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Showing 1 to 20 of 65 for “"Artemisinin"”.
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Discovery of Alternative Artemisinin Binding Sites in Plasmodium falciparum ATPase-6
… malariae, ovale, vivax, and knowlesi species. Artemisinin is an endoperoxide lactone extracted from qinghaosu (Artemisia annua L. or sweet wormwood). It and its derivatives possess uncharacteristically rapid action against Plasmodium falciparum. Artemisinin is unique in its effectiveness in …
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Single and hybrid antimalarials based on artemisinin, chloroquine and ß-lactams : synthesis, antiplasmodial activity, cytotoxicity and effect of selected artemisinin-chloroquine hybrids on the parasitic endocytosis pathway
… reaction. 4-Aminoquinolines were hybridized with artemisinin or 1,4-naphthoquinone derivatives; selected hybrids were further investigated for their effect on the parasitic endocytosis pathway and compared to the effect of chloroquine and artemisinin on the same pathway. The effects of drug …
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Development of Artemisia annua L. as a crop for production of the antimalarial drug artemisinin
Artemisinin is the parent compound for the latest generation of anti-malarial drugs. In many cases of severe or drug-resistant malaria, the artemisinins are the only effective means of treatment for this common and life-threatening parasitic infection. However, the current supply of artemisinin is …
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Malaria treatment seeking behaviour and access to artemisinin combination therapy : a case of Mushin, Lagos, Nigeria
ACTs have been shown to be effective in treating malaria and are currently recommended as first-line drugs for the treatment of uncomplicated malaria in Nigeria because of resistance of malaria to chloroquine (CQ) and sulphadoxine pyrimethamine (SP). However, very little is known about malaria and …
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Artemisinin-Based Combination Therapy (ACTs) Drug Resistance Trends in <em>Plasmodium falciparum</em> Isolates in Southeast Asia
… drugs created to treat and prevent the disease. Artemisinin and its derivatives are the new gold standard for treatment of malaria, yet treatment failures in clinical studies are starting to be reported. Clearly, artemisinin resistance needs to be characterized and dealt with accordingly. In …
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Lipid Targets of the Antimalarial Trioxanes in <i>Plasmodium falciparum</i>
… The antimalarial trioxanes, exemplified by artemisinin, are among the few pharmaceuticals for which clinical resistance has not become widespread. Artemisinin is a naturally occurring sesquiterpene lactone, containing a unique endoperoxide pharmacophore. Despite extensive study, the precise …
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Part A: Antimalarial agents modified at the C-16 position of artemisinin; Part B: Lead optimization of falcipain-2 and falcipain-3 inhibitors
… Agents modified at the C-16 position of Artemisinin. Malaria is a widespread tropical and subtropical parasitic disease which is caused by malarial parasites and transmitted by the infected anopheles mosquitoe. The natural product artemisinin and its derivatives are currently considered …
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An investigation into the molecular mechanisms induced by derivatives of natural products in oesophageal cancer
… an unmet need for novel chemotherapeutic agents. Artemisinin derivatives, currently used to treat malaria, were recently shown to possess potent anticancer activity. This study investigated the potential of two first generation artemisinin derivatives (artesunate and dihydroartemisinin), together …
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Anti-malaria drug treatment in Vietnam
… "Roll Back Malaria". Antimalarial treatment with artemisinin, artesunate, or artemether has proved rapidly effective in the treatment of non complicated and complicated malaria and remarkably nontoxic. However there is a number of important questions that still need urgent attention: Should …
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Evaluating the cost-effectiveness of artemisinin-based combination antimalarial drugs and malaria rapid diagnostic tests within the context of effective vector control : case study of Southern Africa
… of effective vector control, the change to artemisinin-based combination therapies (ACTs) as first line malaria treatment and to evaluate the relevance of using definitive diagnosis (as opposed to clinical diagnosis) as the basis for initiating malaria treatment, especially when using ACTs …
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The characterization of pharmacokinetic properties and evaluation of in vitro drug combination efficacies of novel antimalarial compounds
… of the Chinese peroxidic antimalarial drug artemisinin primarily used in first-line combination therapy for treatment of P. falciparum malaria have proved to be highly effective. However, their use also is now compromised by the development of resistance by the parasite to the artemisinin …
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Synthesis, Chemistry, Biological Evaluation And Structure-Activity Relationships Of Rac- And Chiral 6-Desmethyl-5Β –Hydroxy-D-Secoartemisinin And Analogs
… and Plasmodium knowlesi. The natural product artemisinin is a sesquiterpene lactone with an endoperoxide bridge isolated from the Chinese annual herb qinghao (Artemisia annua L or sweet wormwood). The relatively stable endoperoxide bridge is essential for their antimalarial activity. The …
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Bioassay-guided fractionation of Artemisia afra for in vitro antimalarial activity against Plasmodium falciparum
… with novel modes of action against Plasmodium. Artemisinin or Qinghaosu is one such antimalarial isolated from a Chinese herb, Anemisia annua (Asteraceae) and it is currently undergoing phase I and II clinical trials. The Southern African species, Artemisia afra (African wormwood, wildeals, …
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Molekulární mechanismy indukce programované buněčné smrti v nádorových buňkách.
… práci jsou zkoumány látky shikonin, cnicin a artemisinin. Výsledky ukazují, že shikonin indukuje apoptosu nádorových buněk cestou snížení exprese C-MYC a aktivací tumor supresorové MST1 kinasy. Cnicin také snižuje expresi C-MYC, ale MST1 aktivuje pouze slabě. Artemisinin, na druhou stranu, …
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Discovery, Isolation, and Identification of Antimalarials from Fungal Endophytes
… that our endophytes were indeed producing artemisinin. Growth versus production studies were conducted to optimize our growth and extraction conditions while several other variables, like temperature and culture medium, were evaluated in an effort to improve our yields. Artemisinin …
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Cell cycle checkpoints and checkpoint kinases in the apicomplexan parasites Plasmodium and Toxoplasma
… and are mainly treated by the front-line drug artemisinin. Since the late 2000’s there has been a rise in artemisinin-resistant parasites in the Greater Mekong Subregion, and similar phenotypes have now been detected in some regions of Africa, proving this is becoming a more pressing issue. DNA …
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Novel formulations of a poorly soluble drug using the extrusion process.
… active pharmaceutical ingredients (APIs). Artemisinin was selected as a model drug which being thermolabile in nature and possesses processing challenges to processing HME. A low Tg amphiphillic copolymer, Soluplus® was selected as a matrix material. Drug-polymer compatibility was studied …
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Large–scale data–driven network analysis of human–plasmodium falciparum interactome: extracting essential targets and processes for malaria drug discovery
… Africa is traced mainly to Southeast Asia where artemisinin resistance rate is increasing. Although careful surveillance to monitor the emergence and spread of artemisinin-resistant parasite strains in Africa is on-going, research into new drugs, particularly, for African populations, is critical …
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The Effects of Naturally Occurring Plant Products on Experimental Haemonchus contortus Infection in Gerbils and Sheep
… larvae and treated once or daily for 5 days with artemisinin, Artemisia annua aqueous or ethanolic extract, an orange oil emulsion, or Asimina triloba ethanolic extract. Nine days post-infection, gerbils were euthanized, their stomachs removed, and the worms counted. Significant anthelmintic …
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Antimalarial Drug Resistance: Mechanisms of Emergence in Low-Transmission Settings
… America and Colombia. In 2006, Colombia adopted Artemisinin Combination Therapies (ACTs) as front-line antimalarial treatments, and withdrew the previous frontline therapy, sulfadoxine-pyrimethamine. While sulfadoxine-pyrimethamine resistance is widespread, no resistance to ACTs has been detected …
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