A group of SESQUITERPENES and their analogs that contain a peroxide group (PEROXIDES) within an oxepin ring (OXEPINS).
Agents used in the treatment of malaria. They are usually classified on the basis of their action against plasmodia at different stages in their life cycle in the human. (From AMA, Drug Evaluations Annual, 1992, p1585)
Tests that demonstrate the relative effectiveness of chemotherapeutic agents against specific parasites.
Sesquiterpenes are a class of terpenes consisting of three isoprene units, forming a 15-carbon skeleton, which can be found in various plant essential oils and are known for their diverse chemical structures and biological activities, including anti-inflammatory, antimicrobial, and cytotoxic properties.
Diminished or failed response of an organism, disease or tissue to the intended effectiveness of a chemical or drug. It should be differentiated from DRUG TOLERANCE which is the progressive diminution of the susceptibility of a human or animal to the effects of a drug, as a result of continued administration.
A species of protozoa that is the causal agent of falciparum malaria (MALARIA, FALCIPARUM). It is most prevalent in the tropics and subtropics.
Malaria caused by PLASMODIUM FALCIPARUM. This is the severest form of malaria and is associated with the highest levels of parasites in the blood. This disease is characterized by irregularly recurring febrile paroxysms that in extreme cases occur with acute cerebral, renal, or gastrointestinal manifestations.
A protozoan disease caused in humans by four species of the PLASMODIUM genus: PLASMODIUM FALCIPARUM; PLASMODIUM VIVAX; PLASMODIUM OVALE; and PLASMODIUM MALARIAE; and transmitted by the bite of an infected female mosquito of the genus ANOPHELES. Malaria is endemic in parts of Asia, Africa, Central and South America, Oceania, and certain Caribbean islands. It is characterized by extreme exhaustion associated with paroxysms of high FEVER; SWEATING; shaking CHILLS; and ANEMIA. Malaria in ANIMALS is caused by other species of plasmodia.
The concentration of a compound needed to reduce population growth of organisms, including eukaryotic cells, by 50% in vitro. Though often expressed to denote in vitro antibacterial activity, it is also used as a benchmark for cytotoxicity to eukaryotic cells in culture.
The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses.
Therapy with two or more separate preparations given for a combined effect.

Declining concentrations of dihydroartemisinin in plasma during 5-day oral treatment with artesunate for Falciparum malaria. (1/1442)

Six patients with uncomplicated falciparum malaria received artesunate for 5 days. Plasma concentrations of artesunate and dihydroartemisinin were determined by high-performance liquid chromatography with electrochemical detection. The concentrations of dihydroartemisinin in plasma 2 h after a dose showed a time-dependent decline. Concentrations of artesunate in plasma especially after the last dose, were very low. Despite this, all patients responded with a fast recovery.  (+info)

A randomized, double-blind, comparative trial of a new oral combination of artemether and benflumetol (CGP 56697) with mefloquine in the treatment of acute Plasmodium falciparum malaria in Thailand. (2/1442)

CGP 56697, a new oral fixed combination of artemether and benflumetol, was tested in a double-blinded, randomized trial in 252 adult patients treated either with CGP 56697 (4 x 4 tablets each containing 20 mg of artemether and 120 mg of benflumetol, given at 0, 8, 24, and 48 hr), or with mefloquine (three tablets of 250 mg at initial diagnosis, followed by two tablets of 250 mg at 8 hr). Baseline data of the two groups were comparable. The 28-day cure rate with CGP 56697 was lower than with mefloquine (69.3% versus 82.4%; P = 0.002). However, CGP 56697 was more effective than mefloquine in parasite clearance time (43 hr versus 66 hr; P < 0.001) fever clearance time (32 hr versus 54 hr; P < 0.005), and gametocyte clearance time (152 hr versus 331 hr; P < 0.001). This study revealed that CGP 56697 is effective against multidrug-resistant Plasmodium falciparum malaria in Thailand, but higher doses will probably be needed to improve the cure rate.  (+info)

The pharmacokinetics of artemisinin after administration of two different suppositories to healthy Vietnamese subjects. (3/1442)

Eight healthy Vietnamese male subjects received 400 mg artemisinin formulated into fatty suppositories (FS), and six different subjects received 500 mg of artemisinin formulated in polyethylene glycol suppositories (PEGS). Plasma concentrations were measured by high-performance liquid chromatography with electrochemical detection; concentration versus time curves were analyzed with nonparametric methods. No statistically significant differences were found between the two formulations. The maximum concentration (Cmax) was 100 +/- 102 microg/L (mean +/- SD, range = 24-330) microg/L (FS), the pharmacokinetic lag time (Tlag) was 1.3 +/- 1.0 hr (range = 0-3) (FS), and the time of the maximum concentration (Tmax) was 7.1 +/- 2.1 hr (range = 3-10) hr (FS). Because artemisinin is not available for intravenous dosage, absolute bioavailability cannot be assessed. However, compared with a previous study on oral artemisinin in healthy Vietnamese subjects, bioavailability relative to oral administration was estimated to be approximately 30%. We conclude that therapeutic blood concentrations of artemisinin can be reached after rectal dosage. The dose after rectal administration should probably be higher than after oral administration; doubling or tripling the oral dose might be necessary, which would imply a rectal dose of at least 20 mg/kg of body weight given twice a day.  (+info)

Effect of artemether on glucose uptake and glycogen content in Schistosoma japonicum. (4/1442)

AIM: To study the effect of artemether (Art) on glucose uptake and glycogen content in schistosomes. METHODS: Schistosomes recovered from mice treated intragastrically with Art 300 mg.kg-1 for 24-48 h, were incubated in the drug-free medium containing [U-14C]glucose 11.1 MBq.L-1. The glycogen content, [U-14C]glucose uptake, and incorporation of [U-14C]glucose into worm glycogen in both male and female worms were determined. RESULTS: When above-mentioned schistosomes were exposed to drug-free medium containing [U-14C]glucose for 1-24 h, the glycogen contents of male and female worms decreased 27%-61% and 39%-78%, respectively. Only 3 out of 6 male worm groups showed 23%-35% decrease in glucose uptake, while much less glucose uptake was found in female worms in all groups with reduction rates of 18%-38%. Apart from 2 male groups no apparent change in the incorporation of [U-14C]glucose into the worm glycogen was seen. CONCLUSIONS: Art-induced glycogen reduction in schistosomes was related to an inhibition of glycolysis rather than an interference with glucose uptake.  (+info)

Inhibitory effect of artemether on proteinase of Schistosoma japonicum. (5/1442)

AIM: To study the effect of artemether (Art) on the thio proteinase ("hemoglobinase", Hem) of Schistosoma japonicum. METHODS: Hem was extracted from S japonicum adults. The inhibitory effect of Art on the activity of Hem to degrade human hemoglobin (Hgb) was examined with UV-photometer at 280 nm, SDS-PAGE and scanning at 600 nm on a chromoscanner. RESULTS: Human Hgb was degraded at pH 4.0 by the Hem. The activities of Hem preincubated at 37 degrees C with Art 0.14, 1.4, and 14 mmol.L-1, were inhibited by 30.2%, 39.8%, and 45.0%, respectively. CONCLUSION: Art possesses an inhibitory effect to Hem of S japonicum.  (+info)

Metabolism of the antimalarial endoperoxide Ro 42-1611 (arteflene) in the rat: evidence for endoperoxide bioactivation. (6/1442)

Ro 42-1611 (arteflene) is a synthetic endoperoxide antimalarial. The antimalarial activity of endoperoxides is attributed to iron(II)-mediated generation of carbon-centered radicals. An alpha, beta-unsaturated ketone (enone; 4-[2',4' bis(trifluoromethyl)phenyl]-3-buten-2-one), obtained from arteflene by reaction with iron(II), was identified previously as the stable product of a reaction that, by inference, also yields a cyclohexyl radical. The activation of arteflene in vivo has been characterized with particular reference to enone formation. [14C]Arteflene (35 micromol/kg) was given i.v. to anesthetized and cannulated male rats: 42.2 +/- 7.0% (mean +/- S.D., n = 7) of the radiolabel was recovered in bile over 5 h. In the majority of rats, the principal biliary metabolites were 8-hydroxyarteflene glucuronide (14.2 +/- 3. 9% dose, 0-3 h) and the cis and trans isomers of the enone (13.5 +/- 4.6% dose, 0-3 h). In conscious rats, 15.3 +/- 1.6% (mean +/- S.D., n = 8) of the radiolabel was recovered in urine over 24 h. The principal urinary metabolite appeared to be a glycine conjugate of a derivative of the enone. Biliary excretion of the glucuronide, but not of the enones, was inhibited by ketoconazole. 8-Hydroxyarteflene was formed extensively by rat and human liver microsomes but no enone was found. Bioactivation is a major pathway of arteflene's metabolism in the rat. Although the mechanism of in vivo bioactivation is unclear, the reaction is not catalyzed by microsomal cytochrome P-450 enzymes.  (+info)

Artemether for severe malaria: a meta-analysis of randomized clinical trials. (7/1442)

The treatment of choice for severe malaria is quinine. However, a gradual progression of resistance to quinine has become a concern in parts of the world. Artemisinin-related compounds are a relatively new class of drugs. This meta-analysis assesses the evidence regarding the clinical effectiveness of artemether for severe malaria. Computerized literature searches identified all randomized clinical trials of artemether in comparison with quinine. Standardized data extraction was independently performed by both authors. Results of nine trials, entered in the meta-analysis, demonstrate the absence of a significant difference between artemether and quinine in terms of mortality rate (odds ratio [OR], 0.76; 95% confidence interval [CI], 0.50-1.14). Statistical pooling of data from trials in Southeast Asia showed a trend toward enhanced reduction of mortality (OR, 0.38; 95% CI, 0.14-1.02). These data demonstrate the equality of artemether and quinine for severe malaria and indicate a trend toward greater effectiveness of artemether in regions where there is recognized quinine resistance.  (+info)

Cost-effectiveness analysis of artesunate and quinine + tetracycline for the treatment of uncomplicated falciparum malaria in Chanthaburi, Thailand. (8/1442)

A randomized, controlled, malaria-clinic-based field trial was carried out to compare the cost-effectiveness of a 5-day 700-mg oral artesunate and a 7-day quinine + tetracycline regimen for the treatment of uncomplicated falciparum malaria in Thailand. Cost-effectiveness was determined from the providers' perspective and based on curative effectiveness. A total of 137 patients, aged 15-60 years, attending a malaria clinic were followed for 28 days, 60 of them received quinine + tetracycline and 77 received artesunate. Cure rates were assessed on day 5 (artesunate) and day 7 (quinine + tetracycline), using the intention-to-treat approach. Cost-effectiveness and sensitivity analyses were performed by varying the day 5/day 7 curative effectiveness and cost of artesunate. The cure rate with artesunate (100%) was significantly higher than with quinine + tetracycline (77.4%) (relative risk adjusted for sex (aRR) = 1.32, 95% confidence interval (CI) = 1.12-1.55; referent quinine + tetracycline). Artesunate was more cost-effective than quinine + tetracycline at the following costs: artesunate, < or = US$0.36 per 50-mg tablet; quinine, US$0.06 per 300-mg tablet; tetracycline, US$0.02 per 250-mg capsule; and services per case found, < or = US$11.49. Because of the higher cure rate and higher cost-effectiveness of the artesunate regimen compared with quinine + tetracycline, we recommend its use for the treatment of uncomplicated falciparum malaria in malaria clinics in Thailand.  (+info)

Artemisinins are a class of antimalarial drugs derived from the sweet wormwood plant (Artemisia annua). They are highly effective against Plasmodium falciparum, the most deadly species of malaria parasite. Artemisinins have become an essential component in the treatment of malaria and are often used in combination therapy regimens to reduce the risk of drug resistance.

The artemisinin compounds contain a unique peroxide bridge that is responsible for their antimalarial activity. They work by generating free radicals that can damage the parasite's membranes, leading to its rapid death. Artemisinins have a fast action and can significantly reduce the parasite biomass in the first few days of treatment.

Some commonly used artemisinin-based combination therapies (ACTs) include:

* Artemether-lumefantrine (Coartem)
* Artesunate-amodiaquine (Coarsucam)
* Artesunate-mefloquine (Artequin)
* Dihydroartemisinin-piperaquine (Eurartesim, Duo-Cotecxin)

Artemisinins have also shown potential in treating other conditions, such as certain types of cancer and viral infections. However, more research is needed to establish their safety and efficacy for these indications.

Antimalarials are a class of drugs that are used for the prevention, treatment, and elimination of malaria. They work by targeting the malaria parasite at various stages of its life cycle, particularly the erythrocytic stage when it infects red blood cells. Some commonly prescribed antimalarials include chloroquine, hydroxychloroquine, quinine, mefloquine, and artemisinin-based combinations. These drugs can be used alone or in combination with other antimalarial agents to increase their efficacy and prevent the development of drug resistance. Antimalarials are also being investigated for their potential use in treating other diseases, such as autoimmune disorders and cancer.

Parasitic sensitivity tests, also known as parasite drug susceptibility tests, refer to laboratory methods used to determine the effectiveness of specific antiparasitic medications against a particular parasitic infection. These tests help healthcare providers identify which drugs are most likely to be effective in treating an individual's infection and which ones should be avoided due to resistance or increased risk of side effects.

There are several types of parasitic sensitivity tests, including:

1. In vitro susceptibility testing: This involves culturing the parasite in a laboratory setting and exposing it to different concentrations of antiparasitic drugs. The growth or survival of the parasite is then observed and compared to a control group that was not exposed to the drug. This helps identify the minimum inhibitory concentration (MIC) of the drug, which is the lowest concentration required to prevent the growth of the parasite.
2. Molecular testing: This involves analyzing the genetic material of the parasite to detect specific mutations or gene variations that are associated with resistance to certain antiparasitic drugs. This type of testing can be performed using a variety of methods, including polymerase chain reaction (PCR) and DNA sequencing.
3. Phenotypic testing: This involves observing the effects of antiparasitic drugs on the growth or survival of the parasite in a laboratory setting. For example, a parasite may be grown in a culture medium and then exposed to different concentrations of a drug. The growth of the parasite is then monitored over time to determine the drug's effectiveness.

Parasitic sensitivity tests are important for guiding the treatment of many parasitic infections, including malaria, tuberculosis, and leishmaniasis. These tests can help healthcare providers choose the most effective antiparasitic drugs for their patients, reduce the risk of drug resistance, and improve treatment outcomes.

Sesquiterpenes are a class of terpenes that consist of three isoprene units, hence the name "sesqui-" meaning "one and a half" in Latin. They are composed of 15 carbon atoms and have a wide range of chemical structures and biological activities. Sesquiterpenes can be found in various plants, fungi, and insects, and they play important roles in the defense mechanisms of these organisms. Some sesquiterpenes are also used in traditional medicine and have been studied for their potential therapeutic benefits.

Drug resistance, also known as antimicrobial resistance, is the ability of a microorganism (such as bacteria, viruses, fungi, or parasites) to withstand the effects of a drug that was originally designed to inhibit or kill it. This occurs when the microorganism undergoes genetic changes that allow it to survive in the presence of the drug. As a result, the drug becomes less effective or even completely ineffective at treating infections caused by these resistant organisms.

Drug resistance can develop through various mechanisms, including mutations in the genes responsible for producing the target protein of the drug, alteration of the drug's target site, modification or destruction of the drug by enzymes produced by the microorganism, and active efflux of the drug from the cell.

The emergence and spread of drug-resistant microorganisms pose significant challenges in medical treatment, as they can lead to increased morbidity, mortality, and healthcare costs. The overuse and misuse of antimicrobial agents, as well as poor infection control practices, contribute to the development and dissemination of drug-resistant strains. To address this issue, it is crucial to promote prudent use of antimicrobials, enhance surveillance and monitoring of resistance patterns, invest in research and development of new antimicrobial agents, and strengthen infection prevention and control measures.

'Plasmodium falciparum' is a specific species of protozoan parasite that causes malaria in humans. It is transmitted through the bites of infected female Anopheles mosquitoes and has a complex life cycle involving both human and mosquito hosts.

In the human host, the parasites infect red blood cells, where they multiply and cause damage, leading to symptoms such as fever, chills, anemia, and in severe cases, organ failure and death. 'Plasmodium falciparum' malaria is often more severe and life-threatening than other forms of malaria caused by different Plasmodium species. It is a major public health concern, particularly in tropical and subtropical regions of the world where access to prevention, diagnosis, and treatment remains limited.

Malaria, Falciparum is defined as a severe and often fatal form of malaria caused by the parasite Plasmodium falciparum. It is transmitted to humans through the bites of infected Anopheles mosquitoes. This type of malaria is characterized by high fever, chills, headache, muscle and joint pain, and vomiting. If left untreated, it can cause severe anemia, kidney failure, seizures, coma, and even death. It is a major public health problem in many tropical and subtropical regions of the world, particularly in Africa.

Malaria is not a medical definition itself, but it is a disease caused by parasites that are transmitted to people through the bites of infected female Anopheles mosquitoes. Here's a simple definition:

Malaria: A mosquito-borne infectious disease caused by Plasmodium parasites, characterized by cycles of fever, chills, and anemia. It can be fatal if not promptly diagnosed and treated. The five Plasmodium species known to cause malaria in humans are P. falciparum, P. vivax, P. ovale, P. malariae, and P. knowlesi.

Inhibitory Concentration 50 (IC50) is a measure used in pharmacology, toxicology, and virology to describe the potency of a drug or chemical compound. It refers to the concentration needed to reduce the biological or biochemical activity of a given substance by half. Specifically, it is most commonly used in reference to the inhibition of an enzyme or receptor.

In the context of infectious diseases, IC50 values are often used to compare the effectiveness of antiviral drugs against a particular virus. A lower IC50 value indicates that less of the drug is needed to achieve the desired effect, suggesting greater potency and potentially fewer side effects. Conversely, a higher IC50 value suggests that more of the drug is required to achieve the same effect, indicating lower potency.

It's important to note that IC50 values can vary depending on the specific assay or experimental conditions used, so they should be interpreted with caution and in conjunction with other measures of drug efficacy.

Chloroquine is an antimalarial and autoimmune disease drug. It works by increasing the pH or making the environment less acidic in the digestive vacuoles of malaria parasites, which inhibits the polymerization of heme and the formation of hemozoin. This results in the accumulation of toxic levels of heme that are harmful to the parasite. Chloroquine is also used as an anti-inflammatory agent in the treatment of rheumatoid arthritis, discoid or systemic lupus erythematosus, and photodermatitis.

The chemical name for chloroquine is 7-chloro-4-(4-diethylamino-1-methylbutylamino)quinoline, and it has a molecular formula of C18H26ClN3. It is available in the form of phosphate or sulfate salts for oral administration as tablets or solution.

Chloroquine was first synthesized in 1934 by Bayer scientists, and it has been widely used since the 1940s as a safe and effective antimalarial drug. However, the emergence of chloroquine-resistant strains of malaria parasites has limited its use in some areas. Chloroquine is also being investigated for its potential therapeutic effects on various viral infections, including COVID-19.

Combination drug therapy is a treatment approach that involves the use of multiple medications with different mechanisms of action to achieve better therapeutic outcomes. This approach is often used in the management of complex medical conditions such as cancer, HIV/AIDS, and cardiovascular diseases. The goal of combination drug therapy is to improve efficacy, reduce the risk of drug resistance, decrease the likelihood of adverse effects, and enhance the overall quality of life for patients.

In combining drugs, healthcare providers aim to target various pathways involved in the disease process, which may help to:

1. Increase the effectiveness of treatment by attacking the disease from multiple angles.
2. Decrease the dosage of individual medications, reducing the risk and severity of side effects.
3. Slow down or prevent the development of drug resistance, a common problem in chronic diseases like HIV/AIDS and cancer.
4. Improve patient compliance by simplifying dosing schedules and reducing pill burden.

Examples of combination drug therapy include:

1. Antiretroviral therapy (ART) for HIV treatment, which typically involves three or more drugs from different classes to suppress viral replication and prevent the development of drug resistance.
2. Chemotherapy regimens for cancer treatment, where multiple cytotoxic agents are used to target various stages of the cell cycle and reduce the likelihood of tumor cells developing resistance.
3. Cardiovascular disease management, which may involve combining medications such as angiotensin-converting enzyme (ACE) inhibitors, beta-blockers, diuretics, and statins to control blood pressure, heart rate, fluid balance, and cholesterol levels.
4. Treatment of tuberculosis, which often involves a combination of several antibiotics to target different aspects of the bacterial life cycle and prevent the development of drug-resistant strains.

When prescribing combination drug therapy, healthcare providers must carefully consider factors such as potential drug interactions, dosing schedules, adverse effects, and contraindications to ensure safe and effective treatment. Regular monitoring of patients is essential to assess treatment response, manage side effects, and adjust the treatment plan as needed.

Artemisinins can be used alone, but this leads to a high rate of return of parasites and other drugs are required to clear the ... Artemisinins are not used for malaria prevention because of the extremely short activity (half-life) of the drug. To be ... Artemisinins are generally well tolerated at the doses used to treat malaria. The side effects from the artemisinin class of ... Artemisinins were later found to possess a broad spectrum of activity against a wide range of trematodes, including Schistosoma ...
"Rectal artemisinins rapidly eliminate malarial parasites". EurekAlert!. 2008-03-27. Archived from the original on 3 April 2008 ...
Pacios-Michelena, Anabel; Kasaragod, Vikram Babu; Schindelin, Hermann (2021). "Artemisinins and their impact on inhibitory ... "Elucidating the Molecular Basis for Inhibitory Neurotransmission Regulation by Artemisinins". Neuron. Cell Press. 101 (4): 673- ...
August 2003). "Artemisinins target the SERCA of Plasmodium falciparum". Nature. 424 (6951): 957-961. Bibcode:2003Natur.424.. ...
The consensus is that PfATP6 is a validated target for artemisinins and mammalian SERCA3, in neutrophils, has emerged as a ... August 2003). "Artemisinins target the SERCA of Plasmodium falciparum". Nature. 424 (6951): 957-961. Bibcode:2003Natur.424.. ... Evidence came from a Xenopus oocyte system describing specific interactions between artemisinins and PfATP6 as well as E255L- ... In 2022 it was observed in murine neutrophils that artemisinins were inhibiting migration of these cells. Further investigation ...
Dellicour S, Hall S, Chandramohan D, Greenwood B (February 2007). "The safety of artemisinins during pregnancy: a pressing ... Artemether is an artemisinin derivative and the mechanism of action for artemisinins is.[medical citation needed] Artemether ...
Keiser, J.; Utzinger, J. R. (2007). "Artemisinins and synthetic trioxolanes in the treatment of helminth infections". Current ...
Keiser J, Utzinger J (December 2007). "Artemisinins and synthetic trioxolanes in the treatment of helminth infections". Current ...
The cost of artemisinins limits their use in the developing world. Malaria strains found on the Cambodia-Thailand border are ... Resistance is now common against all classes of antimalarial drugs apart from artemisinins. Treatment of resistant strains ... Artemisinins, discovered by Chinese scientist Tu Youyou and colleagues in the 1970s from the plant Artemisia annua, became the ... to artemisinin monotherapies in subtherapeutic doses for over 30 years and the availability of substandard artemisinins likely ...
They recommend that it be used only when artemisinins are not available. Quinine is also used to treat lupus and arthritis. ...
Artemisinins are sesquiterpene lactones isolated from Artemisia annua, a Chinese traditional medicine. These suppositories are ...
Artesunate is in the class of medications known as artemisinins, which are derivatives from sweet wormwood (Artemisia annua). ... His team, however, demonstrated resistance of Plasmodium falciparum to artemisinins in Western Cambodia. New treatments would ...
The best recognised adverse effect of the artemisinins is that they lower reticulocyte counts. This is not usually of clinical ... It is in the class of medications known as artemisinins, which are derivatives from "qinghao," or sweet wormwood plant ( ... Clark RL (February 2012). "Effects of artemisinins on reticulocyte count and relationship to possible embryotoxicity in ...
The artemisinins became the most potent as well as the safest and most rapidly acting antimalarial drugs, recommended by the ... Weina, PJ (2008). "Artemisinins from folklore to modern medicine--transforming an herbal extract to life-saving drugs". ... For their high efficacy, safety and stability, artemisinins such as artemether and artesunate became the drugs of choice in ... All clinical trials by this time confirmed that artemisinins are more effective than the conventional antimalarial drugs, such ...
Artemisinins and derivatives are proving to be candidates as drugs of choice for trematodiasis. In regions where helminthiasis ...
... evaluation to determine and predict the neurotoxicity of artemisinins". Toxicology. 279 (1-3): 1-9. doi:10.1016/j.tox.2010.09. ...
ISBN 978-7-5046-6996-4. Tu, Y. (2017). From Artemisia annua L. to Artemisinins: The Discovery and Development of Artemisinins ...
The project resulted in the discovery of artemisinins, a class of antimalarial drugs, from the medicinal plant Artemisia annua ...
4-trioxane ring are important potential improvements over the naturally derived artemisinins. The peroxide group in the 1,2,4- ...
... including chloroquine and artemisinins, were used to resist the scourge. Today, artemisinin is present in every remedy applied ...
... traditional Chinese medicine discovered and led to the development of a class of new antimalarial drugs called artemisinins. ...
... artemisinins MeSH D02.455.849.765.424 - farnesol MeSH D02.455.849.765.444 - gossypol MeSH D02.455.849.765.750 - santonin MeSH ... artemisinins MeSH D02.389.338.450 - lipid peroxides MeSH D02.389.338.825 - tert-butylhydroperoxide MeSH D02.389.338.912 - ...
In this study, the antiplasmodial activity of SC83288 against artemisinins was profiled in order to assess its potential to ... The results obtained in this study are consistent with artemisinins and SC83288 having distinct modes of action and different ... Based on growth inhibition and ring survival assays, no cross-resistance was observed between artemisinins and SC83288, using ... supports efforts to continue the clinical development of SC83288 against severe malaria as an alternative to artemisinins in ...
Text; Format: print Publication details: Geneva : World Health Organization, 2007Other title: Use of rectal artemisinin-based suppositories in the management of severe malaria.Title translated: Suppositoires à base dαartemisinine : utilisation des suppositoires à base dartémisinine dans la prise en charge du paludisme grave : rapport dune consultation informelle de lOMS..Online access: Click here to access online Availability: Items available for loan: WHO HQ (1)Call number: WC 770 2007AR. ...
Artemisinins can be used alone, but this leads to a high rate of return of parasites and other drugs are required to clear the ... Artemisinins are not used for malaria prevention because of the extremely short activity (half-life) of the drug. To be ... Artemisinins are generally well tolerated at the doses used to treat malaria. The side effects from the artemisinin class of ... Artemisinins were later found to possess a broad spectrum of activity against a wide range of trematodes, including Schistosoma ...
Artemisinins: A class of drugs used for the treatment (not prevention) of malaria usually as a part of a combination therapy, ...
Artemisinins are the cornerstone of anti-malarial drugs1. Emergence and spread of resistance to them2,3,4 raises risk of wiping ... The emergence of artemisinin resistance is a major threat to world-wide malaria treatment and control and although artemisinins ... Here Kasturi Haldar and colleagues show that artemisinins target the parasite phosphatidylinositol-3-kinase (PfPI3K) to inhibit ... Here we provide biochemical and cellular evidence that artemisinins are potent inhibitors of Plasmodium falciparum ...
Plasmodium falciparum: multifaceted resistance to artemisinins. Malar J. 2016;15:149. DOIPubMedGoogle Scholar ... Ring-stage survival assays (RSA) to evaluate the in-vitro and ex-vivo susceptibility of Plasmodium falciparum to artemisinins [ ...
Berkeley Electronic Press Selected Works
Artemisinins target the SERCA of Plasmodium falciparum. Nature 2003, 424, 957-961. [Google Scholar] [CrossRef] [PubMed] ...
01/01/2013 - "Two malaria drug classes, the 8- aminoquinolines and the artemisinins interact with cytochrome P450s and host ...
recently reported that artemisinins might also help reduce the risk of neurologic complications that are encountered in COVID- ... 2020). Anti-SARS-CoV-2 potential of artemisinins in vitro. ACS Infect Dis. 6 (9), 2524-2531. doi:10.1021/acsinfecdis.0c00522 ... 2014). Postartesunate delayed hemolysis is a predictable event related to the lifesaving effect of artemisinins. Blood 124 (2 ... when these artemisinins were added at clinically achievable micromolar concentrations throughout the infection process or post- ...
Artemether is an artemisinin derivative, and artemisinins is the mode of action. Artemether reacts with ferriprotoporphyrin IX ...
Artemisinins are key anti-malarial drugs, but artemisinin resistance has been increasing; this study identifies the molecular ... target of artemisinins as phosphatidylinositol-3-kinase and increase of the lipid product phosphatidylinositol-3-phosphate ...
Designing Artemisinins with Antimalarial Potential, Combining Molecular Electrostatic Potential, Ligand-Heme Interaction and ...
Fortunately, artemisinins, used as herbal remedies in China for 2,000 years, look promising. Clinical trials were delayed, ...
Antimalarials, Artemisinins, Drug Combinations, Fluorenes, Malaria, Falciparum, Randomized Controlled Trials Unit-dose packaged ... Malaria, Falciparum/drug therapy, Antimalarials/administration & dosage, Artemisinins/administration & dosage, Fluorenes/ ...
Artemether and other artemisinins are associated with maternal toxicity and embryotoxicity and malformations in animals at ...
SESQUITERPENES cyclized into two adjoining cyclohexane rings but with a different configuration from the ARTEMISININS. ...
This is a "connection" page, showing publications Kathryn Colborn has written about Artemisinins. ...
Haemoglobin degradation underpins the sensitivity of early ring stage Plasmodium falciparum to artemisinins. J Cell Sci 2016, ...
Because resistance to artemisinins and piperaquine is increasing in southeast Asia and the… 12/11/2018 In Uganda, artemether- ... Because resistance to artemisinins and piperaquine is increasing in southeast Asia and the prevalence of Plasmodium falciparum ...
Ring-stage Survival Assays (RSA) to Evaluate the In-Vitro and Ex-Vivo Susceptibility of Plasmodium Falciparum to Artemisinins. ... Ring-stage Survival Assays (RSA) to Evaluate the In-Vitro and Ex-Vivo Susceptibility of Plasmodium Falciparum to Artemisinins. ... Evaluting Plasmodium falciparum susceptibility to artemisinins in laboratory strains and fresh isolates ...
Li et al (2017) Artemisinins Target GABAA Receptor Signaling and Impair α Cell Identity. Cell 168 86 PMID: 27916275 ...
Thus, although artemisinins at a dollar or two per course are both inexpensive by U.S. or European standards and highly cost- ... If resistance to artemisinins is allowed to develop and spread before replacement drugs are at hand, malarias toll could rise ... THE ECONOMICS OF ARTEMISININS AND ACTs. By Western standards, artemisinin derivatives are already inexpensive. They also are ... The artemisinins are the only first-line antimalarial drugs appropriate for widespread use that still work against all ...
It is imperative that we act promptly to detect and stem the tide of resistance to artemisinins and ACT partner drugs in Africa ... The emergence of Plasmodium falciparum parasites with delayed clearance after treatment with artemisinins (artemisinin ... 4 Although resistance to artemisinins and partner drugs poses a significant threat to the efficacy of first-line ACTs, its ... as new antimalarial combination regimens that do not rely on artemisinins are not expected to be generally available within the ...
In East Africa, malaria parasites have become resistant to artemisinins, the backbone of current treatment regimens. This ...
In particular, I felt herbal medicine and "ethnopharmacology" had something to offer, see e.g. the discovery of artemisinins ...
  • If resistance to artemisinins is allowed to develop and spread before replacement drugs are at hand, malaria's toll could rise even higher. (nationalacademies.org)
  • The recent emergence of resistance to artemisinins and partner drugs in P. falciparum has raised both regional and global concerns, and elimination efforts are invariably prioritized against this parasite to avert spread. (intechopen.com)
  • The key challenges in the region's fight against malaria emerging resistance to artemisinins, which are central to the efficacy of antimalarial treatment with artemisinin‐based combination therapies. (asiasentinel.com)
  • Evolution of Partial Resistance to Artemisinins in Malaria Parasites in Uganda. (cdc.gov)
  • Here we provide biochemical and cellular evidence that artemisinins are potent inhibitors of Plasmodium falciparum phosphatidylinositol-3-kinase (PfPI3K), revealing an unexpected mechanism of action. (nature.com)
  • The artemisinins are the only first-line antimalarial drugs appropriate for widespread use that still work against all chloroquine-resistant malaria parasites. (nationalacademies.org)
  • In East Africa, malaria parasites have become resistant to artemisinins, the backbone of current treatment regimens. (scitechdaily.com)
  • Artemisinins are the cornerstone of anti-malarial drugs 1 . (nature.com)
  • The central recommendation of this report- a sustained global subsidy of artemisinins coformulated with other antimalarial drugs - is the most economically and biomedically sound means to meet this challenge. (nationalacademies.org)
  • In order to preserve the efficacy of artemisinins as an essential component of life-saving ACTs, WHO has called for a ban on the use of oral artemisinin monotherapies, at various levels, including manufacturers, international drug suppliers, national health authorities and international aid and funding agencies involved in the funding of essential antimalarial medicines. (allcountries.org)
  • The investigators showed that a class of antimalarial drugs known as artemisinins, typified by the FDA-approved drug artemether , were capable of inhibiting ARX levels, reducing glucagon, and increasing insulin in an in vitro alpha-cell model. (medscape.com)
  • Based on growth inhibition and ring survival assays, no cross-resistance was observed between artemisinins and SC83288, using parasite lines that were resistant to either one of these drugs. (biomedcentral.com)
  • Partnered with other drugs as artemisinin-based combination therapy (ACT), artemisinins have formed the backbone of malaria treatment and control since 2006 [ 2 ]. (biomedcentral.com)
  • If falciparum malaria sufferers had the same broad access to artemisinins that currently exists for chloroquine, the rising burden of malaria in the world today would halt or reverse. (nationalacademies.org)
  • There are currently no effective alternatives to artemisinins for the treatment of P. falciparum malaria either on the market or towards the end of the development pipeline. (allcountries.org)
  • In this review, we aim to provide a comprehensive update of the current knowledge of the effects of artemisinins in relation to respiratory diseases to identify gaps that need to be filled in the course of repurposing artemisinins for the treatment of respiratory diseases. (nus.edu.sg)
  • In addition, we postulate whether artemisinins can also be repurposed for the treatment of COVID-19 given its anti-viral and anti-inflammatory properties. (nus.edu.sg)
  • The challenge, therefore, is twofold: to facilitate widespread use of artemisinins while, at the same time, to preserve their effectiveness for as long as possible. (nationalacademies.org)
  • Progressively, research has found that artemisinins displayed multiple pharmacological actions against inflammation, viral infections, and cell and tumour proliferation, making it effective against diseases. (nus.edu.sg)
  • Chief among these new treatments are the "artemisinins," paradoxically both an ancient and a modern class of drug that can still cure any form of human malaria. (nationalacademies.org)
  • In this study, the antiplasmodial activity of SC83288 against artemisinins was profiled in order to assess its potential to replace, or be combined with, artemisinin derivatives. (biomedcentral.com)
  • The last new class of antimalarials-artemisinins-came into wide use more than a decade ago. (nih.gov)
  • The efficacy and safety of artemisinins and their derivatives in oral, rectal, and intramuscular dosage forms have been widely studied ( 5 - 11 ). (cdc.gov)
  • WHO and its Evidence Review Group ( ERG ) on malaria in pregnancy recommended to review its malaria policy for treatment of pregnant women as a result of a meta-analysis on the safety of artemisinins in the first trimester of pregnancy. (lstmed.ac.uk)
  • Beginning in 2008, however, studies in Southeast Asia identified poor results from artemisinins and eventually from artemisinin-based combination malaria treatments. (nih.gov)
  • Artemisinins in malaria treatment in the UK. (nih.gov)
  • Scientists soon found the primary reason - a protein (PfK13) in P. falciparum had developed mutations that made it partially resistant to artemisinins. (nih.gov)
  • SESQUITERPENES cyclized into two adjoining cyclohexane rings but with a different configuration from the ARTEMISININS. (ouhsc.edu)
  • Artemisinins with improved pharmacokinetic properties may offer therapeutic benefit in combination with conventional therapeutic strategies in AML. (nih.gov)
  • The pharmacology of artemisinins is problematic and should be considered in designing AML treatment strategies with currently available agents. (nih.gov)
  • Investigate antileukemic activity of artemisinins, artesunate (ART), and dihydroartemisinin (DHA), in combination with cytarabine, a key component of acute myeloid leukemia (AML) chemotherapy using in vitro and in vivo models. (nih.gov)
  • The current artemisinins have been in use since the late 1970s and have relatively poor thermal, chemical and metabolic stabilities - all are metabolized or hydrolyzed in vivo to dihydroartemisinin (DHA) that itself undergoes facile decomposition in vivo. (eurekaselect.com)
  • As artemisinins induce the most rapid reduction in parasitaemia of any drug, common sense dictates that any new artemisinin derivative, selected on the bases of more robust chemical and thermal stability, metabolic stability with respect to the generation of DHA in vivo , and relatively benign neurotoxicity should be used in any new ACT whose components are rationally chosen in order to counter resistant malaria and inhibit transmission. (eurekaselect.com)
  • Discover new partner drugs for combination with artemisinins to treat malaria. (nih.gov)
  • The current artemisinins possess neurotoxicity as demonstrated in animal models, an issue that mandates increased vigilance in view of trends to use of protracted treatment regimens involving sequential administration of different ACTs against the resistant disease. (eurekaselect.com)
  • In the food vacuole, haemozoin synthesis, corresponding to detoxification of the waste from haemoglobin by the parasite, is specially affected by quinolines [ 6 ] and artemisinins. (biomedcentral.com)
  • Artemisinins are not used for malaria prevention because of the extremely short activity (half-life) of the drug. (wikipedia.org)
  • Nanomal lead Professor Sanjeev Krishna, from St George's, said: "Recent research suggests there's a real danger that artemisinins could eventually become obsolete, in the same way as other anti-malarials. (medgadget.com)