Artemisinin-based combination therapy (ACT) is the recommended first-line treatment for Plasmodium falciparum malaria. It has been suggested that the cytotoxic effect of artemisinin is mediated by free radicals followed by the alkylation of P. falciparum proteins. The endoperoxide bridge, the active moiety of artemisinin derivatives, is cleaved in the presence of ferrous iron, generating reacti...

Oxidative stress, owing to the excessive production of ROS (reactive oxygen species), is one of the leading causes for the progression of AD (Alzheimer’s disease). Increasing evidences suggested that oxidative stress insult impaired the physiological functioning of neuronal cells by inducing cell apoptosis. The search for drug candidates that can effectively protect neurons from oxidative stres...

Artemisinin (qinghaosu), extracted from the Chinese herb Artemisia annua L. in 1972, and its three major derivatives--artemether, artesunate and dihydroartemisinin--were firstly identified as antimalarials and found active against all species of the malaria parasite. Since the early 1980s, artemisinin and its derivatives have been found efficacious against Schistosoma spp., notably larval paras...

Novel artemisinin-glycolipid hybrids were directly synthesized from 12β (C-C)-type deoxoartemisinin and glycolipid and exhibited exceptional in vitro anticancer activity, particularly against the oral carcinoma cancer cell lines, respectively. The artemisinin-glycolipid hybrids, with effective concentrations under 20 µM, demonstrated better anticancer activity than either artemisinin or glycoli...

Current first-line artemisinin antimalarials are threatened by the emergence of resistant Plasmodium falciparum. Decreased sensitivity is evident in the initial (early ring) stage of intraerythrocytic development, meaning that it is crucial to understand the action of artemisinins at this stage. Here, we examined the roles of iron (Fe) ions and haem in artemisinin activation in early rings usin...

Artemisinin resistance in Plasmodium falciparum threatens global efforts in the elimination or eradication of malaria. Several studies have associated mutations in the PfATP6 gene in conjunction with artemisinin resistance, but the underlying molecular mechanism of the resistance remains unexplored. Associated mutations act as a biomarker to measure the artemisinin efficacy. In the proposed wor...

Artemisinin (quinghaosu) is a natural compound, isolated from Artemisia annua L. (Compositae), of current interest in treatment of drug-resistant malaria. Aim of the current study was to hit upon novel artemisinin sources as alternative to A. annua. Therefore, ten species of the genus Artemisia (A. santonicum L., A. taurica Willd., A. spicigera K. Koch, A. herba-alba Asso, A. haussknechtii Bois...

The immediate efficacies of two oral dosage regimens of artemisinin were investigated in 77 male and female adult Vietnamese falciparum malaria patients randomly assigned to treatment with either 500 mg of artemisinin daily for 5 days (group A; n = 40) or artemisinin at a dose of 100 mg per day for 2 days, with the dose increased to 250 mg per day for 2 consecutive days and with a final dose of...

artemisia annua is still the only commercial source of artemisinin. to date, a number of biochemical and molecular studies about artemisinin’s biosynthetic pathway have been carried out. in metabolic engineering approach, isolation and characterization of promoters leads to an understanding of which cis-acting elements are responsible for the regulation of gene expression. dbr2 is a key enzyme ...

artemisinin and its derivatives are very important new class of antimalarial drugs. one of the most important artemisinin derivatives is artemether. the antiparasitic activity of artemether as a derivative of artemisinin is related to endoperoxide bridge in its structure. the aim of this study was the evaluation of antileishmanial effect of artemether, with more focus on its apoptotic effect. i...