AnatomyOrganismsDiseasesChemicals and DrugsAnalytical, Diagnostic and Therapeutic Techniques and EquipmentPhenomena and ProcessesDisciplines and OccupationsInformation ScienceHealth CareGeographicals
ChloroquineAntimalarialsDrug ResistancePlasmodium falciparumParasitic Sensitivity TestsProtozoan ProteinsMalaria, FalciparumMembrane Transport ProteinsMefloquineArtemisininsQuinineMalariaAmodiaquinePyrimethamineSulfadoxineDNA, ProtozoanDrug CombinationsDrug Resistance, MultipleSesquiterpenesDrug Resistance, BacterialFluorenesInhibitory Concentration 50Drug Resistance, MicrobialParasitemiaGenes, ProtozoanPlasmodiumSenegalPlasmodium vivaxMalaria, VivaxQuinolinesPlasmodium bergheiAnti-Bacterial AgentsIndonesiaMutationDrug Resistance, NeoplasmMultidrug Resistance-Associated ProteinsGuyanaDihydropteroate SynthasePromethazineMicrobial Sensitivity TestsTetrahydrofolate DehydrogenaseATP-Binding Cassette TransportersGenes, MDRPrimaquinePapua New GuineaPolymerase Chain ReactionMembrane ProteinsCameroonProguanilVerapamilDrug Resistance, Multiple, BacterialPhenanthrenesGenotypePlasmodium cynomolgiThailandDisease ResistanceErythrocytesPoint MutationTanzaniaPolymorphism, GeneticPacific IslandsP-GlycoproteinMolecular Sequence DataTetraoxanesSequence Analysis, DNAPolymorphism, Restriction Fragment LengthSelf MedicationHaplotypesEthanolaminesDrug Resistance, FungalHydroxychloroquineInsecticide ResistanceTrophozoitesPhenotypeAllelesAtovaquoneBacterial ProteinsDrug Therapy, CombinationDrug Resistance, ViralFolic Acid AntagonistsMacrolidesbeta-Lactam ResistanceMutation, MissenseBlackwater FeverVascular ResistanceDapsonebeta-LactamasesPlant DiseasesSpiro CompoundsHemeproteinsAminoquinolinesNaphthyridinesInsecticidesPeroxidesTetracycline ResistanceDrug Evaluation, PreclinicalDosage FormsAmino Acid SequencePyrethrinsNigeria
PlasmodiumFalciparumHydroxychloroquineParasitesCompoundsVivoMutationsPhosphateDrugs including cTransporterArtemisinin resistanceAntiplasmodialPyrimethaminePfCRTDrugWidespreadWidelyParasite resistanceAtovaquoneAntimicrobialHemeEfficacyAnticancerInfectionStrainsDigestive vacuoleMutationUnclearPotencyChemicallyPiperaquineCandidates1980sEffectiveArtemisininsRheumatoid arthritisSyntheticTreat malariaAntiviralExperimentsActionTreatmentToxicParasitemiaTherapeuticAfricaActivityClinicalLupus
Plasmodium24
Falciparum14
  • It has been found that certain strains of P. falciparum have become resistant to 4-aminoquinoline compounds (including chloroquine and hydroxychloroquine). (drugs.com)
  • During the 1980s, a similar scenario was observed with sulfadoxine-pyrimethamine (SP) when this association was recommended to replace chloroquine as first-line treatment in uncomplicated falciparum malaria ( 5 , 6 ). (cdc.gov)
  • CONCLUSIONS We were able to easily obtain a collection of heterocyclic compounds with in vitro anti-P. falciparum activity that can be used as scaffolds for the design and development of new antiplasmodial drugs. (scielo.br)
  • SC83288 is fast-acting and able to clear P. falciparum parasites at low nanomolar concentrations in vitro, as well as in a humanized SCID mouse model system in vivo. (biomedcentral.com)
  • SC83288, an amicarbalide derivative, is active against P. falciparum blood stages at low nanomolar concentrations in vitro, with IC 50 values of 3 nM. (biomedcentral.com)
  • In vitro resistance to SC83288 develops slowly and might involve mutational changes in the Ca 2+ transporting PfATP6, the P. falciparum SERCA orthologue. (biomedcentral.com)
  • The most active compounds were further screened in vitro against the chloroquine resistant strain P. falciparum, (RKL9) and showed IC50 value range of 0.0198-0.096 µM, compared to IC50 value of 0.19420 µM for chloroquine sulphate. (bvsalud.org)
  • The antiplasmodial activity was tested in vitro against chloroquine-resistant P. falciparum at 100 μg/ml for 72 h. (phcog.com)
  • P. falciparum is a resistant strains of chloroquine. (vedantu.com)
  • P. falciparum codes the pump by the chloroquine resistance transporter (PfCRT) gene. (vedantu.com)
  • In vivo antiplasmodial studies with P. falciparum infected mice showed an effect of 4,7-dichloroquinoline compared to chloroquine. (nature.com)
  • PfATP6 and Artemisinin Resistance in P. falciparum FIG 1 Development of transgenic lines in 3D7 with the PfATP6 S769N mutation. (2medicalcare.com)
  • 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)
  • Chloroquine and related drugs gametocidal (for species except for P falciparum ) and schizonticidal (for parasites in blood but not tissue). (medscape.com)
Hydroxychloroquine6
  • For instance, a study in France published on March 20 in the International Journal of Antimicrobial Agents described the treatment of 42 patients hospitalized with COVID-19, 26 of whom received a version of chloroquine called hydroxychloroquine and 16 of whom received routine care. (the-scientist.com)
  • Hydroxychloroquine is now the most commonly prescribed antimalarial for treatment of autoimmune disease. (ccjm.org)
  • The primary mechanism by which hydroxychloroquine modulates systemic lupus erythematosus is by suppressing activation of Toll-like receptors, which exist on the surface of endosomes and play a significant role in the innate immune response and in autoimmune disease. (ccjm.org)
  • Antimalarial drugs such as hydroxychloroquine prevent Toll-like receptor activation by binding directly to nucleic acids in the activation pathway. (ccjm.org)
  • Chloroquine and hydroxychloroquine are closely related to each other. (vedantu.com)
  • Among several drug candidates, chloroquine (CQN) and hydroxychloroquine (H-CQN) were tested intensively, and any contentious therapeutic effect of both has been discussed controversially in the light of severe side effects and missing efficacy. (mdpi.com)
Parasites21
  • The most active in vitro compounds were evaluated against P. berghei parasites in mice. (scielo.br)
  • The epicenter of piperaquine resistance appears to be western Cambodia where in 2014 over 40% of dihydroartemisinin-piperaquine treatments failed to eliminate parasites from the patient's blood. (wikipedia.org)
  • The mechanism by which parasites become resistant to piperaquine remains unclear. (wikipedia.org)
  • however, parasites that are resistant to chloroquine remain sensitive to piperaquine. (wikipedia.org)
  • The resistant parasites use its transmembrane pump to remove chloroquine from the digestive vacuole. (vedantu.com)
  • These chloroquine-resistant parasites pump out 40 times more than the chloroquine-sensitive parasites. (vedantu.com)
  • A Ca²⁺ channel blocker Verapamil has found to restore the ability of chloroquine to treat resistance parasites. (vedantu.com)
  • A major problem in the global fight against malaria is the widespread resistance of the parasites against the currently available drugs. (gla.ac.uk)
  • Previous studies have shown that depletion of GSH has an antimalarial effect, but it remained unclear whether parasites were killed directly or died because their host cell could not survive the depletion of GSH. (gla.ac.uk)
  • The findings of this study suggest that in parasites bearing mutant PfCRT, GSH is transported into the digestive vacuole where it is able to contribute to resistance by degrading heme, before the tripeptide itself is degraded by peptidases inside the vacuole, consistent with the overall reduction of GSH levels in CQ resistant parasites. (gla.ac.uk)
  • however, ART resistance is due to other genetic factors in some resistant parasites that do not contain k13 mutations [ 6 , 7 ]. (biorxiv.org)
  • A genome-wide association study identified variants in the ferredoxin fd ), apicoplast ribosomal protein S10 ( arps10 ), multidrug resistance protein 2 ( mdr2 ), and chloroquine resistance transporter ( crt ) genes as additional factors contributing to ART resistance, in which a missense fd mutation fd -D193Y) was the most frequent variant among resistant parasites [ 8 ]. (biorxiv.org)
  • As WHO has been gathering over, none of these candidate genes appears to be responsible for resources for eliminating and containing ART-resistant parasites the observed ART resistance in western Cambodia surveillance efforts have intensified in the GMS, where ART The proposal of PfATP6 as the primary target of ARTs in ma- use has the longest history. (2medicalcare.com)
  • Meanwhile, research aimed to deci- laria parasites was initially based on the structural resemblance of pher the underlying mechanisms of ART resistance has become a ARTs to thapsigargin, a specific inhibitor of mammalian SERCAs. (2medicalcare.com)
  • Here, we define the conditions under which P. cynomolgi can be adapted to long term in vitro culture to yield parasites that share many of the morphological and phenotypic features of P. vivax . (nature.com)
  • We show that the in vitro-cultured P. cynomolgi (from ex vivo or cryopreserved stocks) retain the key characteristics that these parasites share with P. vivax . (nature.com)
  • We further demonstrate that these parasites are suitable for high-throughput screening for antimalarial compounds. (nature.com)
  • However, due to the long-term large-scale use of chloroquine, some malaria parasites have developed drug resistance. (medicaltrend.org)
  • The spread of drug resistance may depend on the transmission of drug-resistant parasites by the mosquito. (biomedcentral.com)
  • Some studies have shown an association between the spread of drug resistance and levels of transmission of drug-resistant parasites by the mosquito. (biomedcentral.com)
  • In contrast, parasites resistant to the antimalarial atovaquone fail to transmit by mosquitoes, and the lack of transmission suggests that resistance will be unable to spread in the field, greatly enhancing the utility of atovaquone in malaria control [ 3 ]. (biomedcentral.com)
Compounds6
  • Heterocyclic compounds, such as dihydropyrimidinones (DHPM), synthesised via the Biginelli multicomponent reaction, as well as bicyclic compounds synthesised from DHPMs, have emerged as potential antimalarial candidates in the last few years. (scielo.br)
  • Additionally, we performed an in silico target fishing approach with the most active compounds, aiming to shed some light into the mechanism at a molecular level. (scielo.br)
  • Particularly, efforts should be devoted to developing fast-acting anti-malarial compounds in case clinical resistance increases to the first-line artemisinin-based combination therapy. (biomedcentral.com)
  • Their antifolate mechanism was confirmed via the ability of folic and folinic acids to reverse the antileishmanial activity of these compounds, comparably to Lm-PTR1 inhibitor trimethoprim. (bvsalud.org)
  • Aggressive research efforts to develop an alternative led to field testing of one of its derivative compounds, chloroquine, by the US Army in 1943. (ccjm.org)
  • All these compounds were found more potent than chloroquine and clotrimazole, the standard drugs. (biomedcentral.com)
Vivo3
  • The next steps for developing the use of this therapeutic combination in the treatment of gallbladder cancer will be a pre-clinical trial using animal models of gallbladder carcinoma in order to test the efficacy and efficiency of chloroquine and 5-FU in-vivo. (biomedcentral.com)
  • The claims of potential antimalarial activity of Cannabis sativa in vivo have not been well established nor the consequences defined. (thctotalhealthcare.com)
  • GIST cells were treated with IR700-12A8 and NIR light in vitro and vivo, and cell viability, histology and apoptosis were evaluated. (thno.org)
Mutations9
  • CQ resistance is associated with mutations in the CQ resistance transporter (PfCRT), a membrane protein of the digestive vacuole that allows the efflux of the drug form its site of action. (gla.ac.uk)
  • nonetheless, mutations of Fd gene ( fd ) may modulate ART resistance and Fd would be an important target for antimalarial drugs. (biorxiv.org)
  • Drug resistance is a major problem in the treatment of malaria, and Ernesto Freire's laboratory is working on the development of new strategies in which drug molecules are conferred with adaptive properties that allow them to maintain efficacy in the face of naturally existing polymorphisms and mutations associated with drug resistance. (child-survival.org)
  • Antimicrobial resistance occurs through different mechanisms, which include spontaneous (natural) genetic mutations and horizontal transfer of resistant genes through deoxyribonucleic acid (DNA). (who.int)
  • Resistance-conferring reversion mutations may lead to neoantigen generation, presenting immunotherapy targets. (aacrjournals.org)
  • PARP inhibitors and platinum-based drugs are approved to treat breast and ovarian cancers with defects in homologous recombination machinery (e.g., due to mutations in BRCA1 / 2 , RAD51C / D , or PALB2 ), but the development of resistance is common. (aacrjournals.org)
  • paper shows, effective resistance requires several mutations. (blogspot.com)
  • We'll only deal with two mutations even though we know that more are required for effective chloroquine resistance. (blogspot.com)
  • What I am going to do is try and get an estimate of the probability of creating a two-mutation chloroquine resistant strain in a single individual via a two-sequential mutations pathway. (blogspot.com)
Phosphate4
Drugs including c1
  • Seidah is currently experimenting with drugs including chloroquine as potential SARS-CoV-2 treatments and using material sent to him by pharmaceutical firms. (the-scientist.com)
Transporter2
  • Although Aotus and Saimiri monkey models have provided useful information about P. vivax biology, most of the data have been gained through comparative studies investigating polymorphisms in orthologous genes encoding resistance to pyrimethamine ( dhfr gene), sulfadoxine ( dhps gene), or chloroquine ( chloroquine resistant transporter or mdr-1 genes). (cdc.gov)
  • In contrast, amplification of the gene for the parasite transporter PfMDR1, a mechanism of parasite resistance to mefloquine, is inversely correlated with piperaquine resistance. (wikipedia.org)
Artemisinin resistance2
  • This study further supports efforts to continue the clinical development of SC83288 against severe malaria as an alternative to artemisinins in areas critically affected by artemisinin-resistance. (biomedcentral.com)
  • Driven by increasing political commitment, motivated by recent achievements in malaria control, and urged by the imminent threat of emerging artemisinin resistance, the GMS countries have endorsed a regional malaria elimination plan with a goal of eliminating malaria by 2030. (intechopen.com)
Antiplasmodial3
  • In this study, we attempted to uncover the antiplasmodial properties of Garcinia celebica , an Indonesian medicinal plant, along with the responsible compound and its possible mechanism. (phcog.com)
  • In vitro antiplasmodial IC 50 value of the most potent compound 5d was found to be 4.40 nM which is even less than all the three reference drugs chloroquine (18.7 nM), pyrimethamine (11 nM) and artimisinin (6 nM). (biomedcentral.com)
  • Therefore here in this study, we have decided to construct the molecular hybrids based on 1,4-DHP and pyrazole moieties using acyl hydrazone linkage which may possibly circumvent the antiplasmodial drug resistance (Fig. 1 ). (biomedcentral.com)
Pyrimethamine4
  • It also reviews the way drug resistance develops and spreads, methods used to assess the presence and level of drug resistance, and the extent to which chloroquine and sulfadoxine/pyrimethamine (SP)-the two most widely used antimalarial drugs in the world today-have now lost efficacy. (nationalacademies.org)
  • Resistance to sulfadoxine-pyrimethamine has also been detected. (who.int)
  • Drug resistance to first-line antimalarial drugs (e.g. chloroquine, sulfadoxine-pyrimethamine and artemisinin) is a major constrain in malaria control. (unl.pt)
  • Mechanism of action for pyrimethamine same as that of proguanil (ie, inhibits dihydrofolate reductase). (medscape.com)
PfCRT1
  • From the sequence and laboratory evidence it's utterly parsimonious and consistent with all the data-especially including the extreme rarity of the origin of chloroquine resistance-to think that a first, required mutation to PfCRT is strongly deleterious while the second may partially rescue the normal, required function of the protein, plus confer low chloroquine transport activity. (blogspot.com)
Drug34
  • ARALEN is an antimalarial and amebicidal drug. (drugs.com)
  • Slightly more than half of the urinary drug products can be accounted for as unchanged chloroquine. (drugs.com)
  • Our understanding of the molecular mechanisms of antimalarial drug resistance developed by P. vivax is less comprehensive. (cdc.gov)
  • O n March 16, SpaceX founder Elon Musk tweeted that the anti-malaria drug chloroquine was "maybe worth considering" as a treatment for COVID-19. (the-scientist.com)
  • The drug has a long track record in medicine, having been used since the 1940s as an antimalarial. (the-scientist.com)
  • If chloroquine is shown to be effective against SARS-CoV-2, it will not be via the same mechanism by which the drug functions as an antimalarial. (the-scientist.com)
  • In addition to first- and second-line antimalarial drug treatments, adjunctive and supportive care measures (e.g., intravenous fluids, blood transfusions, supplemental oxygen, antiseizure medications) may be needed for severe manifestations. (nationalacademies.org)
  • Piperaquine was developed under the Chinese National Malaria Elimination Programme in the 1960s and was adopted throughout China as a replacement for the structurally similar antimalarial drug chloroquine. (wikipedia.org)
  • Due to widespread parasite resistance to piperaquine, the drug fell out of use as a monotherapy, and is instead used as a partner drug for artemisinin combination therapy. (wikipedia.org)
  • In the 1970s and 1980s piperaquine became the primary antimalarial drug of the Chinese National Malaria Control Programme due to increased parasite resistance to chloroquine. (wikipedia.org)
  • Xiao Liang and colleagues have recently published a promising early study on this subject in Cell & Bioscience , reporting the results of a preliminary experiment using the antimalarial drug chloroquine to aid treatment of the cancer. (biomedcentral.com)
  • The researchers explored the use of chloroquine, a drug traditionally used as an anti-malarial, in combination with a chemotherapeutic agent to enhance its effect and prevent resistance. (biomedcentral.com)
  • Chloroquine is a synthetic drug mainly used for the treatment of malaria. (vedantu.com)
  • The chloroquine has a lysosomotropic character, which helps to perform as an antimalarial drug. (vedantu.com)
  • Chloroquine drug concentrates on acidic food vacuole of the parasite and enters into the essential process. (vedantu.com)
  • SUMMARY Studies done between 1997 and 2003 are reviewed to give an overall picture of antimalarial drug resistance in the Eastern Mediterranean Region of the World Health Organization (WHO). (who.int)
  • An overview of drug resistance gion. (who.int)
  • It is of great importance to identify new drug target as well as to understand the mechanisms that lead to drug resistance in the first instance in order to potentially reverse the resistant phenotypes and to avoid the development of resistance in the future. (gla.ac.uk)
  • Apart form its other functions GSH has previously been suggested to be involved in resistance to the antimalarial drug chloroquine (CQ). (gla.ac.uk)
  • CQ was for a long time the first line antimalarial drug due to its high efficiency, low cost and low toxicity, but is now widely inefficient in the treatment of the disease. (gla.ac.uk)
  • Combination treatment of malaria has become the accepted paradigm in malaria control, with the particular aim of delaying and possibly reversing the development of drug resistance [ 2 ]. (biomedcentral.com)
  • These numbers are going up, rather than down, because of increasing drug resistance of the malaria parasite and increasing insecticide resistance of the mosquito vector. (child-survival.org)
  • Also, there are increasing cases of antibiotics resistance among most causative agents of diseases in human beings, which calls for an alternative drug discovery using natural sources. (frontiersin.org)
  • As parasite has developed resistance to artemisinin drugs in Southern Asia, the contribution of the partner drug gets more attention. (biomedcentral.com)
  • The specific drug of choice is based on the pattern and prevalence of drug resistance in the patient's geographic area. (medscape.com)
  • Owing to the emergence of drug resistance, drugs that have been efficacious in the past may no longer be effective. (medscape.com)
  • Fixed-dose drug combinations may be an alternative if response is not seen to the above drugs and if drug resistance is suspected. (medscape.com)
  • The success of these alternative antimalarial drugs in treating acute drug-resistant malaria may not be reflected in treating HMS. (medscape.com)
  • Before the discovery of artemisinin, chloroquine was an effective antimalarial drug. (medicaltrend.org)
  • Unfortunately, even today, even the "magic antimalarial drug" artemisinin has developed drug resistance. (medicaltrend.org)
  • The report also includes a summary on the status of drug resistance for TB, HIV and malaria. (who.int)
  • The study of herbal medicine spans the knowledge of biology, history, source, physical and chemical nature, and mechanism of action, traditional, medicinal and therapeutic use of drug. (thctotalhealthcare.com)
  • Our objectives are to investigate the synergistic effects of GSK-3β in combination with autophagy inhibitors to evade GSK-3β drug resistance. (mdpi.com)
  • Malaria drug resistance in Tanzania / by T. K. Mutabingwa. (who.int)
Widespread1
  • It has been difficult to abandon chloroquine as first-line treatment even though resistance to it is widespread. (who.int)
Widely3
  • Atabrine (quinacrine), the first antimalarial widely used, had numerous side effects including yellowing of the skin. (ccjm.org)
  • However, for P. vivax , the most widely distributed and difficult to treat malaria parasite, a strict preference for reticulocytes thwarts efforts to maintain it in vitro. (nature.com)
  • If atovaquone were used as widely as chloroquine, we'd expect about a billion or more origins of resistance to it by now, not a measly handful. (blogspot.com)
Parasite resistance3
  • Increasing parasite resistance has imposed restrictions to the currently available antimalarial drugs. (scielo.br)
  • By the late 1980s, the use of piperaquine as an antimalarial monotherapy diminished as increasing parasite resistance to piperaquine was observed. (wikipedia.org)
  • As a new generation of artemisinin-based combinations, NQ is used in combination with artemisinin (ARCO ® ), which is recommended to be taken orally as a single-dose regimen to improve patient compliance and avoid rapid development of parasite resistance [ 8 ]. (biomedcentral.com)
Atovaquone2
Antimicrobial1
  • Antimicrobial resistance (AMR) remains an alarming public health threat worldwide. (who.int)
Heme5
  • Like chloroquine, piperaquine is thought to function by accumulating in the parasite digestive vacuole and interfering with the detoxification of heme into hemozoin. (wikipedia.org)
  • Chloroquine covers hemozoin molecules to prevent further biocrystallization of heme thus helps to heme buildup. (vedantu.com)
  • The chloroquine join to heme to form the FP-chloroquine complex. (vedantu.com)
  • GSH is able to degrade heme, the target of CQ, in vitro and it has been suggested that elevated GSH levels contribute to CQ resistance. (gla.ac.uk)
  • David Sullivan and his team are investigating how current malaria drugs like chloroquine inhibit heme crystallization to kill the parasite, and they are screening existing FDA-approved drugs for antimalarial action based on this process. (child-survival.org)
Efficacy1
  • in western Cambodia, manifested as delayed parasite clearance, is a big threat to the long-term efficacy of this family of antimalarial drugs. (2medicalcare.com)
Anticancer1
  • The induction of autophagy is a mechanism of secondary resistance to various anticancer treatments. (mdpi.com)
Infection3
  • Seidah tells The Scientist that the mechanism by which chloroquine disrupts infection by a coronavirus remains unclear. (the-scientist.com)
  • A major focus in Nirbhay Kumar's laboratory is investigating molecular mechanisms involved in the differentiation and development of sexual stages of the parasite leading to mosquito infection and malaria transmission with the goal of developing a transmission-blocking vaccine. (child-survival.org)
  • Because epidemiologic and other data suggest that HMS is related to malarial infection, antimalarial drugs have been used and have been effective. (medscape.com)
Strains1
  • These strains are showing resistant behaviour to chloroquine this is because mainly due to the evolution of species. (vedantu.com)
Digestive vacuole1
  • Chloroquine transfers CQ2+ protons as the digestive vacuole is acidic. (vedantu.com)
Mutation1
Unclear1
  • however, the precise mechanisms of action of the active metabolite(s) are unclear. (bvsalud.org)
Potency2
  • C3 showed antimalarial potency similar to the iron chelators. (biorxiv.org)
  • In silico binding study of compound 5d with plasmodial cysteine protease falcipain-2 indicated the inhibition of falcipain-2 as the probable reason for the antimalarial potency of compound 5d . (biomedcentral.com)
Chemically1
  • It is one of the quinoline derivatives and a member of chemically related antimalarial agents. (vedantu.com)
Piperaquine2
  • Like chloroquine, piperaquine can prolong the QT interval. (wikipedia.org)
  • Amplification of the parasite proteases plasmepsin 2 and plasmepsin 3, both involved in degrading host hemoglobin, is associated with resistance to piperaquine. (wikipedia.org)
Candidates1
  • The in vitro antipromastigote and antiamastigote activity are promising for all candidates and superior to the reference miltefosine, in a low or sub micromolar range of activity. (bvsalud.org)
1980s1
Effective7
  • Thus, the search for new, effective and safe antimalarial drugs is crucial. (scielo.br)
  • Coartem Tablets have been shown to be effective in geographical regions where resistance to chloroquine has been reported. (nih.gov)
  • The authors suggest that the combination therapy of chloroquine and 5-FU should be considered as an effective strategy for the treatment of gallbladder carcinoma in the future. (biomedcentral.com)
  • The spread of resistance could be slowed down by the adoption of effective national policies and control programmes. (who.int)
  • Antimalarial drugs have been the only drugs to be used in hyperreactive malarial syndrome (HMS) and have been shown to be effective in treatment. (medscape.com)
  • Chloroquine and proguanil appear to be equally effective. (medscape.com)
  • NIR fluorescence imaging using IR700-12A8 and subsequent NIR irradiation could be a very effective theranostic technology for GIST, the underlying mechanism of which appears to involve acute necrosis and supposedly late apoptosis induced by singlet oxygen. (thno.org)
Artemisinins3
  • This chapter describes antimalarial drugs currently in use, with an emphasis on the artemisinins. (nationalacademies.org)
  • 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)
  • The results obtained in this study are consistent with artemisinins and SC83288 having distinct modes of action and different mechanisms of resistance. (biomedcentral.com)
Rheumatoid arthritis1
  • Eight years after the war ended, Shee 4 reported that chloroquine had a beneficial effect on lupus and rheumatoid arthritis in US soldiers. (ccjm.org)
Synthetic1
  • Methylene blue (MB) was the first synthetic antimalarial to be discovered and was used during the late 19th and early 20th centuries against all types of malaria. (biomedcentral.com)
Treat malaria1
  • Since World War II, antimalarial drugs have been intensively used to prevent or treat malaria ( 1 ). (cdc.gov)
Antiviral1
  • His 2005 study reported "strong antiviral effects" in animal cells in vitro. (the-scientist.com)
Experiments4
  • Small-scale experiments in which chloroquine has been given to COVID-19 patients in China and Australia have also shown encouraging results as far as shortening the course of the disease. (the-scientist.com)
  • A number of other chloroquine experiments on humans are in the works. (the-scientist.com)
  • The lysosomotropic properties allow it for the use of in vitro experiments pertaining to intracellular lipid-related disease namely apoptosis and autophagy. (vedantu.com)
  • In vitro metabolism experiments were performed in the liver microsomes of male or female mice, rat or human. (biomedcentral.com)
Action6
  • However, the mechanism of plasmodicidal action of chloroquine is not completely certain. (drugs.com)
  • In other words, in each life-cycle stage the parasite manifests unique biological properties that can offer a target for the action of one or more antimalarial drugs. (nationalacademies.org)
  • This preliminary experiment used gallbladder cancer cell lines in-vitro to model the mechanism of action which would occur within the body. (biomedcentral.com)
  • The action of the toxic FP and FP- chloroquine results in cell lysis and supports parasite cell autodigestion. (vedantu.com)
  • This review aimed to present the various mechanisms of action used by endophytes in protecting a plant and report some bioactivities of importance to people with special emphasis on endophytic bacteria and fungi. (frontiersin.org)
  • The phenomenon of sulfonamide-resistant infections was first discussed in the late 1960s, but the mechanism of action underlying the effectiveness of sulfa drugs only gradually became known, with increasing knowledge of the interaction between PABA and this important class of antibiotics. (interactionsguide.com)
Treatment2
  • Antimalarials should not be given concomitantly, unless there is no other treatment option, due to limited safety data. (nih.gov)
  • The pre-treatment of carcinoma cells with chloroquine resulted in an increased effectiveness of the chemotherapeutic agent 5-fluorouracil (5-FU), causing increased cancer cell death. (biomedcentral.com)
Toxic1
  • Chloroquine makes it toxic for the parasite to digest its host's hemoglobin. (the-scientist.com)
Parasitemia1
Therapeutic2
  • The therapeutic mechanisms of these SP vary, hence it is yet to be studied precisely. (springer.com)
  • We also investigated the therapeutic mechanisms. (thno.org)
Africa1
  • This report presents the status of AMR in Africa by analysing the main types of resistance and the underlying genes where possible. (who.int)
Activity2
  • In vitro studies with trophozoites of Entamoeba histolytica have demonstrated that chloroquine also possesses amebicidal activity comparable to that of emetine. (drugs.com)
  • Based on a structure-guided approach, they were designed to possess antileishmanial activity through antifolate mechanism, via targeting Leishmania major pteridine reductase 1 (Lm-PTR1). (bvsalud.org)
Clinical1
Lupus1
  • A serendipitous consequence of the mass use of antimalarials during World War II was the discovery that they could be used to treat inflammatory arthritis and lupus. (ccjm.org)