Relevant bibliographies by topics / Plasmodium falciparum. Malaria Antimalarials. Malariotherapy

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Academic literature on the topic 'Plasmodium falciparum. Malaria Antimalarials. Malariotherapy'

Author: Grafiati
Published: 4 June 2021
Last updated: 16 February 2022

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Journal articles on the topic "Plasmodium falciparum. Malaria Antimalarials. Malariotherapy"

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Giannangelo, Carlo, Dovile Anderson, Xiaofang Wang, Jonathan L. Vennerstrom, Susan A. Charman, and Darren J. Creek. "Ozonide Antimalarials Alkylate Heme in the Malaria Parasite Plasmodium falciparum." ACS Infectious Diseases 5, no. 12 (October 17, 2019): 2076–86. http://dx.doi.org/10.1021/acsinfecdis.9b00257.

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Dembele, Laurent, Yaw Aniweh, Nouhoum Diallo, Fanta Sogore, Cheick Papa Oumar Sangare, Aboubecrin Sedhigh Haidara, Aliou Traore, et al. "Plasmodium malariae and Plasmodium falciparum comparative susceptibility to antimalarial drugs in Mali." Journal of Antimicrobial Chemotherapy 76, no. 8 (May 22, 2021): 2079–87. http://dx.doi.org/10.1093/jac/dkab133.

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Abstract Objectives To evaluate Plasmodium malariae susceptibility to current and lead candidate antimalarial drugs. Methods We conducted cross-sectional screening and detection of all Plasmodium species malaria cases, which were nested within a longitudinal prospective study, and an ex vivo assessment of efficacy of a panel of antimalarials against P. malariae and Plasmodium falciparum, both PCR-confirmed mono-infections. Reference compounds tested included chloroquine, lumefantrine, artemether and piperaquine, while candidate antimalarials included the imidazolopiperazine GNF179, a close analogue of KAF156, and the Plasmodium phosphatidylinositol-4-OH kinase (PI4K)-specific inhibitor KDU691. Results We report a high frequency (3%–15%) of P. malariae infections with a significant reduction in ex vivo susceptibility to chloroquine, lumefantrine and artemether, which are the current frontline drugs against P. malariae infections. Unlike these compounds, potent inhibition of P. malariae and P. falciparum was observed with piperaquine exposure. Furthermore, we evaluated advanced lead antimalarial compounds. In this regard, we identified strong inhibition of P. malariae using GNF179, a close analogue of KAF156 imidazolopiperazines, which is a novel class of antimalarial drug currently in clinical Phase IIb testing. Finally, in addition to GNF179, we demonstrated that the Plasmodium PI4K-specific inhibitor KDU691 is highly inhibitory against P. malariae and P. falciparum. Conclusions Our data indicated that chloroquine, lumefantrine and artemether may not be suitable for the treatment of P. malariae infections and the potential of piperaquine, as well as new antimalarials imidazolopiperazines and PI4K-specific inhibitor, for P. malariae cure.
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Subramanian, Gowtham, Abdul Sadeer, Kalyani Mukherjee, Tadayuki Kojima, Pallavi Tripathi, Renugah Naidu, Shan Wen Tay, Jia Hao Pang, Sumod A. Pullarkat, and Rajesh Chandramohanadas. "Evaluation of ferrocenyl phosphines as potent antimalarials targeting the digestive vacuole function of Plasmodium falciparum." Dalton Transactions 48, no. 3 (2019): 1108–17. http://dx.doi.org/10.1039/c8dt04263b.

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Wicht, Kathryn J., Sachel Mok, and David A. Fidock. "Molecular Mechanisms of Drug Resistance in Plasmodium falciparum Malaria." Annual Review of Microbiology 74, no. 1 (September 8, 2020): 431–54. http://dx.doi.org/10.1146/annurev-micro-020518-115546.

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Understanding and controlling the spread of antimalarial resistance, particularly to artemisinin and its partner drugs, is a top priority. Plasmodium falciparum parasites resistant to chloroquine, amodiaquine, or piperaquine harbor mutations in the P. falciparum chloroquine resistance transporter (PfCRT), a transporter resident on the digestive vacuole membrane that in its variant forms can transport these weak-base 4-aminoquinoline drugs out of this acidic organelle, thus preventing these drugs from binding heme and inhibiting its detoxification. The structure of PfCRT, solved by cryogenic electron microscopy, shows mutations surrounding an electronegative central drug-binding cavity where they presumably interact with drugs and natural substrates to control transport. P. falciparum susceptibility to heme-binding antimalarials is also modulated by overexpression or mutations in the digestive vacuole membrane–bound ABC transporter PfMDR1 ( P. falciparum multidrug resistance 1 transporter). Artemisinin resistance is primarily mediated by mutations in P. falciparum Kelch13 protein (K13), a protein involved in multiple intracellular processes including endocytosis of hemoglobin, which is required for parasite growth and artemisinin activation. Combating drug-resistant malaria urgently requires the development of new antimalarial drugs with novel modes of action.
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Opsenica, Dejan Milos, and Bogdan Aleksandar Šolaja. "Artemisinins and synthetic peroxides as highly efficient antimalarials." Macedonian Journal of Chemistry and Chemical Engineering 31, no. 2 (December 20, 2012): 137. http://dx.doi.org/10.20450/mjcce.2012.50.

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Malaria is devastating disease and global public health problem, with nearly half world population exposed to risk. Illness is caused by five Plasmodium species, P. falciparum, P. ovale, P. vivax, P. malarie and P. knowlesi, from which P. falciparum is the most serious one causing cerebral malaria and is the major reason for malaria mortality. Vaccine against malaria is not expected in the near future and chemotherapy remains as most feasible alternative for treatment of the disease. The development of widespread drug-resistance to chloroquine (CQ), the most successful antimalarial drug up to date, has resulted in severe health issues for countries in malaria endemic regions. Organic peroxides, like artemisinins, 1,2,4-trioxanes, 1,2,4-trioxolanes, 1,2,4,5-tetraoxanes and their chimeras, are the best choice for malaria treatment nowadays. These therapeutics are fast acting, non-toxic, low costing and without reported data of parasite resistance. Stability of peroxide bonds enables synthetic comfort and resulting in diversity of synthesised structures. The most important classes of peroxide antimalarials with promising representatives are reviewed and possible mechanisms of action were presented in details.
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Miller III, Whelton A., Joshua Teye, Angela O. Achieng, Reagan M. Mogire, Hoseah Akala, John M. Ong'echa, Brijesh Rathi, Ravi Durvasula, Prakasha Kempaiah, and Samuel K. Kwofie. "Antimalarials: Review of Plasmepsins as Drug Targets and HIV Protease Inhibitors Interactions." Current Topics in Medicinal Chemistry 18, no. 23 (January 10, 2019): 2022–28. http://dx.doi.org/10.2174/1568026619666181130133548.

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Malaria is a major global health concern with the majority of cases reported in regions of South-East Asia, Eastern Mediterranean, Western Pacific, the Americas, and Sub-Saharan Africa. The World Health Organization (WHO) estimated 216 million worldwide reported cases of malaria in 2016. It is an infection of the red blood cells by parasites of the genus Plasmodium with most severe and common forms caused by Plasmodium falciparum (P. falciparum or Pf) and Plasmodium vivax (P. vivax or Pv). Emerging parasite resistance to available antimalarial drugs poses great challenges to treatment. Currently, the first line of defense includes artemisinin combination therapies (ACTs), increasingly becoming less effective and challenging to combat new occurrences of drug-resistant parasites. This necessitates the urgent need for novel antimalarials that target new molecular pathways with a different mechanism of action from the traditional antimalarials. Several new inhibitors and potential drug targets of the parasites have been reported over the years. This review focuses on the malarial aspartic proteases known as plasmepsins (Plms) as novel drug targets and antimalarials targeting Plms. It further discusses inhibitors of hemoglobin-degrading plasmepsins Plm I, Plm II, Plm IV and Histo-aspartic proteases (HAP), as well as HIV protease inhibitors of plasmepsins.
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Morales-Bayuelo, Alejandro. "New molecular target insights about protein kinases of the Plasmodium falciparum. Using molecular docking and DFT-based reactivity descriptors." Journal of Theoretical and Computational Chemistry 16, no. 08 (December 2017): 1750076. http://dx.doi.org/10.1142/s0219633617500766.

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Currently, there is increasing interest in the potential of malaria inhibitors in Plasmodium falciparum activity. In this work, is propose a possible alternative to classifying 154 antimalarials, with P. falciparum activity. These antimalarials were synthesized by the Chibale’s group ( http://www.kellychibaleresearch.uct.ac.za/ ), with the goal of finding new insights on the binding pocket of the protein kinase PfPK5, PfPK7, PfCDPK1, PfCDPK4, PfMAP1, and PfPK6 of the malaria parasite. However, there is only information about crystallography of PfPK5 and PfPK7. The protein kinases PfCDPK1, PfCDPK4, PfMAP1, and PfPK6 were modeled using molecular homology. The validation used shows that our homology models can be an alternative for the protein kinases from P. falciparum, unknown today. The antimalarials were classified by taking into account the interactions in the hinge zone. These ligands bind to the kinase through the formation of one of two hydrogen bonds, with the backbone residues of the hinge region connecting the kinase N- and C-terminal loops. These interactions were supported by a reactivity chemistry analysis, using global chemical reactivity descriptors such as chemical potential, hardness, softness, electrophilicity, and the Fukui functions as local reactivity descriptors, within the Density Functional Theory (DFT) context.
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Wilson, Danny W., Christine Langer, Christopher D. Goodman, Geoffrey I. McFadden, and James G. Beeson. "Defining the Timing of Action of Antimalarial Drugs against Plasmodium falciparum." Antimicrobial Agents and Chemotherapy 57, no. 3 (January 14, 2013): 1455–67. http://dx.doi.org/10.1128/aac.01881-12.

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ABSTRACTMost current antimalarials for treatment of clinicalPlasmodium falciparummalaria fall into two broad drug families and target the food vacuole of the trophozoite stage. No antimalarials have been shown to target the brief extracellular merozoite form of blood-stage malaria. We studied a panel of 12 drugs, 10 of which have been used extensively clinically, for their invasion, schizont rupture, and growth-inhibitory activity using high-throughput flow cytometry and new approaches for the study of merozoite invasion and early intraerythrocytic development. Not surprisingly, given reported mechanisms of action, none of the drugs inhibited merozoite invasionin vitro. Pretreatment of erythrocytes with drugs suggested that halofantrine, lumefantrine, piperaquine, amodiaquine, and mefloquine diffuse into and remain within the erythrocyte and inhibit downstream growth of parasites. Studying the inhibitory activity of the drugs on intraerythrocytic development, schizont rupture, and reinvasion enabled several different inhibitory phenotypes to be defined. All drugs inhibited parasite replication when added at ring stages, but only artesunate, artemisinin, cycloheximide, and trichostatin A appeared to have substantial activity against ring stages, whereas the other drugs acted later during intraerythrocytic development. When drugs were added to late schizonts, only artemisinin, cycloheximide, and trichostatin A were able to inhibit rupture and subsequent replication. Flow cytometry proved valuable forin vitroassays of antimalarial activity, with the free merozoite population acting as a clear marker for parasite growth inhibition. These studies have important implications for further understanding the mechanisms of action of antimalarials, studying and evaluating drug resistance, and developing new antimalarials.
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Tanaka, Takeshi Q., W. Armand Guiguemde, David S. Barnett, Maxim I. Maron, Jaeki Min, Michele C. Connelly, Praveen Kumar Suryadevara, R. Kiplin Guy, and Kim C. Williamson. "Potent Plasmodium falciparum Gametocytocidal Activity of Diaminonaphthoquinones, Lead Antimalarial Chemotypes Identified in an Antimalarial Compound Screen." Antimicrobial Agents and Chemotherapy 59, no. 3 (December 15, 2014): 1389–97. http://dx.doi.org/10.1128/aac.01930-13.

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ABSTRACTForty percent of the world's population is threatened by malaria, which is caused byPlasmodiumparasites and results in an estimated 200 million clinical cases and 650,000 deaths each year. Drug resistance has been reported for all commonly used antimalarials and has prompted screens to identify new drug candidates. However, many of these new candidates have not been evaluated against the parasite stage responsible for transmission, gametocytes. IfPlasmodium falciparumgametocytes are not eliminated, patients continue to spread malaria for weeks after asexual parasite clearance. Asymptomatic individuals can also harbor gametocyte burdens sufficient for transmission, and a safe, effective gametocytocidal agent could also be used in community-wide malaria control programs. Here, we identify 15 small molecules with nanomolar activity against late-stage gametocytes. Fourteen are diaminonaphthoquinones (DANQs), and one is a 2-imino-benzo[d]imidazole (IBI). One of the DANQs identified, SJ000030570, is a lead antimalarial candidate. In contrast, 94% of the 650 compounds tested are inactive against late-stage gametocytes. Consistent with the ineffectiveness of most approved antimalarials against gametocytes, of the 19 novel compounds with activity against known anti-asexual-stage targets, only 3 had any strong effect on gametocyte viability. These data demonstrate the distinct biology of the transmission stages and emphasize the importance of screening for gametocytocidal activity. The potent gametocytocidal activity of DANQ and IBI coupled with their efficacy against asexual parasites provides leads for the development of antimalarials with the potential to prevent both the symptoms and the spread of malaria.
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Kaddouri, Halima, Serge Nakache, Sandrine Houzé, France Mentré, and Jacques Le Bras. "Assessment of the Drug Susceptibility of Plasmodium falciparum Clinical Isolates from Africa by Using a Plasmodium Lactate Dehydrogenase Immunodetection Assay and an Inhibitory Maximum Effect Model for Precise Measurement of the 50-Percent Inhibitory Concentration." Antimicrobial Agents and Chemotherapy 50, no. 10 (October 2006): 3343–49. http://dx.doi.org/10.1128/aac.00367-06.

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ABSTRACT The extension of drug resistance among malaria-causing Plasmodium falciparum parasites in Africa necessitates implementation of new combined therapeutic strategies. Drug susceptibility phenotyping requires precise measurements. Until recently, schizont maturation and isotopic in vitro assays were the only methods available, but their use was limited by technical constraints. This explains the revived interest in the development of replacement methods, such as the Plasmodium lactate dehydrogenase (pLDH) immunodetection assay. We evaluated a commercially controlled pLDH enzyme-linked immunosorbent assay (ELISA; the ELISA-Malaria antigen test; DiaMed AG, Cressier s/Morat, Switzerland) to assess drug susceptibility in a standard in vitro assay using fairly basic laboratory equipment to study the in vitro resistance of malaria parasites to major antimalarials. Five Plasmodium falciparum clones and 121 clinical African isolates collected during 2003 and 2004 were studied by the pLDH ELISA and the [8-3H]hypoxanthine isotopic assay as a reference with four antimalarials. Nonlinear regression with a maximum effect model was used to estimate the 50% inhibitory concentration (IC50) and its confidence intervals. The two methods were observed to have similar reproducibilities, but the pLDH ELISA demonstrated a higher sensitivity. The high correlation (r = 0.98) and the high phenotypic agreement (κ = 0.88) between the two methods allowed comparison by determination of the IC50s. Recently collected Plasmodium falciparum African isolates were tested by pLDH ELISA and showed drug resistance or decreased susceptibilities of 62% to chloroquine and 11.5% to the active metabolite of amodiaquine. No decreased susceptibility to lumefantrine or the active metabolite of artemisinin was detected. The availability of this simple and highly sensitive pLDH immunodetection assay will provide an easier method for drug susceptibility testing of malaria parasites.
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Dissertations / Theses on the topic "Plasmodium falciparum. Malaria Antimalarials. Malariotherapy"

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Botha, Maria Magdalena. "Structure-based inhibitor design and validation : application to Plasmodium falciparum glutathione S-transferase." Diss., Pretoria : [s.n.], 2007. http://upetd.up.ac.za/thesis/available/etd-07212008-140458/.

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Birkholtz, Lyn-Marie. "Functional and structural characterization of the unique bifunctional enzyme complex involved in regulation of polyamine metabolism in Plasmodium falciparum." Pretoria : [s.n.], 2005. http://upetd.up.ac.za/thesis/available/etd-06302005-120320/.

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Van, Brummelen Anna Catharina. "Functional genomics analysis of the effects of co-inhibition of the malarial S-adenosylmethionine decarboxylase/ornithine decarboxylase." Pretoria : [s.n.], 2009. http://upetd.up.ac.za/thesis/available/etd-05302009-124548.

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Human, Esmaré. "Kinetic analysis of a recombinantly expressed Plasmodium falciparum dihydrofolate synthase-folylpolyglutamate synthase." Pretoria : [s.n.], 2007. http://upetd.up.ac.za/thesis/available/etd-06252008-093616/.

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Thesis (MSc Natural and Agricultural Sciences (Biochemistry))-University of Pretoria, 2007.
Summary in English and Afrikaans. Includes bibliographical references. Available on the Internet via the World Wide Web.
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Birkholtz, Lyn-Marie. "Functional and structural charaterization of the unique bifunctional enzyme complex involved in regulation of polyamine metabolism in Plasmodium falciparum." Thesis, University of Pretoria, 2001. http://hdl.handle.net/2263/25944.

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Malaria remains one of the most serious tropical infectious diseases affecting mankind. The prevention of the disease is hampered by the increasing resistance of the parasite to existing chemotherapies. The need for novel therapeutic targets and drugs is therefore of the utmost importance and detailed knowledge of the biochemistry of the parasite is imperative. This study was directed at the biochemical characterisation of the polyamine metabolic pathway of P. falciparum in order to elucidate differences between the parasite and its human host that can be exploited in the design of novel antimalarials. The thesis focussed on the two rate-limiting enzymes in polyamine biosynthesis, S¬adenosylmethionine decarboxylase (AdoMetDC) and ornithine decarboxylase (ODC), which occur as a unique bifunctional complex in P. falciparum. The genomic structure of the bifunctional gene indicated a single, monocistronic transcript with large untranslated regions that were predicted to be involved in unique translational regulatory mechanisms. This gives rise to a bifunctional protein containing both decarboxylase activities on a single polypeptide forming a heterotetrameric complex. Activity of the decarboxylases decreases dramatically if these proteins are expressed in their monofunctional forms as homodimeric ODC and heterotetrameric AdoMetDC. The deduced amino acid sequence indicated that all the essential residues for catalysis are conserved and highlighted the presence of three parasite-specific insertions. The parasite-specific inserts were shown to be essential for the catalytic activity of the respective domains and also to influence the activity of the neighbouring domain, indicating that intramolecular communication exists in the heterotetrameric complex. The most structured and smallest insert was also shown to mediate protein-protein interactions between the two domains and to stabilise the complex. Further structure- functional characterisations of specifically the ODC domain were deduced from a comparative homology model. The model predicted an overall structure corresponding to those of other homologous proteins. The validity of the model is supported by mutagenesis results. However, certain parasite-specific properties were identified in the active site pocket and dimerisation interface. The former was exploited in the rational design of novel putative ODC inhibitors directed only against the P. falciparumprotein by in silico screening of chemical structure libraries. This study therefore describes the identification of certain parasite-specific properties in a unique bifunctional protein involved in regulation of polyamine metabolism of P. falciparum. Such discoveries are invaluable in strategies aimed at elucidating biochemical and metabolic differences between the parasite and its human host that could be exploited in the design of alternative, parasite-specific chemotherapies. Moreover, the thesis also contributed new knowledge on certain less well-understood biological phenomena characteristic of P. falciparum, the nature and origin of bifunctional proteins and the functional properties of parasite-specific inserts found in some proteins of the parasite.
Thesis (PhD (Biochemistry))--University of Pretoria, 2002.
Biochemistry
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Dhoogra, Minishca. "Gene expression profiling of polyamine-depleted Plasmodium falciparum." Diss., Pretoria : [s.n.], 2007. http://upetd.up.ac.za/thesis/available/etd-12132007-103643/.

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Kayano, Ana Carolina Andrade Vitor 1984. "Avaliação in vivo e in vitro da atividade antimalárica de Caesalpinia pluviosa e análise da fração ativa." [s.n.], 2011. http://repositorio.unicamp.br/jspui/handle/REPOSIP/316725.

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Orientador: Fabio Trindade Maranhão Costa
Dissertação (mestrado) - Universidade Estadual de Campinas, Instituto de Biologia
Made available in DSpace on 2018-08-18T14:00:00Z (GMT). No. of bitstreams: 1 Kayano_AnaCarolinaAndradeVitor_M.pdf: 4619978 bytes, checksum: 3bf657caae96f9c4faf7fcdf7e519956 (MD5) Previous issue date: 2011
Resumo: Para superar o problema do aumento de resistência às drogas, os medicamentos tradicionais são fontes importantes na investigação de potenciais novos antimaláricos. Caesalpinia pluviosa, mais conhecida como 'sibipiruna', é originária do Brasil e estudos mostraram que este gênero apresenta várias propriedades farmacológicas, incluindo a atividade antimalárica. O extrato bruto obtido da casca foi submetido ao fracionamento com diferentes solventes resultando em sete frações. Para avaliar a citotoxicidade do extrato e frações em células MCF-7 foi realizado o ensaio de MTT. Essas amostras foram testadas in vitro contra P. falciparum cloroquino sensível (3D7) e resistente (S20) e in vivo em camundongos infectados por P. chabaudi. A interação da fração etanólica 100% de C. pluviosa com o artesunato foi avaliado e análises de espectrometria de massas foram realizados. As frações etanólica 100% e metanólica 50% apresentaram atividade antimalárica significativa em concentrações não tóxicas, e o ensaio de interação medicamentosa do artesunato com a fração etanólica 100% foi sinérgico. Essa fração foi capaz de inibir significativamente a parasitemia dos animais de forma dose dependente após 4 dias de tratamento (0-3 dia pós infecção). Além disso, análise de espectrometria de massas revelou a presença do íon m/z 303.0450, sugerindo a presença de quercetina. No entanto, em uma segunda análise com o padrão de quercetina mostrou íons diferentes como m/z 137 e 153. Nossos resultados mostram que a fração etanólica 100% de C. pluviosa apresentou atividade antimalárica in vitro em concentrações não tóxicas e esse efeito foi potencializado com a presença de artesunato. Além disso, essa atividade antimalárica foi também sustentada após o tratamento in vivo de camundongos infectados. Finalmente, as análises de espectrometria de massas sugerem que um novo composto, provavelmente um isômero da quercetina, possa estar relacionado à atividade antimalárica da fração etanólica 100%
Abstract: To overcome the problem of increasing drug resistance traditional medicines are an important source for investigation of potential new antimalarials. Caesalpinia pluviosa, commonly named 'sibipiruna', is originated from Brazil and studies showed that this genus present multiple therapeutic properties, including antimalarial activity. Crude extract obtained from stem bark was purified with different solvents, resulting in seven fractions. MTT assay was performed to evaluate cytotoxicity in MCF-7 cells. The crude extract and its fractions were tested in vitro against chloroquine-sensitive (3D7) and -resistant (S20) strains of Plasmodium falciparum and in vivo in P. chabaudi-infected mice. In vitro interaction with artesunate and C. pluviosa fraction was assessed and mass spectrometry analyses were conducted. At non-toxic concentrations the 100% ethanolic and 50% methanolic fractions presented significant antimalarial activity against both 3D7 and S20 strains, and drug interaction assays with artesunate showed a synergistic effect with 100% ethanolic fraction. This fraction was able to inhibit mice parasitemia significantly and in a dose dependent manner after 4 days treatment (0-3 post-infection). Moreover, mass spectrometry analyses revealed the presence of an ion corresponding to m/z 303.0450, suggesting the presence of quercetin. However, a second set of analyses, with the standard quercetin, showed distinct ions of m/z 137 and 153. Our findings show that the 100% ethanolic fraction of C. pluviosa exhibited antimalarial activity in vitro at non-toxic concentrations and this effect was potentiated with the presence of artesunate. Moreover, this antimalarial activity was also sustained in vivo after treatment of infected mice. Finally, mass spectrometry analyses suggest a new compound, most likely an isomer of quercetin, related with antimalarial activity of the 100% ethanolic fraction
Mestrado
Imunologia
Mestre em Genética e Biologia Molecular
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Gupta, Seema. "Experimental pharmacodynamic and kinetic studies related to new combination therapies against falciparum malaria /." Stockholm : Karolinska institutet, 2007. http://diss.kib.ki.se/2007/978-91-7357-066-4/.

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Yao, Jia. "Synthesis of silver nanoparticles and their role against a thiazolekinase enzyme from Plasmodium falciparum." Thesis, Rhodes University, 2014. http://hdl.handle.net/10962/d1020894.

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Malaria, a mosquito-borne infectious disease, caused by the protozoan Plasmodium genus, is the greatest health challenges worldwide. The plasmodial vitamin B1 biosynthetic enzyme PfThzK diverges significantly, both structurally and functionally from its counterpart in higher eukaryotes, thereby making it particularly attractive as a biomedical target. In the present study, PfThzK was recombinantly produced as 6×His fusion protein in E. coli BL21, purified using nickel affinity chromatography and size exclusion chromatography resulting in 1.03% yield and specific activity 0.28 U/mg. The enzyme was found to be a monomer with a molecular mass of 34 kDa. Characterization of the PfThzK showed an optimum temperature and pH of 37°C and 7.5 respectively, and it is relatively stable (t₁/₂=2.66 h). Ag nanoparticles were synthesized by NaBH₄/tannic acid, and characterized by UV-vis spectroscopy and transmission electron microscopy. The morphologies of these Ag nanoparticles (in terms of size) synthesized by tannic acid appeared to be more controlled with the size of 7.06±2.41 nm, compared with those synthesized by NaBH₄, with the sized of 12.9±4.21 nm. The purified PfThzK was challenged with Ag NPs synthesized by tannic acid, and the results suggested that they competitively inhibited PfThzK (89 %) at low concentrations (5-10 μM) with a Ki = 6.45 μM.
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Ursing, Johan. "Plasmodium Falciparum response to chloroquine and artemisinin based combination therapy (Act) in Guinea Bissau." Stockholm : Karolinska institutet, 2009. http://diss.kib.ki.se/2009/978-91-7409-695-8/.

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Books on the topic "Plasmodium falciparum. Malaria Antimalarials. Malariotherapy"

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Guidelines for the epidemiological evaluation of plasmodium falciparum sporozoite vaccines. Geneva: World Health Organization, 1986.

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Book chapters on the topic "Plasmodium falciparum. Malaria Antimalarials. Malariotherapy"

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Budi Setia Asih, Puji, and Din Syafruddin. "Plasmodium vivax and Drug Resistance." In Plasmodium Species and Drug Resistance [Working Title]. IntechOpen, 2021. http://dx.doi.org/10.5772/intechopen.97320.

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Resistance to antimalarial drugs is a threat to global efforts to eliminate malaria by 2030. Currently, treatment for vivax malaria uses chloroquine or ACT for uncomplicated P. vivax whereas primaquine is given to eliminate latent liver stage infections (a method known as radical cure). Studies on P. vivax resistance to antimalarials and the molecular basis of resistance lags far behind the P. falciparum as in vitro cultivation of the P. vivax has not yet been established. Therefore, data on the P. vivax resistance to any antimalarial drugs are generated through in vivo studies or through monitoring of antimalarial treatments in mixed species infection. Indirect evidence through drug selective pressure on the parasites genome, as evidenced by the presence of the molecular marker(s) for drug resistance in areas where P. falciparum and P. vivax are distributed in sympatry may reflect, although require validation, the status of P. vivax resistance. This review focuses on the currently available data that may represent the state-of-the art of the P. vivax resistance status to antimalarial to anticipate the challenge for malaria elimination by 2030.
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H. Asakawa, Ami, and Roman Manetsch. "A Comprehensive Review of 4(1H)-Quinolones and 4(1H)-Pyridones for the Development of an Effective Antimalarial." In Plasmodium Species and Drug Resistance [Working Title]. IntechOpen, 2021. http://dx.doi.org/10.5772/intechopen.97084.

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Malaria is a global public health issue. Despite the efforts in malaria prevention, nearly half the world’s population is at risk of infection. Until present-day, researchers are struggling to design and discover an efficacious antimalarial. In comparison to most common antimalarial chemotypes that eliminate erythrocytic stages of P. falciparum, 4(1H)-quinolones and 4(1H)-pyridones exhibit antimalarial activity against multiple stages of the parasite. They have potential to treat blood stages of multidrug resistant P. falciparum malaria, eradicate dormant exoerythro stages of relapsing malaria species (P. vivax), and prevent transmission of infectious gametocytes to mosquitoes. However, thus far, the advancement of these chemotypes towards pre-clinical and clinical development has been impeded due to poor physicochemical properties, poor oral bioavailability, and poor dose-proportionality limiting preclinical safety and toxicity studies. Despite all these challenges, 4(1H)-quinolones and 4(1H)-pyridones continue to be at the forefront for the development of the next-generation antimalarials as they would have tremendous global public health impact and could significantly enhance current malaria elimination efforts.
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Luzzatto, Lucio. "Glucose-6-phosphate dehydrogenase deficiency." In Oxford Textbook of Medicine, edited by Chris Hatton and Deborah Hay, 5472–79. Oxford University Press, 2020. http://dx.doi.org/10.1093/med/9780198746690.003.0541.

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Abstract:
Deficiency of the enzyme glucose-6-phosphate dehydrogenase (G6PD) in red blood cells is an inherited abnormality due to mutations of the G6PD gene on the X chromosome that renders the cells vulnerable to oxidative damage. The condition is widespread in many populations living in or originating from tropical and subtropical areas of the world because it confers a selective advantage against Plasmodium falciparum malaria. Clinical features—G6PD deficiency is mostly an asymptomatic trait, but it predisposes to acute haemolytic anaemia in response to exogenous triggers, including (1) ingestion of fava beans—favism; (2) certain bacterial and viral infections; and (3) some drugs—notably some antimalarials (e.g. primaquine), some antibiotics (e.g. sulphanilamide, dapsone, nitrofurantoin), and even aspirin in high doses. Other manifestations include (1) severe neonatal jaundice; and (2) chronic nonspherocytic haemolytic anaemia—the latter is only seen with rare specific genetic variants. The acute haemolytic attack typically starts with malaise, weakness, and abdominal or lumbar pain, followed by the development of jaundice and passage of dark urine (haemoglobinuria). Most episodes resolve spontaneously. Diagnosis relies on the direct demonstration of decreased activity of G6PD in red cells: a variety of screening tests are available, with (ideally) subsequent confirmation by quantitative assay. Prevention is by avoiding exposure to triggering factors of previously screened subjects. Prompt blood transfusion is indicated in severe acute haemolytic anaemia and may be life-saving.
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