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Chloroquine: Autophagy inhibitor, antimalarial, bitter taste receptor agonist in fight against COVID-19, a reality check

April 22, 2021 - 08:29 -- Open Access
Sharma P, McAlinden KD, Ghavami S, Deshpande DA
Eur J Pharmacol. 2021 Apr 15;897:173928

The recent SARS-CoV-2 pandemic poses one of the greatest challenges to modern medicine. Therefore, identification of new therapeutic strategies seems essential either based on novel vaccines or drugs or simply repurposing existing drugs. Notably, due to their known safety profile, repurposing of existing drugs is the fastest and highly efficient approach to bring a therapeutic to a clinic for any new indication. One such drug that has been used extensively for decades is chloroquine (CQ, with its derivatives) either for malaria, lupus and rheumatoid arthritis.

NOT Open Access | Antimalarial Quinacrine and Chloroquine Lose Their Activity by Decreasing Cationic Amphiphilic Structure with a Slight Decrease in pH

March 30, 2021 - 14:21 -- NOT Open Access
Kitagawa T, Matsumoto A, Terashima I, Uesono Y
J Med Chem. 2021 Mar 27

Quinacrine (QC) and chloroquine (CQ) have antimicrobial and antiviral activities as well as antimalarial activity, although the mechanisms remain unknown. QC increased the antimicrobial activity against yeast exponentially with a pH-dependent increase in the cationic amphiphilic drug (CAD) structure. CAD-QC localized in the yeast membranes and induced glucose starvation by noncompetitively inhibiting glucose uptake as antipsychotic chlorpromazine (CPZ) did.

NOT Open Access | Discovery of Potent and Fast-Acting Antimalarial Bis-1,2,4-triazines

March 26, 2021 - 16:11 -- NOT Open Access
Priebbenow DL, Mathiew M, Baell JB, et al.
J Med Chem. 2021 Mar 24

Novel 3,3'-disubstituted-5,5'-bi(1,2,4-triazine) compounds with potent in vitro activity against Plasmodium falciparum parasites were recently discovered. To improve the pharmacokinetic properties of the triazine derivatives, a new structure-activity relationship (SAR) investigation was initiated with a focus on enhancing the metabolic stability of lead compounds.

Antioxidant and antimalarial properties of Sophora exigua Craib. root extract in Plasmodium berghei-infected mice

March 24, 2021 - 14:11 -- Open Access
Kaewdana K, Chaniad P, Jariyapong P, Phuwajaroanpong A, Punsawad C
Trop Med Health. 2021 Mar 19;49(1):24

Sophora exigua Craib. is commonly used in Thailand to reduce fever and increase postpartum breast milk production in women who have hypogalactia. However, there has been no report on the antioxidant and antimalarial properties of this plant. This study aimed to investigate the antioxidant and antimalarial activities of S. exigua root extract and to evaluate its acute toxicity in mice to confirm its safety.

Community acceptability to antimalarial mass drug administrations in Magude district, Southern Mozambique: A mixed methods study

March 24, 2021 - 14:03 -- Open Access
Galatas B, Nhantumbo H, Munguambe K, et al.
PLoS One. 2021 Mar 23;16(3):e0249080

This study aimed to capture the acceptability prior to, during and after the implementation of the first year of MDA rounds conducted under the Magude project, a malaria elimination project in southern Mozambique.

NOT Open Access | Genomic and Genetic Approaches to Studying Antimalarial Drug Resistance and Plasmodium Biology

March 17, 2021 - 17:19 -- NOT Open Access
Okombo J, Kanai M, Deni I, Fidock DA
Trends Parasitol. 2021 Mar 11:S1471-4922(21)00035-0

Recent progress in genomics and molecular genetics has empowered novel approaches to study gene functions in disease-causing pathogens. In the human malaria parasite Plasmodium falciparum, the application of genome-based analyses, site-directed genome editing, and genetic systems that allow for temporal and quantitative regulation of gene and protein expression have been invaluable in defining the genetic basis of antimalarial resistance and elucidating candidate targets to accelerate drug discovery efforts.

NOT Open Access | Variation in Calculating and Reporting Antimalarial Efficacy against Plasmodium falciparum in Sub-Saharan Africa: A Systematic Review of Published Reports

March 17, 2021 - 17:13 -- NOT Open Access
Plucinski MM, Hastings IM, Moriarty LF, Venkatesan M, Felger I, Halsey ES
Am J Trop Med Hyg. 2021 Mar 15:tpmd201481

Antimalarials, in particular artemisinin-based combination therapies (ACTs), are critical tools in reducing the global burden of malaria, which is concentrated in sub-Saharan Africa. Performing and reporting antimalarial efficacy studies in a transparent and standardized fashion permit comparison of efficacy outcomes across countries and time periods. This systematic review summarizes study compliance with WHO laboratory and reporting guidance pertaining to antimalarial therapeutic efficacy studies and evaluates how well studies from sub-Saharan Africa adhered to these guidelines.

NOT Open Access | Effects of the antimalarial lumefantrine on Lemna minor, Raphidocelis subcapitata and Chlorella vulgaris

March 17, 2021 - 16:55 -- NOT Open Access
Chia MA, Ameh I, Agee JT, Otogo RA, Shaba AF, Bashir H, Umar F, Yisa AG, Uyovbisere EE, Sha'aba RI
Environ Toxicol Pharmacol. 2021 Mar 11;85:103635

Lumefantrine is used to treat uncomplicated malaria caused by pure or mixed Plasmodium falciparum infections and as a prophylactic against recrudescence following artemether therapy. However, the pharmaceutical is released into the aquatic environment from industrial effluents, hospital discharges, and human excretion. This study assessed the effects of lumefantrine on the growth and physiological responses of the microalgae Chlorella vulgaris and Raphidocelis subcapitata (formerly known as Selenastrum capricornutum and Pseudokirchneriella subcapitata) and the aquatic macrophyte Lemna minor.

Not Open Access | Structure activity refinement of phenylsulfonyl piperazines as antimalarials that block erythrocytic invasion

March 17, 2021 - 09:37 -- NOT Open Access
Nguyen W, Dans MG, Sleebs BE, et al.
Eur J Med Chem. 2021 Mar 15;214:113253

The emerging resistance to combination therapies comprised of artemisinin derivatives has driven a need to identify new antimalarials with novel mechanisms of action. Central to the survival and proliferation of the malaria parasite is the invasion of red blood cells by Plasmodium merozoites, providing an attractive target for novel therapeutics. A screen of the Medicines for Malaria Venture Pathogen Box employing transgenic P. falciparum parasites expressing the nanoluciferase bioluminescent reporter identified the phenylsulfonyl piperazine class as a specific inhibitor of erythrocyte invasion.

NOT Open Access | Robenidine Analogues Are Potent Antimalarials in Drug-Resistant Plasmodium falciparum

March 17, 2021 - 09:31 -- NOT Open Access
Krollenbrock A, Li Y, Kelly JX, Riscoe MK
ACS Infect Dis. 2021 Mar 16

Robenidine is a veterinary drug used in the poultry industry to treat coccidiosis caused by parasites in the Eimeria genus. Though this compound and related aminoguanidines have recently been studied in other pathogens, the chemotype has not been systematically explored to optimize antimalarial activity despite the close genetic relationship between Eimeria and Plasmodium (both are members of the Apicomplexa phylum of unicellular, spore-forming parasites).


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