Phyllanthus amarus on chloroquine-susceptible and resistant strains of Plasmodium berghei, toxicity and its consequential effects on mitochondrial permeability transition (mPT) pore opening.

Protein modification characteristics of the malaria parasite Plasmodium falciparum and the infected erythrocytes

November 7, 2020 - 13:04 -- Open Access
Author(s): 
Wang J, Jiang N, Sang X, Yang N, Feng Y, Chen R, Wang X, Chen Q
Reference: 
Mol Cell Proteomics. 2020 Nov 4:mcp.RA120.002375

Malaria elimination is still pending on the development of novel tools that rely on a deep understanding of parasite biology. Proteins of all living cells undergo a myriad number of posttranslational modifications (PTMs) that are critical to multifarious life processes. An extensive proteome-wide dissection revealed a fine PTM map of most proteins in both Plasmodium falciparum, the causative agent of severe malaria, and the infected red blood cells.

Tutankhamun's Antimalarial Drug for Covid-19

November 4, 2020 - 10:28 -- Open Access
Author(s): 
Sommer AP, Försterling HD, Sommer KE
Reference: 
Drug Res (Stuttg). 2020 Oct 30

Drug repositioning is a strategy that identifies new uses of approved drugs to treat conditions different from their original purpose. Current efforts to treat Covid-19 are based on this strategy. The first drugs used in patients infected with SARS-CoV-2 were antimalarial drugs. It is their mechanism of action, i. e., rise in endosomal pH, which recommends them against the new coronavirus.

Not Open Access | Two in one: bifonctional derivatives of trolox acting as antimalarial and antioxidant agents

October 13, 2020 - 12:31 -- NOT Open Access
Author(s): 
Souard F, Nicolle E, Cressend D, Valentin A, Boumendjel A
Reference: 
Future Med Chem. 2020 Oct 9

The aim of the present work was to set-up compounds that are able to act simultaneously as antimalarial and antioxidants. Trolox, a known antioxidant was chosen as a core structure to ensure the antioxidant activity and contribute to antiplasmodial effect.

NOT Open Access | Synthesis, structure-activity relationship and antimalarial efficacy of 6-chloro-2-arylvinylquinolines

September 23, 2020 - 09:30 -- NOT Open Access
Author(s): 
Huang G, Murillo Solano C, Yuan Y, et al.
Reference: 
J Med Chem. 2020 Sep 22

There is an urgent need to develop new efficacious antimalarials to address the emerging drug-resistant clinical cases. Our previous phenotypic screening identified styrylquinoline UCF501 as a promising antimalarial compound.

Not Open Access | Probing the B- & C-rings of the antimalarial tetrahydro-β-carboline MMV008138 for steric and conformational constraints

September 10, 2020 - 08:33 -- NOT Open Access
Author(s): 
Ding S, Ghavami M, Butler JH, Merino EF, Slebodnick C, Cassera MB, Carlier PR
Reference: 
Bioorg Med Chem Lett. 2020 Sep 5:127520

The antimalarial candidate MMV008138 (1a) is of particular interest because its target enzyme (IspD) is absent in human. To achieve higher potency, and to probe for steric demand, a series of analogs of 1a were prepared that featured methyl-substitution of the B- and C-rings, as well as ring-chain transformations.

Antimalarial artemisinin-based combination therapies (ACT) and COVID-19 in Africa: In vitro inhibition of SARS-CoV-2 replication by mefloquine-artesunate

August 19, 2020 - 09:15 -- Open Access
Author(s): 
Gendrot M, Duflot I, Boxberger M, Delandre O, Jardot P, Le Bideau M, Andreani J, Fonta I, Mosnier J, Rolland C, Hutter S, La Scola B, Pradines B
Reference: 
Int J Infect Dis. 2020 Aug 14:S1201-9712(20)30661-5

At the end of November 2019, a novel coronavirus responsible for respiratory tract infections (COVID-19) emerged in China. Despite drastic containment measures, this virus, known as severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), spread in Asia and Europe. The pandemic is ongoing with particular hotspot in Southern Europe and America. Many studies predicted a similar epidemic in Africa as that currently seen in Europe and the United States of America. However, reported data do not confirm these predictions. One of the hypotheses that could explain the later emergence and spread of COVID-19 pandemic in African countries is the use of antimalarial drugs to treat malaria, and more particularly artemisinin-based combination therapy (ACT).

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