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NOT Open Access | The Effect of Gastric pH on the Pharmacokinetics-Pharmacodynamics of Naphthoquine in Rodents, as well as in Human Predicted Using a PBPK Model

February 2, 2021 - 17:02 -- NOT Open Access
Xie Y, Liu H, Chen X, Xing J
Curr Drug Metab. 2021 Jan 28

Fixed-dose combination of artemisinin and naphthoquine (NQ) is a new artemisinin-based combination therapy for the treatment of uncomplicated Plasmodium falciparum. NQ absorption has been reported to be affected by food in human.

NOT Open Access | Polyoxometalates as catalysts for fluorescence amplification in rapid and sensitive detection of artemisinin.

January 27, 2021 - 15:26 -- NOT Open Access
Gao Y, Tian M, Jia Y, Wang X, Yang L
Anal Chim Acta. 2021 Jan 25;1143:101-108

The combination therapy based on artemisinin is the most effective method to treat malaria. Sensitive, rapid and accurate detection of artemisinin is very important to monitor clinical pharmaceutical effect as well as the drug quality control. In this work, catalytic performance of polyoxometalates (POMs), vanadomolybdophosphoric heteropoly acid (H5PMo10V2O40, PMoV2) and tungstophosphoric heteropoly acid (Na5PW11O39Cu, PW11Cu), are investigated. It is indicated that the POMs exhibit peroxidase-like activity, which efficiently catalyze the artemisinin/thiamine reaction to produce fluorescent product thiochrome.

NOT Open Access | Artemisinin inhibits TLR4 signaling by targeting co-receptor MD2 in microglial BV-2 cells and prevents lipopolysaccharideinduced blood brain barrier leakage in mice

January 19, 2021 - 16:11 -- NOT Open Access
Zhang T, Zhang X, Lin C, Wu S, Wang F, Wang H, Wang Y, Peng Y, Hutchinson MR, Li H, Wang X
J Neurochem. 2021 Jan 16

Artemisinin and its derivatives have been the frontline drugs for treating malaria. In addition to the antiparasitic effect, accumulating evidence shows that artemisinins can alleviate neuroinflammatory responses in the central nervous system (CNS). However, the precise mechanisms underlying their anti-neuroinflammatory effects are unclear. Herein we attempted to delineate the molecule target of artemisinin in microglia. In vitro protein intrinsic fluorescence titrations and saturation transfer difference (STD)-NMR showed the direct binding of artemisinin to TLR4 co-receptor MD2.

NOT Open Access | Dihydroartemisinin, an active metabolite of artemisinin, interferes with Leishmania braziliensis mitochondrial bioenergetics and survival

January 12, 2021 - 14:55 -- NOT Open Access
Grazzia N, Boaventura S Jr, Garcia VL, Gadelha FR, Miguel DC
Parasitol Res. 2021 Jan 8

Leishmaniasis is one of the most neglected parasitic infections of the world and current therapeutic options show several limitations. In the search for more effective drugs, plant compounds represent a powerful natural source. Artemisinin is a sesquiterpene lactone extracted from Artemisia annua L. leaves, from which dihydroartemisinin (DQHS) and artesunic acid (AA)/artesunate are examples of active derivatives.

Increase in Kelch 13 Polymorphisms in Plasmodium falciparum, Southern Rwanda

January 7, 2021 - 09:11 -- Open Access
Bergmann C, van Loon W, Habarugira F, Tacoli C, Jäger JC, Savelsberg D, Nshimiyimana F, Rwamugema E, Mbarushimana D, Ndoli J, Sendegeya A, Bayingana C, Mockenhaupt FP
Emerg Infect Dis. 2021 Jan;27(1):294-296

Artemisinin resistance in Plasmodium falciparum is associated with nonsynonymous mutations in the Kelch 13 (K13) propeller domain.

Not Open Access | Antiplasmodial Combined Formulation of Artemisinin with Peschiera fuchsiaefolia Bis-Indole Alkaloids

January 6, 2021 - 13:20 -- NOT Open Access
Konan KV, Le TC, Mateescu MA
J Pharm Sci. 2021 Jan;110(1):135-145

Antimalarial agents used as monotherapy are increasingly ineffective due to the emergence of Plasmodium resistant strains. Artemisinin (Arte), extracted from Artemisia annua, presents a good efficiency against the Plasmodium strains and is currently used to treat malaria. To avoid the appearance of new resistant strains to artemisinin, the use of Artemisinin-based Combination Therapy (ACT) with another antimalaria agent was recommended by WHO to provide an effective cure and delayed resistance.

NOT Open Access | Enhanced Antimalarial Efficacy Obtained by Targeted Delivery of Artemisinin in Heparin-Coated Magnetic Hollow Mesoporous Nanoparticles

December 29, 2020 - 15:29 -- NOT Open Access
Wang X, Xie Y, Jiang N, Wang J, Liang H, Liu D, Yang N, Sang X, Feng Y, Chen R, Chen Q
ACS Appl Mater Interfaces. 2020 Dec 24

Malaria is one of the deadliest infectious diseases threatening half of the world population. With the deterioration of the parasiticidal effect of the current antimalarials, novel approaches such as screening of more specific inhibitors and targeted delivery of drugs have been under intensive research. Herein, we prepare hollow mesoporous ferrite nanoparticles (HMFNs) of 200 nm with ferromagnetic properties using a one-pot hydrothermal reaction. A magnetically targeted drug-delivery system coloaded with artemisinin in the inner magnetite shell and heparin on the outer mesoporous shell (HMFN@ART@HEP) is developed.

NOT Open Access | Recent advances in Quantitative Structure-Activity Relationship models of antimalarial drugs

December 29, 2020 - 15:15 -- NOT Open Access
Ojha PK, Kumar V, Roy J, Roy K
Expert Opin Drug Discov. 2020 Dec 26

Due to emerging resistance to the first-line artemisinin-based antimalarials and lack of efficient vaccines and limited chemotherapeutic alternatives, there is an urgent need to develop new antimalarial compounds. In this regard, quantitative structure-activity relationship (QSAR) modeling can provide essential information about required physicochemical properties and structural parameters of antimalarial drug candidates.

Is malaria parasite ex-vivo viability reduction really "superior" to observed parasite clearance rate

December 29, 2020 - 15:06 -- Open Access
White NJ, Watson JA
J Infect Dis. 2020 Dec 28:jiaa790

Ina study of 10 P. falciparum infected volunteers with submicroscopic parasitemias given a single 200mg dose of artesunate, Rebelo et al (1) report a substantial difference in the ex-vivo growth of sequentially sampled circulating ring stage(2) parasites comparing infections with artemisin insensitive (Pfkelch wild type) and artemisinin resistant(PfkelchR539T)parasites.

NOT Open Access | Eugenol disrupts Plasmodium falciparum intracellular development during the erythrocytic cycle and protects against cerebral malaria

December 16, 2020 - 09:59 -- NOT Open Access
Pontes KAO, Silva LS, Pinheiro AAS, et al.
Biochim Biophys Acta Gen Subj. 2020 Dec 12:129813

Malaria is a parasitic disease that compromises the human host. Currently, control of the Plasmodium falciparum burden is centered on artemisinin-based combination therapies. However, decreased sensitivity to artemisinin and derivatives has been reported, therefore it is important to identify new therapeutic strategies.


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