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antimalarial drug

Methodological approaches for analysing data from therapeutic efficacy studies

May 26, 2021 - 09:16 -- Open Access
Solange Whegang Youdom and Leonardo K. Basco
Malaria Journal 2021 20:228, 21 May 2021

Several anti-malarial drugs have been evaluated in randomized clinical trials to treat acute uncomplicated Plasmodium falciparum malaria. The outcome of anti-malarial drug efficacy studies is classified into one of four possible outcomes defined by the World Health Organization: adequate clinical and parasitological response, late parasitological failure, late clinical failure, early treatment failure.

NOT Open Access | Heme Detoxification in the Malaria Parasite: A Target for Antimalarial Drug Development

May 19, 2021 - 13:36 -- NOT Open Access
de Villiers KA, Egan TJ
Acc Chem Res. 2021 May 13

Over the last century, malaria deaths have decreased by more than 85%. Nonetheless, there were 405 000 deaths in 2018, mostly resulting from Plasmodium falciparum infection. In the 21st century, much of the advance has arisen from the deployment of insecticide-treated bed nets and artemisinin combination therapy. However, over the past few decades parasites with a delayed artemisinin clearance phenotype have appeared in Southeast Asia, threatening further gains. The effort to find new drugs is thus urgent. A prominent process in blood stage malaria parasites, which we contend remains a viable drug target, is hemozoin formation. This crystalline material consisting of heme can be readily seen when parasites are viewed microscopically.

NOT Open Access | An integrated virtual screening and drug repurposing strategy for the discovery of new antimalarial drugs against Plasmodium falciparum phosphatidylinositol 3-kinase

May 18, 2021 - 13:32 -- NOT Open Access
Verma K, Lahariya AK, Dubey S, Verma AK, Das A, Schneider KA, Bharti PK
J Cell Biochem. 2021 May 17

The emergence and spread of drug resistance in Plasmodium falciparum, the parasite causing the most severe form of human malaria, is a major threat to malaria control and elimination programs around the globe. With P. falciparum having evolved widespread resistance against a number of previously widely used drugs, currently, artemisinin (ART) and its derivatives are the cornerstones of first-line treatments of uncomplicated malaria. However, growing incidences of ART failure reflect the spread of ART-resistant P. falciparum strains.

NOT Open Access | Review of the mechanism underlying mefloquine-induced neurotoxicity

April 29, 2021 - 07:14 -- NOT Open Access
Martins AC, Paoliello MMB, Docea AO, Santamaria A, Tinkov AA, Skalny AV, Aschner M
Crit Rev Toxicol. 2021 Apr 27:1-8

Mefloquine, a potent blood schizontocide, is effective against drug-resistant Plasmodium falciparum. This property, along with its unique pharmacokinetic profile, makes mefloquine a widely prescribed antimalarial drug. However, several epidemiological studies have raised concerns on the safety of mefloquine as prophylaxis for malaria. Well-documented side-effects of mefloquine include abnormal dreams, insomnia, anxiety, and depressed mood, as well as nausea and dizziness (the last two most frequent effects).

NOT Open Access | Design, synthesis and biological evaluation of mono- and bisquinoline methanamine derivatives as potential antiplasmodial agents

April 20, 2021 - 15:27 -- NOT Open Access
Bokosi FRB, Beteck RM, Mbaba M, Mtshare TE, Laming D, Hoppe HC, Khanye SD
Bioorg Med Chem Lett. 2021 Apr 15;38:127855

Several classes of antimalarial drugs are currently available, although issues of toxicity and the emergence of drug resistant malaria parasites have reduced their overall therapeutic efficiency. Quinoline based antiplasmodial drugs have unequivocally been long-established and continue to inspire the design of new antimalarial agents. Herein, a series of mono- and bisquinoline methanamine derivatives were synthesised through sequential steps; Vilsmeier-Haack, reductive amination, and nucleophilic substitution, and obtained in low to excellent yields.

NOT Open Access | Plasmodium falciparum Ferredoxin-NADP(+) Reductase-Catalyzed Redox Cycling of Plasmodione Generates Both Predicted Key Drug Metabolites: Implication for Antimalarial Drug Development

April 20, 2021 - 15:10 -- NOT Open Access
Cichocki BA, Donzel M, Heimsch KC, Lesanavičius M, Feng L, Montagut EJ, Becker K, Aliverti A, Elhabiri M, Čėnas N, Davioud-Charvet E
ACS Infect Dis. 2021 Apr 15

Plasmodione (PD) is a potent antimalarial redox-active 3-benzyl-menadione acting at low nanomolar range concentrations on different malaria parasite stages. The specific bioactivation of PD was proposed to occur via a cascade of redox reactions starting from one-electron reduction and then benzylic oxidation, leading to the generation of several key metabolites including corresponding benzylic alcohol (PD-bzol, for PD benzhydrol) and 3-benzoylmenadione (PDO, for PD oxide).

NOT Open Access | Antimalarial drug resistance markers in human immunodeficiency virus (HIV)-positive and HIV-negative adults with asymptomatic malaria infections in Port Harcourt, Nigeria

April 7, 2021 - 12:16 -- NOT Open Access
Chijioke-Nwauche I, Oguike MC, Nwauche CA, Beshir KB, Sutherland CJ
Trans R Soc Trop Med Hyg. 2021 Apr 6:trab061

In Nigeria, indiscriminate use of antimalarial drugs may contribute to the threat of drug resistance, but this has not been evaluated among people living with human immunodeficiency virus (HIV).

NOT Open Access | Multi-omics approaches to improve malaria therapy

April 1, 2021 - 08:55 -- NOT Open Access
Zhou M, Varol A, Efferth T
Pharmacol Res. 2021 Mar 22:105570

Malaria contributes to the most widespread infectious diseases worldwide. Even though current drugs are commercially available, the ever-increasing drug resistance problem by malaria parasites poses new challenges in malaria therapy. Hence, searching for efficient therapeutic strategies is of high priority in malaria control. In recent years, multi-omics technologies have been extensively applied to provide a more holistic view of functional principles and dynamics of biological mechanisms. We briefly review multi-omics technologies and focus on recent malaria progress conducted with the help of various omics methods.

NOT Open Access | Structure-switching aptamer sensors for the specific detection of piperaquine and mefloquine

March 24, 2021 - 15:06 -- NOT Open Access
Coonahan ES, Yang KA, Pecic S, De Vos M, Wellems TE, Fay MP, Andersen JF, Tarning J, Long CA
Sci Transl Med. 2021 Mar 17;13(585):eabe1535

Tracking antimalarial drug use and efficacy is essential for monitoring the current spread of antimalarial drug resistance. However, available methods for determining tablet quality and patient drug use are often inaccessible, requiring well-equipped laboratories capable of performing liquid chromatography-mass spectrometry (LC-MS). Here, we report the development of aptamer-based fluorescent sensors for the rapid, specific detection of the antimalarial compounds piperaquine and mefloquine-two slow-clearing partner drugs in current first-line artemisinin-based combination therapies (ACTs).

NOT Open Access | Superoxide: A major role in the mechanism of action of essential antimalarial drugs

March 17, 2021 - 16:48 -- NOT Open Access
Egwu CO, Tsamesidis I, Pério P, Augereau JM, Benoit-Vical F, Reybier K
Free Radic Biol Med. 2021 Mar 12:S0891-5849(21)00150-7

Understanding the mode of action of antimalarials is central to optimizing their use and the discovery of new therapeutics. Currently used antimalarials belong to a limited series of chemical structures and their mechanisms of action are continually debated. Whereas the involvement of reactive species that in turn kill the parasites sensitive to oxidative stress, is accepted for artemisinins, little is known about the generation of such species in the case of quinolines or hydroxynaphtoquinone. Moreover, the nature of the reactive species involved has never been characterized in Plasmodium-infected erythrocytes.


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