Heme alkylation by the antimalarial drug artemisinin is reported in vivo, within infected mice that have been treated at pharmacologically relevant doses. Adducts resulting from the alkylation of heme by the drug were characterized in the spleen of treated mice, and their glucuroconjugated derivatives were present in the urine. Because these heme-artemisinin adducts were not observed in noninfe...

Artemisinin, a sesquiterpene with endoperoxide bond, possesses potent antimalarial activity against the ring and late stage of chloroqine-resistant Plasmodium falciparum malaria both in vitro and in vivo. The mode of antimalarial activity of artemisinin is iron-dependent. The aim of this study was to investigate the reactions of artemisinin with ferrous and ferric ions in aqueous buffer. Artemi...

Malaria has been treated for over 350 years with quinine and quinine-derived drugs. However, in several areas of the world, some strains of the malarial parasite Plasmodium falciparum have developed resistance against these drugs. Recently, the World Health Organization (WHO) recommended the use of artemisinin-combination treatments (ACT) as the first-line treatment for multidrug-resistant falc...

Endoperoxide antimalarials based on the ancient Chinese drug Qinghaosu (artemisinin) are currently our major hope in the fight against drug-resistant malaria. Rational drug design based on artemisinin and its analogues is slow as the mechanism of action of these antimalarials is not clear. Here we report that these drugs, at least in part, exert their effect by interfering with the plasmodial h...

The susceptibility of Pneumocystis carinii to artemisinin (qinghaosu) was determined in short-term primary culture. In untreated cultures, trophozoites increased an average of fivefold over 4 days. Inhibition of parasite growth in cultures treated with artemisinin at concentrations as low as 0.5 microM was seen. In contrast, artemisinin concentrations up to 100 microM had no effect on feeder la...

Immunocompromised patients are at risk of developing toxoplasmosis, and although chemotherapy is available, standard treatments are often complicated by severe side effects. Artemisinin is a new highly potent antimalarial drug that has activity against Toxoplasma gondii in vitro. However, artemisinin derivatives have previously been ineffective in vivo using a rat model of toxoplasmosis. In the...

In the study we focus on determining the contents of artemisinin in Artemisia annua L. from different geographical origins of southwest district of China. The artemisinin contents of eleven samples are measured by the high performance liquid chromatography (HPLC). As a result, Artemisinin exists in different parts of A. annua plant and the content is as follow: inflorescences > leaves > stems. ...

Artemisinin is a potential antimalarial drug effective against the multidrug resistant forms of Malarial Parasites. The current production of artemisinin is insufficient to meet the global demand. In the present study microbial biotransformation of arteannuin B, a biogenetic precursor of artemisinin to the later has been investigated. Screening studies carried out on several soil borne microorg...

Artemisinin is a kind of Fe2+-dependent drugs. Artemisinin and Fe2+ co-transport systems can improve its anti-tumor effect. In this study, a visible light-sensitive nanoplatform (HA-TiO2-IONPs/ART) was developed. Detailed investigation demonstrated that HA-TiO2-IONPs/ART could realize Fe2+ and artemisinin synchronous co-delivery and tumor-responsive release. This feature enhanced the anti-tumor...

With the rapidly spreading resistance of Plasmodium falciparum to available non-artemisinin antimalarial drugs, new and novel pharmaceuticals are needed. ARCO is a new generation ACT, one of several artemisinin-based combinations developed in China to counter antimalarial drug resistance. ARCO is a derivative of two independently developed antimalarials, artemisinin and naphthoquine phosphate, ...