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antimalarial drugs

Purification and initial characterization of Plasmodium falciparum K(+) channels, PfKch1 and PfKch2 produced in Saccharomyces cerevisiae

September 23, 2020 - 09:02 -- Open Access
Author(s): 
Molbaek K, Tejada M, Ricke CH, Scharff-Poulsen P, Ellekvist P, Helix-Nielsen C, Kumar N, Klaerke DA, Pedersen PA
Reference: 
Microb Cell Fact. 2020 Sep 21;19(1):183

Resistance towards known antimalarial drugs poses a significant problem, urging for novel drugs that target vital proteins in the malaria parasite Plasmodium falciparum. However, recombinant production of malaria proteins is notoriously difficult. To address this, we have investigated two putative K+ channels, PfKch1 and PfKch2, identified in the P. falciparum genome.

NOT Open Access | Exploration of Anti-plasmodial Activity of Prunus cerasoides Buch.-Ham. ex D. Don (family: Rosaceae) and Its Wood Chromatographic Fractions

September 22, 2020 - 10:14 -- NOT Open Access
Author(s): 
Sachdeva C, Kumar S, Kaushik NK
Reference: 
Acta Parasitol. 2020 Sep 17

Increasing resistance to the currently available antimalarial drugs is a leading cause of failure to control malaria. Plant-based medicines are commonly used to manage numerous infections, making medicinal plants the best possible source of alternative antimalarial drugs. The objective of this study is therefore to identify antimalarial potential of Prunus cerasoides.

Antimalarial drugs inhibit the replication of SARS-CoV-2: an in vitro evaluation

September 15, 2020 - 14:26 -- Open Access
Author(s): 
Gendrot M, Andreani J, Pradines B, et al.
Reference: 
Travel Med Infect Dis. 2020 Sep 8:101873

In December 2019, a new severe acute respiratory syndrome coronavirus (SARS-CoV-2) causing coronavirus diseases 2019 (COVID-19) emerged in Wuhan, China. African countries see slower dynamic of COVID-19 cases and deaths. One of the assumptions that may explain this later emergence in Africa, and more particularly in malaria endemic areas, would be the use of antimalarial drugs.

Artemisinin Derivatives Stimulate DR5-Specific TRAIL-Induced Apoptosis by Regulating Wildtype P53

September 12, 2020 - 14:54 -- Open Access
Author(s): 
Zhou X, Zijlstra SN, Soto-Gamez A, Setroikromo R, Quax WJ
Reference: 
Cancers (Basel). 2020 Sep 4;12(9):E2514

Artemisinin derivatives, widely known as commercial anti-malaria drugs, may also have huge potential in treating cancer cells. It has been reported that artemisinin derivatives can overcome resistance to tumor necrosis factor-related apoptosis-inducing ligand (TRAIL)-induced apoptosis in liver and cervical cancer cells. In our study, we demonstrated that artesunate (ATS) and dihydroartemisinin (DHA) are more efficient in killing colon cancer cells compared to artemisinin (ART).

Not Open Access | Artemisinin Resistance and the Unique Selection Pressure of a Short-acting Antimalarial

August 10, 2020 - 16:11 -- NOT Open Access
Author(s): 
Khoury DS, Cao P, Zaloumis SG, Davenport MP
Reference: 
Trends Parasitol. 2020 Aug 5:S1471-4922(20)30187-2

Resistance to the artemisinin derivatives, our most effective antimalarial drugs, has not manifest as a classical resistance phenotype in which parasites can tolerate higher drug concentrations.

NOT Open Access | Updated pharmacokinetic considerations for the use of antimalarial drugs in pregnant women

August 3, 2020 - 15:37 -- NOT Open Access
Author(s): 
Moore BR, Davis TME
Reference: 
Expert Opin Drug Metab Toxicol. 2020 Jul 30

The association between pregnancy and altered drug pharmacokinetic (PK) properties is acknowledged, as is its impact on drug plasma concentrations and thus therapeutic efficacy. However, there have been few robust PK studies of antimalarial use in pregnancy. Given that inadequate dosing for prevention or treatment of malaria in pregnancy can result in negative maternal/infant outcomes, along with the potential to select for parasite drug resistance, it is imperative that reliable pregnancy-specific dosing recommendations are established.

Hydroxychloroquine in rheumatic autoimmune disorders and beyond

July 28, 2020 - 14:03 -- Open Access
Author(s): 
Nirk EL, Reggiori F, Mauthe M
Reference: 
EMBO Mol Med. 2020 Jul 26:e12476q

Initially used as antimalarial drugs, hydroxychloroquine (HCQ) and, to a lesser extent, chloroquine (CQ) are currently being used to treat several diseases. Due to its cost-effectiveness, safety and efficacy, HCQ is especially used in rheumatic autoimmune disorders (RADs), such as systemic lupus erythematosus, primary Sjögren's syndrome and rheumatoid arthritis.

Molecular epidemiology of resistance to antimalarial drugs in the Greater Mekong subregion: an observational study

July 20, 2020 - 15:55 -- Open Access
Author(s): 
Imwong M, Dhorda M, White NJ, et al.
Reference: 
Lancet Infect Dis. 2020 Jul 14:S1473-3099(20)30228-0

The Greater Mekong subregion is a recurrent source of antimalarial drug resistance in Plasmodium falciparum malaria. This study aimed to characterise the extent and spread of resistance across this entire region between 2007 and 2018.

Polymorphisms of pfcrt, pfmdr1, and K13-propeller genes in imported falciparum malaria isolates from Africa in Guizhou province, China

July 20, 2020 - 15:28 -- Open Access
Author(s): 
She D, Wang Z, Liang Q, Lu L, Huang Y, Zhang K, An D, Wu J
Reference: 
BMC Infect Dis. 2020 Jul 16;20(1):513

Imported falciparum malaria from Africa has become a key public health challenge in Guizhou Province since 2012. Understanding the polymorphisms of molecular markers of drug resistance can guide selection of antimalarial drugs for the treatment of malaria. This study was aimed to analyze the polymorphisms of pfcrt, pfmdr1, and K13-propeller among imported falciparum malaria cases in Guizhou Province, China.

NOT Open Access | A Chemically Stable Fluorescent Mimic of Dihydroartemisinin, Artemether, and Arteether with Conserved Bioactivity and Specificity Shows High Pharmacological Relevance to the Antimalarial Drugs

July 20, 2020 - 14:52 -- NOT Open Access
Author(s): 
Sissoko A, Vásquez-Ocmín P, Duval R, et al.
Reference: 
ACS Infect Dis. 2020 Jul 10; 6(7):1532-1547

Three novel tracers designed as fluorescent surrogates of artemisinin-derived antimalarial drugs (i.e., dihydroartemisinin, artemether, arteether, and artemisone) were synthesized from dihydroartemisinin.

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