Artemisinins are a family of sesquiterpene trioxane lactone anti-malarial agents originally derived from Artemisia annua L. The anti-malarial action of artemisinins involves the formation of free radicals via cleavage of the endoperoxide bond in its structure, which mediate eradication of the Plasmodium species. With its established safety record in millions of malarial patients, artemisinins a...

The potent anti-malarial drug artemisinins are additionally anti-tumorigenic and inhibitory to yeast growth. The action mechanism of artemisinins, however, is not well understood. Heme and mitochondrial membrane are both suggested to be involved in the action of artemisinins. Because heme is also synthesized in the mitochondrion, mitochondria appear to be a critical organelle for artemisinins' ...

Artemisinins form the most important class of antimalarial currently available, particularly because they are effective against parasites resistant to almost all the other classes. Their mechanism of action is controversial. Some aspects of this controversy are reviewed here. Whilst there is no clinical resistance yet identified to artemisinins, the potential to examine the relationship between...

We examined the effects of praziquantel and the artemisinins on adult Echinostoma caproni. In vitro, both praziquantel and the artemisinins exhibited exposure-response relationships. In vivo, worm burden reductions of 100% were achieved with single oral doses of praziquantel, artesunate, and artemether at 50, 700, and 1,100 mg/kg of body weight, respectively.

Artemisinins with activity against K-1 strains of P. falciparum were modeled the HF/3-21G method. To identify key features artemisinins necessary for their activities, MEP maps built and used. The PCA HCA studies showed that variables HOMO-1 energy, DM, Q1, BA, nCs are responsible separation between more active less compounds. A PLS model three principal components explaining 89% total informat...

There are more than half a billion cases of malaria every year. Combinations of an artemisinin with other antimalarial drugs are now recommended treatments for Plasmodium falciparum malaria in most endemic areas. These treatment regimens act rapidly to relieve symptoms and effect cure. There is considerable controversy on how artemisinins work and over emerging indications of resistance to this...

We synthesized C-10 substituted triazolyl artemisinins by the Huisgen cycloaddition reaction between dihydroartemisinins (2) and variously substituted 1, 2, 3-triazoles (8a-8h). The antimalarial activities of 32 novel artemisinin derivatives were screened against a chloroquine-resistant parasite. Among them, triazolyl artemisinins with electron-withdrawing groups showed stronger antimalarial ac...

In 2010, there were estimated 219 million cases of malaria resulting in 666,000 deaths and two-thirds were children. Children are more vulnerable than adults to malaria parasites. In sub-Saharan African countries, maternal malaria is associated with up to 200,000 estimated infant deaths yearly. Malaria is caused by five Plasmodium parasites namely: Plasmodium falciparum, Plasmodium vivax, Plasm...

Artemisinins have become essential antimalarial drugs for increasingly widespread drug-resistant malaria strains. Although tremendous efforts have been devoted to decipher how this class of molecules works, their exact antimalarial mechanism is still an enigma. Several hypotheses have been proposed to explain their actions, including alkylation of heme by carbon-centered free radicals, interfer...