Artemisinin and its derivatives are a promising new class of antimalarial agents containing an endoperoxide bridge. [14C]Artemisinin alkylated various proteins in vitro. Between 5 and 18% of added drug bound to hemoproteins such as catalase, cytochrome c, and hemoglobin. However, it did not react with heme-free globin. For catalase and hemoglobin, most of the drug reacted with the protein moiet...

The interest of Western medicine in Traditional Chinese Medicine (TCM) as a source of drug leads/new drugs to treat diseases without available efficient therapies has been dramatically augmented in the last decades by the extensive work and the outstanding findings achieved within this kind of medicine. The practice of TCM over thousands of years has equipped scientists with substantial experie...

Cytochrome P450 enzymes affected by artemisinin antimalarials – pharmacokinetic and pharmacogenetic aspects With more than 500 million cases and at least 1 million deaths each year, malaria is a major global health problem. The main problem with malaria control is the emerging drug resistance among parasites causing the infection. Consequently, there is an urgent need for new drugs. The artemis...

Artemisinin, a sesquiterpene lactone, is the active antimalarial constituent of Artemisia annua. Several fungal strains Saccharomyces cerevisiae, Aspergillus flavus, Aspergillus niger and Picchia pastoris were used to biotransform artemisinin. Among these strains, A. flavus was the only microorganism capable of transforming artemisinin to deoxyartemisinin in higher yields than the previous repo...

Artemisinin resistance represents a global concern, which requires a concerted and coordinated effort at a global level. Lessons learned from the experience of drug combination therapies in HIV, TB, and HCV infections showed that combination therapies reduce the risk of drug resistance development. In order to maximize the effectiveness of artemisinin and its derivates and to protect it from th...

Artemisia annua became a valuable agricultural crop after the World Health Organization recommended artemisinin as a component of ACT (artemisinin-combination based therapies) for malaria in 2001. A cloned, greenhouse-grown, A. annua (Artemis) subjected to an acidic soil and macronutrient deficit was evaluated for artemisinin production. Lack of lime (L) and macronutrients (N, P, and K) reduced...

Despite the importance of Artemisia annua L. as the only source of the anti-parasitic drug artemisinin, little is known on the effects of biotic and abiotic stress on artemisinin accumulation. Water deficit is the most limiting factor on plant growth, however it can trigger secondary metabolite accumulation, depending on the plant growth stage and intensity. A. annua cultivated in growth chambe...

Artemisinin-based combination therapies are the most effective drugs to treat Plasmodium falciparum malaria. Reduced sensitivity to artemisinin monotherapy, coupled with the emergence of parasite resistance to all partner drugs, threaten to place millions of patients at risk of inadequate treatment of malaria. Recognizing the significance and immediacy of this possibility, the Fogarty Internati...

MCF7 cells are an estrogen-responsive human breast cancer cell line that expresses both estrogen receptor (ER) alpha and ERbeta. Treatment of MCF7 cells with artemisinin, an antimalarial phytochemical from the sweet wormwood plant, effectively blocked estrogen-stimulated cell cycle progression induced by either 17beta-estradiol (E(2)), an agonist for both ERs, or by propyl pyrazole triol (PPT),...

Drugs are primary weapons for reducing malaria in human populations. However emergence of resistant parasites has repeatedly curtailed the lifespan of each drug that is developed and deployed. Currently the most effective anti-malarial is artemisinin, which is extracted from the leaves of Artemisia annua. Due to poor pharmacokinetic properties and prudent efforts to curtail resistance to monoth...