Artemisinin, the endoperoxide sesquiterpene lactone produced by the Chinese medicinal
herb Artemisia annua, is very difficult to synthesise. Moreover, its production by mean of cell,
tissue or organ cultures is very low. Presently, only its extraction from cultivated plants is ...

Abstract Increasing resistance of Plasmodium falciparum malaria to antimalarial drugs is
posing a major threat to the global effort to “Roll Back Malaria”. Chloroquine and sulfadoxine-
pyrimethamine (SP) are being rendered increasingly ineffective, resulting in increasing ...

Artemisinin and its derivatives are well known antimalaria drugs and particularly useful for
the treatment of infection of Plasmodium falciparum malaria parasites resistant to traditional
antimalarials. Artemisinin has an endoperoxide bridge that is activated by intraparasitic ...

Abstract The compounds derived from the Chinese medicinal plant qinghao (Artemisia
annua) are the most rapidly acting of all antimalarial drugs. They are effective when given
parenterally, orally or by suppository. No serious adverse effect has yet been reported in ...

The artemisinin derivatives, dihydroartemisinin (DHA), artesunate, atemether and arteether,
are currently used for treatment of malaria in artemisinin combination therapies (ACT) with
longer half-life drugs. The demand is enormous-in 2005, the estimated global demand for ...

Background. Artemisinin is of special biological interest because of its outstanding
antimalarial activity. Recently, it was reported that artemisinin has antitumor activity. Its
derivatives, artesunate, arteether, and artemeter, also have antitumor activity against ...

Abstract Purpose of review: Artemisinin-based combination treatments have been the
mainstay of treatment for falciparum malaria in Southeast Asia for more than 10 years and
are now increasingly recommended as first-line treatment throughout the rest of the world.

Evidence is reviewed elucidating the mechanism of iron-induced triggering of antimalarial
trioxanes. As prodrugs, trioxanes undergo homolytic, inner-sphere, reductive cleavage by
ferrous iron to form sequentially oxy radicals, carbon radicals, high-valent iron-oxo ...

Abstract Parasite resistance to conventional antimalarial medicines has led, in recent years,
to a dramatic shift in malaria treatment. Sixty-seven countries with endemic Plasmodium
falciparum malaria, 41 of them in Africa, have recently adopted the highly effective ...

Multiple drug resistance is a significant problem in small-cell lung cancer (SCLC).
Artemisinin (ART) is a natural product used to treat drug-resistant malaria. The drug is
effective because the Fe2+ present in infected erythrocytes acts non-enzymatically to ...

Two authors independently assessed trials for eligibility and risk of bias, and extracted data.
We analysed primary outcomes in line with the WHO'Protocol for assessing and monitoring
antimalarial drug efficacy'and compared drugs using risk ratios (RR) and 95% confidence ...

Abstract: Artemisia annua is currently the only commercial source of the sesquiterpene
lactone artemisinin. Since artemisinin was discovered as the active component of A. annua
in early 1970s, hundreds of papers have focused on the anti-parasitic effects of ...

Abstract Artemisia annua L.(annual wormwood) contains the antimalarial artemisinin.
Aqueous preparations of the dried herb are included in the pharmacopoeia of the People's
Republic of China for treatment of fever and malaria. Fourteen healthy male volunteers ...

Abstract BackgroundArtemisinin-based combination therapy (ACT) reduces microscopically
confirmed gametocytemia and mosquito infection. However, molecular techniques have
recently revealed high prevalences of submicroscopic gametocytemia. Our objective here ...

Dihydroartemisinic acid (2) was isolated as a natural product from Artemisia annua in a 66%
yield, and its structure was confirmed by 1H and 13C NMR spectroscopy. Compound 2
could be chemically converted to artemisinin (4) under conditions that may also be ...

Background Artemisinin combination therapy (ACT) is now the recommended first-line
treatment for falciparum malaria throughout the world. Initiatives to eliminate malaria are
critically dependent on its efficacy. There is recent worrying evidence that artemisinin ...

In only two steps and in 70% overall yield, naturally occurring trioxane artemisinin (1) was
converted on a gram scale into C-10-carba trioxane dimer 3. This new, very stable dimer
was then transformed easily in one additional step into four different dimers 4-7. Alcohol ...

In the 1970s, Chinese government scientists working on a secret “Project 523” developed a
new class of potent antimalarial drugs, the artemisinins or qinghaosu derivatives. In mostly
unpublished work that has just been recognized by a 2011 Lasker Award to Tu Youyou, ...

A discrepancy seems to prevail with regard to the toxicity and safety of the artemisinin family
of antimalarials. While these compounds have been found to be virtually void of any serious
side effects in humans, their neurotoxicity in animal models has raised concerns about ...

:: Abstract The emergence and spread of drug resistant malaria represents a considerable
challenge to controlling malaria. To date, malaria control has relied heavily on a
comparatively small number of chemically related drugs, belonging to either the quinoline ...

Artemisinin was reduced to dihydroartemisinin and coupled to a carboxylic acid derivative of
quinine via an ester linkage. This novel hybrid molecule had potent activity against the 3D7
and (drug-resistant) FcB1 strains of Plasmodium falciparum in culture. The activity was ...

Abstract In western Cambodia, malaria parasites clear slowly from the blood after treatment
with artemisinin derivatives, but it is unclear whether this results from parasite, host, or other
factors specific to this population. We measured heritability of clearance rate by evaluating ...

Nine C-10 non-acetal derivatives of the natural trioxane artemisinin (1) were prepared as
dimers using some novel chemistry. As designed, each dimer was stable chemically. C-10
Olefinic dimers 7 and C-10 saturated dimers 8-13 all showed good to excellent ...

Artemisinin, a sesquiterpene lactone endoperoxide derived from the glandular secretory
trichomes (GSTs) of Artemisia annua, provides the basis for the most effective treatments of
malaria. The biology and biochemistry of GSTs of the Asteraceae and their biosynthesis of ...

Abstract The isolation in 1972 of artemisinin by Chinese scientists, and their development of
all the derivatives now used in the treatment of malaria today, were of outstanding
importance. The results which have accumulated both from the Chinese work and from ...

... Titre du document / Document title. Some aspects of the chemistry and biological activity of
artemisinin and related antimalarials. ... Résumé / Abstract. Developments taken place in the field
of artemisinin and related antimalarials during the last five years have been reviewed ...

Mechanism-based rational design and gram-scale chemical synthesis have produced some
new trioxane and endoperoxide antimalarial drug candidates that are efficacious and safe.
This review summarises recent achievements in this area of peroxide drug development ...

The discovery that the sesquiterpene peroxide yingzhaosu A (13) and 1, 2, 4-trioxane
artemisinin (14) are active against chloroquine-resistant strains of Plasmodium falciparum,
has opened a new era in the chemotherapy of malaria. In vitro and in vivo tests with ...

The bioavailability of β-and γ-cyclodextrin artemisinin complexes was evaluated in
comparison with a normal commercially available preparation, Artemisinin 250®. Twelve
healthy male volunteers participated in the study conducted according to a three-way ...

Abstract Artemisinin and its derivatives are currently recommended as first-line antimalarials
in regions where Plasmodium falciparum is resistant to traditional drugs. The cytotoxic
activity of these endoperoxides toward rapidly dividing human carcinoma cells and cell ...

We describe an analysis of genome variation in 825 P. falciparum samples from Asia and
Africa that identifies an unusual pattern of parasite population structure at the epicenter of
artemisinin resistance in western Cambodia. Within this relatively small geographic area, ...

This year's Lasker DeBakey Clinical Research Award goes to Youyou Tu for the discovery of
artemisinin and its use in the treatment of malaria—a medical advance that has saved
millions of lives across the globe, especially in the developing world.

This article reviews the discovery and the further studies on qinghaosu and its derivatives or
analogs over the last decades in the fields of medicinal chemistry and some pharmacology
research, with an emphasis on the progress achieved in China.

Abstract The study compared the clinical efficacy and safety of oral artemisinin and oral
artesunate as well as artemisinin pharmacokinetics during and after resolution of falciparum
malaria. Forty adults with symptomatic falciparum malaria were allocated at random to ...

Artemisinin, a sesquiterpene endoperoxide derived from a traditional Chinese herbal
remedy for fevers, is a promising new antimalarial drug, particularly useful against multidrug
resistant strains of P. falciparum. Despite widespread clinical use, its mode of action ...

Abstract Combination regimens that include artemisinin derivatives are recommended as
first line antimalarials in most countries where malaria is endemic. However, the mechanism
of action of artemisinin is not fully understood and the usefulness of this drug class is ...

Background Drug resistance in Plasmodium falciparum poses a major threat to malaria
control. Combination antimalarial therapy including artemisinins has been advocated
recently to improve efficacy and limit the spread of resistance, but artemisinins are ...

BACKGROUND: Artemisinin-resistant Plasmodium falciparum has been reported in Pailin,
western Cambodia, detected as a slow parasite clearance rate in vivo. Emergence of this
phenotype in western Thailand and possibly elsewhere threatens to compromise the ...

Abstract 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, ...

Abstract Artemisinin isolated from the aerial parts of Artemisia annua L. is a promising and
potent antimalarial drug which has a remarkable activity against chloroquine-resistant and
chloroquine-sensitive strains of Plasmodium falciparum, and is useful in treatment of ...

Abstract From aseptically grown Artemisia annua plantlets, shoot cultures were initiated.
Using different concentrations of auxine, cytokinine and sucrose, a suitable culture medium
was developed, with respect to the growth of the shoots and their artemisinin ...

Artemisinin, a sesquiterpene lactone endoperoxide, and a number of its precursors,
metabolites and semisynthetic derivatives have shown to possess antimalarial properties.
Several methods have been reported for the measurement of artemisinin and its main ...

The present review describes the current status of synthetic cyclic peroxides, trioxanes and
trioxolanes that show significant promise as antimalarial drugs because of their artemisinin-
like activity. The literature from 1996 onwards is critically surveyed to provide an update ...

Abstract The potent antimalarial sesquiterpene lactone, artemisinin, is produced in low
quantities by the plant Artemisia annua L. The source and regulation of the isopentenyl
diphosphate (IPP) used in the biosynthesis of artemisinin has not been completely ...

Methods A narrative description of the process of anti-malarial drug policy change, financing
and implementation in Kenya is assembled from discussions with stakeholders, reports,
newspaper articles, minutes of meetings and email correspondence between actors in the ...

In only four chemical steps from naturally occurring artemisinin (1), trioxane dimers 6 and 7
were prepared on a multigram scale in overall 32-44% yields. In mice, both isonicotinate N-
oxide dimer 6 and isobutyric acid dimer 7 were considerably more antimalarially ...

Artemisinin (1, qinghaosu), and the derivatives dihydroartemisinin (DHA, 2), artemether (3),
and artesunate (4) are the most potent and rapidly acting antimalarial drugs.[1–3]
Nevertheless, artemether (3) and artesunate (4) have short terminal half-lives, a ...

Abstract In all experimental mammals tested (rats, dogs, primates), intramuscular injections
of the oil-soluble antimalarial artemisinin derivatives artemether and arteether have
produced an unusual pattern of selective damage to brain stem centers predominantly ...

Abstract The recent emergence of artemisinin-resistant Plasmodium falciparum malaria in
western Cambodia could threaten prospects for malaria elimination. Identification of the
genetic basis of resistance would provide tools for molecular surveillance, aiding efforts to ...

Early parasitological diagnosis and treatment with artemisinin-based combination therapies
(ACTs) are key components of worldwide malaria elimination programmes. In general, use
of ACTs has been limited to patients with falciparum malaria whereas blood-stage ...

ABSTRACT Artemisinin (ART)-based combination therapies (ACTs) are the first-line drugs—
and often the last treatments—that can effectively cure Plasmodium falciparum infections.
Unfortunately, the decreased clinical efficacy of artesunate, one of the major ART ...

Background Artemisinin resistance in Plasmodium falciparum has emerged in Southeast
Asia and now poses a threat to the control and elimination of malaria. Mapping the
geographic extent of resistance is essential for planning containment and elimination ...

Dihydroartemisinic acid hydroperoxide (2) was isolated for the first time as a natural product
from the plant Artemisia annua in a 29% yield. Its structure was identified by 1H and 13C
NMR spectroscopy. Compound 2 is known as an intermediate of the photochemical ...

Abstract Plasmodium falciparum is the most important parasitic pathogen in humans,
causing hundreds of millions of malaria infections and millions of deaths each year. At
present there is no effective malaria vaccine and malaria therapy is totally reliant on the ...

Artemisinin and its derivatives, artesunate and artemether, represent a new class of
antimicrobial drug with potent activity against Plasmodium falciparum. Although they show
excellent efficacy in both severe and uncomplicated malaria, dosage regimens still need ...

Artemisinin reacts with iron to form free radicals that kill cells. Since cancer cells uptake
relatively large amount of iron than normal cells, they are more susceptible to the toxic effect
of artemisinin. In previous research, we have shown that artemisinin is more toxic to ...

Abstract The biological mode of action of artemisinin, a potent antimalarial, has long been
controversial. Previously we established a yeast model addressing its mechanism of action
and found mitochondria the key in executing artemisinin's action. Here we present data ...

ABSTRACT The sesquiterpene endoperoxide antimalarial agents arteether and artemether
have been reported to cause neurotoxicity with a discrete distribution in the brain stems of
rats and dogs after multiple doses. The nature and distribution of the brain lesions suggest ...

This is a reprint of a Cochrane review, prepared and maintained by The Cochrane Collaboration
and published in The Cochrane Library 2010, Issue 1 http://www.thecochranelibrary.com ... Artemisinin 
derivatives for treating severe malaria (Review) Copyright © 2010 The Cochrane ...

Abstract Artemisinin, a sesquiterpene lactone derived from the sweet wormwood plant
Artemisia annua, and its bioactive derivatives exhibit potent anticancer effects in a variety of
human cancer cell model systems. The pleiotropic response in cancer cells includes ...

Background Artemisinin combination therapies (ACT), which are increasingly being
introduced for treatment of Plasmodium falciparum malaria, are more effective against
sexual stage parasites (gametocytes) than previous first-line antimalarials and therefore ...

We determined the cytotoxicity of some artemisinin derivatives against EN2 tumor cells
using the MTT assay. Artemisinin (1) was clearly more cytotoxic than deoxyartemisinin (2),
which lacks the endoperoxide bridge. Ether-linked dimers of dihydroartemisinin with ...

Abstract Parasite clearance data from 18,699 patients with falciparum malaria treated with
an artemisinin derivative in areas of low (n= 14,539), moderate (n= 2077), and high (n=
2083) levels of malaria transmission across the world were analyzed to determine the ...

Abstract: This review covers developments in relation to artemisinin-based antimalarial
agents. Topics covered include a brief introduction to the history and treatment of malaria,
and more recently, drug resistant malaria; the discovery of the naturally occurring novel ...

Background The Home Management of Malaria (HMM) strategy was developed using
chloroquine, a now obsolete drug, which has been replaced by artemisinin-based
combination therapy (ACT) in health facility settings. Incorporation of ACT in HMM would ...

Production of fine chemicals from heterologous pathways in microbial hosts is frequently
hindered by insufficient knowledge of the native metabolic pathway and its cognate
enzymes; often the pathway is unresolved, and the enzymes lack detailed characterization ...

The potent antimalarial activity of chloroquine against chloroquine-sensitive strains can be
attributed, in part, to its high accumulation in the acidic environment of the heme-rich
parasite food vacuole. A key component of this intraparasitic chloroquine accumulation ...