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NOT Open Access | Systematic review of artemisinin embryotoxicity in animals: Implications for malaria control in human pregnancy

July 7, 2020 - 13:15 -- NOT Open Access
González R, Pons-Duran C, Bardají A, Leke RGF, Clark R, Menendez C
Toxicol Appl Pharmacol. 2020 Jul 2:115127

Pregnant women are one of the most susceptible and vulnerable groups to malaria, the most important parasitic disease worldwide. Artemisinin-based combination therapies (ACTs) are recommended for the treatment of uncomplicated malaria in all population groups including pregnant women. However, due to the embryotoxicity observed in animal studies, ACTs have long been contraindicated during the first trimester in pregnant women.

Ultrastructural alterations in Plasmodium falciparum induced by chalcone derivatives

June 17, 2020 - 12:54 -- Open Access
Sinha S, Radotra BD, Medhi B, Batovska DI, Markova N, Sehgal R
BMC Res Notes. 2020 Jun 15; 13(1):290

Chalcones (1, 3-diaryl-2-propen-1-ones) and their derivatives are widely explored from the past decade for its antimalarial activity. To elucidate their mechanism of action on the malaria parasite, the ultrastructural changes with the action of these derivatives in different organelles of the parasite were studied in vitro. Infected RBCs [CQ sensitive (MRC-2) and CQ resistant (RKL-9) Plasmodium strain] were treated with three chalcone derivatives 1, 2 and 3 and standard drugs, i.e., CQ and artemisinin at twice their respective IC50 values for 24 h and then harvested, washed, fixed, embedded and stained to visualize ultra-structure changes before and after intervention of treatment under in vitro condition through transmission electron microscope.

Pregnancy outcomes and risk of placental malaria after artemisinin-based and quinine-based treatment for uncomplicated falciparum malaria in pregnancy: a WorldWide Antimalarial Resistance Network systematic review and individual patient data meta-analysis

June 2, 2020 - 13:57 -- Open Access
Saito M, Mansoor R, Guérin PJ, et al.
BMC Med. 2020 Jun 2; 18(1):138

Malaria in pregnancy, including asymptomatic infection, has a detrimental impact on foetal development. Individual patient data (IPD) meta-analysis was conducted to compare the association between antimalarial treatments and adverse pregnancy outcomes, including placental malaria, accompanied with the gestational age at diagnosis of uncomplicated falciparum malaria infection.

Anti-malarial drug, artemisinin and its derivatives for the treatment of respiratory diseases

May 19, 2020 - 14:18 -- Open Access
Cheong DHJ, Daniel Tan WS, Fred Wong WS, Tran T
Pharmacol Res. 2020 May 13:104901

Artemisinins are sesquiterpene lactones with a peroxide moiety that are isolated from the herb Artemisia annua. It has been used for centuries for the treatment of fever and chills, and has been recently approved for the treatment of malaria due to its endoperoxidase properties. Progressively, research has found that artemisinins displayed multiple pharmacological actions against inflammation, viral infections, and cell and tumour proliferation, making them effective against diseases. Moreover, it has displayed a relatively safe toxicity profile.

Experimentally engineered mutations in a ubiquitin hydrolase, UBP-1, modulate in vivo susceptibility to artemisinin and chloroquine in Plasmodium berghei

April 29, 2020 - 09:05 -- Open Access
Simwela NV, Hughes KR, Roberts AB, Rennie MT, Barrett MP, Waters AP
Antimicrob Agents Chemother. 2020 Apr 27. pii: AAC.02484-19

As resistance to artemisinins (current frontline drugs in malaria treatment) emerges in south East Asia, there is an urgent need to identify the genetic determinants and understand the molecular mechanisms underpinning such resistance. Such insights could lead to prospective interventions to contain resistance and prevent the eventual spread to other malaria endemic regions. Artemisinin reduced susceptibility in South East Asia (SEA) has been primarily linked to mutations in P. falciparum Kelch-13, which is currently widely recognised as a molecular marker of artemisinin resistance.

Agrobacterium-Mediated Transformation of Chrysanthemum with Artemisinin Biosynthesis Pathway Genes

April 27, 2020 - 13:00 -- Open Access
Firsov A, Mitiouchkina T, Shaloiko L, Pushin A, Vainstein A, Dolgov S
Plants (Basel). 2020 Apr 21;9(4). pii: E537

Artemisinin-based drugs are the most effective medicine for the malaria treatment. To date, the main method of artemisinin production is its extraction from wormwood plants Artemisia annua L. Due to the limitation of this source, considerable efforts are now directed to the development of methods for artemisinin production using heterologous expression systems. Artemisinin is a sesquiterpene lactone, synthesized through the cyclization of farnesyl diphosphate involved in other sesquiterpene biosynthetic systems.

Plasmodium falciparum ATP4 inhibitors to treat malaria: worthy successors to artemisinin

April 13, 2020 - 15:19 -- Open Access
Ashley EA, Phyo AP
Lancet Infect Dis. 2020 Apr 7. pii: S1473-3099(20)30139-0

Progress in controlling malaria has slowed in recent years and the annual death toll remains above 400 000 globally, with most deaths caused by Plasmodium falciparum. The joint threats of increasing resistance to insecticides, artemisinin derivatives, and almost all other antimalarials in current use make the development of new classes of antimalarials a high priority.

NOT Open Access | Effects and Mechanism of Action of Artemisinin on Mitochondria of Plasmodium berghei

April 7, 2020 - 06:22 -- NOT Open Access
Hou HP, Zhang GP, Ma LN, Su P, Zhang ZX, Dai BQ, Ye ZG
Chin J Integr Med. 2020 Apr;26(4):277-282

To study the antimalarial effects and mechanisms of artemisinin (Qinghaosu in Chinese, QHS) on mitochondria in mice infected with Plasmodium berghei.

NOT Open Access | Artemisinin sensitizes tumor cells to NK cell-mediated cytolysis

April 7, 2020 - 06:04 -- NOT Open Access
Lu Z, Bi J, Wan X
Biochem Biophys Res Commun. 2020 Apr 2;524(2):418-423

The antimalarial drug Artemisinin has been reported to possess direct anti-tumor effects on various types of tumor cells. However, its anti-tumor potential has not been fully revealed, and its effects on tumor susceptibility to immune surveillance by the host are still unknown. Natural killer (NK) cells are the first line in tumor surveillance by the host, and have been recognized as a promising target for tumor immunotherapy.

Dried Leaf Artemisia Annua Improves Bioavailability of Artemisinin via Cytochrome P450 Inhibition and Enhances Artemisinin Efficacy Downstream

February 17, 2020 - 12:34 -- Open Access
Desrosiers MR, Mittelman A, Weathers PJ
Biomolecules. 2020 Feb 7;10(2). pii: E254

Artemisia annua L. and artemisinin, have been used for millennia to treat malaria. We used human liver microsomes (HLM) and rats to compare hepatic metabolism, tissue distribution, and inflammation attenuation by dried leaves of A. annua (DLA) and pure artemisinin. For HLM assays, extracts, teas, and phytochemicals from DLA were tested and IC50 values for CYP2B6 and CYP3A4 were measured.


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