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

Author: Grafiati

Published: 4 June 2021

Last updated: 16 February 2022

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1

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 (2019): 2076–86. http://dx.doi.org/10.1021/acsinfecdis.9b00257.

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Dembele, Laurent, Yaw Aniweh, Nouhoum Diallo, et al. "Plasmodium malariae and Plasmodium falciparum comparative susceptibility to antimalarial drugs in Mali." Journal of Antimicrobial Chemotherapy 76, no. 8 (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 ana

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Subramanian, Gowtham, Abdul Sadeer, Kalyani Mukherjee, et al. "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 (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 el

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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 (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

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Miller III, Whelton A., Joshua Teye, Angela O. Achieng, et al. "Antimalarials: Review of Plasmepsins as Drug Targets and HIV Protease Inhibitors Interactions." Current Topics in Medicinal Chemistry 18, no. 23 (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. Current

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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 (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, PfCD

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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 (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

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Tanaka, Takeshi Q., W. Armand Guiguemde, David S. Barnett, et al. "Potent Plasmodium falciparum Gametocytocidal Activity of Diaminonaphthoquinones, Lead Antimalarial Chemotypes Identified in an Antimalarial Compound Screen." Antimicrobial Agents and Chemotherapy 59, no. 3 (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. Asymptom

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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 (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 im

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Van Tyne, Daria, Alessandro D. Uboldi, Julie Healer, Alan F. Cowman, and Dyann F. Wirth. "Modulation of PF10_0355 (MSPDBL2) Alters Plasmodium falciparum Response to Antimalarial Drugs." Antimicrobial Agents and Chemotherapy 57, no. 7 (2013): 2937–41. http://dx.doi.org/10.1128/aac.02574-12.

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ABSTRACTMalaria's ability to rapidly adapt to new drugs has allowed it to remain one of the most devastating infectious diseases of humans. Understanding and tracking the genetic basis of these adaptations are critical to the success of treatment and intervention strategies. The novel antimalarial resistance locusPF10_0355(Pfmspdbl2) was previously associated with the parasite response to halofantrine, and functional validation confirmed that overexpression of this gene lowered parasite sensitivity to both halofantrine and the structurally related antimalarials mefloquine and lumefantrine, pre

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Caramello, Pietro, Francesca Canta, Ilaria Cavecchia, et al. "Pharmacodynamic Analysis of Antimalarials Used in Plasmodium falciparum Imported Malaria in Northern Italy." Journal of Travel Medicine 12, no. 3 (2006): 127–32. http://dx.doi.org/10.2310/7060.2005.12305.

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Nyamwihura, Rogers J., Huaisheng Zhang, Jasmine T. Collins, Olamide Crown, and Ifedayo Victor Ogungbe. "Nopol-Based Quinoline Derivatives as Antiplasmodial Agents." Molecules 26, no. 4 (2021): 1008. http://dx.doi.org/10.3390/molecules26041008.

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Malaria remains a significant cause of morbidity and mortality in Sub-Saharan Africa and South Asia. While clinical antimalarials are efficacious when administered according to local guidelines, resistance to every class of antimalarials is a persistent problem. There is a constant need for new antimalarial therapeutics that complement parasite control strategies to combat malaria, especially in the tropics. In this work, nopol-based quinoline derivatives were investigated for their inhibitory activity against Plasmodium falciparum, one of the parasites that cause malaria. The nopyl-quinolin-8

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Ramharter, M., H. Noedl, H. Winkler, et al. "In Vitro Activity and Interaction of Clindamycin Combined with Dihydroartemisinin against Plasmodium falciparum." Antimicrobial Agents and Chemotherapy 47, no. 11 (2003): 3494–99. http://dx.doi.org/10.1128/aac.47.11.3494-3499.2003.

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ABSTRACT Combination regimens are considered a valuable tool for the fight against drug-resistant falciparum malaria. This study was conducted to evaluate the antimalarial potential of clindamycin in combination with dihydroartemisinin in continuously cultured and in freshly isolated Plasmodium falciparum parasites, measuring the inhibition of Plasmodium falciparum histidine-rich protein II synthesis. Interaction analysis revealed a synergistic or additive mode of interaction at various concentration ratios in all continuously cultured parasites at the 50% effective concentration (EC50) level.

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Baniecki, Mary Lynn, Dyann F. Wirth, and Jon Clardy. "High-Throughput Plasmodium falciparum Growth Assay for Malaria Drug Discovery." Antimicrobial Agents and Chemotherapy 51, no. 2 (2006): 716–23. http://dx.doi.org/10.1128/aac.01144-06.

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ABSTRACT New therapeutic agents for the treatment of malaria, the world's most deadly parasitic disease, are urgently needed. Malaria afflicts 300 to 500 million people and results in 1 to 2 million deaths annually, and more than 85% of all malaria-related mortality involves young children and pregnant women in sub-Saharan Africa. The emergence of multidrug-resistant parasites, especially in Plasmodium falciparum, has eroded the efficacy of almost all currently available therapeutic agents. The discovery of new drugs, including drugs with novel cellular targets, could be accelerated with a who

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Majeed, Muhammad Zafar, Muhammad Shahbaz Hussain, and Faiza Sarwar. "PREVALENCE OF HUMAN MALARIA." Professional Medical Journal 23, no. 06 (2016): 655–59. http://dx.doi.org/10.29309/tpmj/2016.23.06.1602.

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Malaria is one of the devastating diseases worldwide. More than 3 billion peoplelive under the threat of malaria in endemic countries and kills more than one million each year.Malaria leads to multiple hematological (thrombocytopenia) and other abnormalities like renalsystem, nervous system with increased morbidity and mortality. Aim: The present study wasconducted to determine the prevalence of human malaria, its correlation with thrombocytopeniaand treatment in patients of District Rahim Yar Khan. Materials and Methods: A total of 200patients including 140 males and 60 females were the part

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Drinkwater, Nyssa, Komagal Kannan Sivaraman, Rebecca S. Bamert, et al. "Structure and substrate fingerprint of aminopeptidase P from Plasmodium falciparum." Biochemical Journal 473, no. 19 (2016): 3189–204. http://dx.doi.org/10.1042/bcj20160550.

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Malaria is one of the world's most prevalent parasitic diseases, with over 200 million cases annually. Alarmingly, the spread of drug-resistant parasites threatens the effectiveness of current antimalarials and has made the development of novel therapeutic strategies a global health priority. Malaria parasites have a complicated lifecycle, involving an asymptomatic ‘liver stage’ and a symptomatic ‘blood stage’. During the blood stage, the parasites utilise a proteolytic cascade to digest host hemoglobin, which produces free amino acids absolutely necessary for parasite growth and reproduction.

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Tanaka, Takeshi Q., Edgar Deu, Alvaro Molina-Cruz, et al. "Plasmodium Dipeptidyl Aminopeptidases as Malaria Transmission-Blocking Drug Targets." Antimicrobial Agents and Chemotherapy 57, no. 10 (2013): 4645–52. http://dx.doi.org/10.1128/aac.02495-12.

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ABSTRACTThePlasmodium falciparumandP. bergheigenomes each contain three dipeptidyl aminopeptidase (dpap) homologs.dpap1and -3 are critical for asexual growth, but the role ofdpap2, the gametocyte-specific homolog, has not been tested. If DPAPs are essential for transmission as well as asexual growth, then a DPAP inhibitor could be used for treatment and to block transmission. To directly analyze the role of DPAP2, adpap2-minusP. berghei(Pbdpap2Δ) line was generated. ThePbdpap2Δ parasites grew normally, differentiated into gametocytes, and generated sporozoites that were infectious to mice when

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Oyakhirome, Sunny, Saadou Issifou, Peter Pongratz, et al. "Randomized Controlled Trial of Fosmidomycin-Clindamycin versus Sulfadoxine-Pyrimethamine in the Treatment of Plasmodium falciparum Malaria." Antimicrobial Agents and Chemotherapy 51, no. 5 (2007): 1869–71. http://dx.doi.org/10.1128/aac.01448-06.

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ABSTRACT Fosmidomycin-clindamycin therapy given every 12 h for 3 days was compared with a standard single oral dose of sulfadoxine-pyrimethamine. The two treatments showed comparably good tolerabilities and had an identical high degree of efficacy of 94% in a randomized trial carried out with 105 Gabonese children aged 3 to 14 years with uncomplicated malaria. These antimalarials merit further clinical exploration.

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Murithi, James M., Cécile Pascal, Jade Bath, et al. "The antimalarial MMV688533 provides potential for single-dose cures with a high barrier to Plasmodium falciparum parasite resistance." Science Translational Medicine 13, no. 603 (2021): eabg6013. http://dx.doi.org/10.1126/scitranslmed.abg6013.

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The emergence and spread of Plasmodium falciparum resistance to first-line antimalarials creates an imperative to identify and develop potent preclinical candidates with distinct modes of action. Here, we report the identification of MMV688533, an acylguanidine that was developed following a whole-cell screen with compounds known to hit high-value targets in human cells. MMV688533 displays fast parasite clearance in vitro and is not cross-resistant with known antimalarials. In a P. falciparum NSG mouse model, MMV688533 displays a long-lasting pharmacokinetic profile and excellent safety. Selec

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Antia-Obong, O. E., A. A. A. Alaribe, M. U. Young, A. Bassy, and B. V. Etim. "Chloroquine-Resistant Plasmodium Falciparum Among Children in Calabar, South Eastern Nigeria." Tropical Doctor 27, no. 3 (1997): 146–49. http://dx.doi.org/10.1177/004947559702700309.

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Sixty-nine children aged between 6 and 60 months with parasitologically proven Plasmodium falciparum malaria were treated with chloroquine (2.5 mg/kg) in the Children's Emergency Room of the University of Calabar Teaching Hospital (UCTH) in 1993. Thirty subjects (mean age 27.8 months) and 39 (mean age 29.5 months) received chloroquine phosphate suppository (Pharma Deko) and chloroquine sulphate syrup (May & Baker), respectively. The World Health Organization (WHO) 14-day in vivo field test was used in evaluating the response to treatment. In both treatment groups the responses were similar

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Tang, Yu-Qing, Qian Ye, He Huang, and Wei-Yi Zheng. "An Overview of Available Antimalarials: Discovery, Mode of Action and Drug Resistance." Current Molecular Medicine 20, no. 8 (2020): 583–92. http://dx.doi.org/10.2174/1566524020666200207123253.

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: Malaria is one of the three most deadly infectious diseases in the world and seriously endangers human health and life. To reduce the public health burden of this disease, scientists have focused on the discovery and development of effective antimalarial drugs, from quinine and chloroquine to antifolates and artemisinin and its derivatives, which all play a profound role in the treatment of malaria. However, drugresistant strains of Plasmodium falciparum have emerged due to frequent use of antimalarials and have become increasingly resistant to existing antimalarial drugs, causing disastrous

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Borrmann, Steffen, Ayola A. Adegnika, Michel A. Missinou, et al. "Short-Course Artesunate Treatment of Uncomplicated Plasmodium falciparum Malaria in Gabon." Antimicrobial Agents and Chemotherapy 47, no. 3 (2003): 901–4. http://dx.doi.org/10.1128/aac.47.3.901-904.2003.

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ABSTRACT Artesunate is one of the most important antimalarial agents available, since it is effective against parasites that have developed resistance to conventional antimalarials in sub-Saharan Africa. Antimalarial combination chemotherapies with artesunate (4 mg/kg of body weight once daily for 3 days) as one partner have been proposed. However, the efficacy of a 3-day course of artesunate alone has never been evaluated in individuals in Africa (which has 90% of the worldwide malaria burden) living in regions of hyperendemicity, where a considerable degree of immunity might substantially en

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Frausin, Gina, Renata Braga Souza Lima, Ari de Freitas Hidalgo, Paul Maas, and Adrian Martin Pohlit. "Plants of the Annonaceae traditionally used as antimalarials: a review." Revista Brasileira de Fruticultura 36, spe1 (2014): 315–37. http://dx.doi.org/10.1590/s0100-29452014000500038.

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Species of the Annonaceae family are used all over the tropics in traditional medicine in tropical regions for the treatment of malaria and other illnesses. Phytochemical studies of this family have revealed chemical components which could offer new alternatives for the treatment and control of malaria. Searches in scientific reference sites (SciFinder Scholar, Scielo, PubMed, ScienceDirect and ISI Web of Science) and a bibliographic literature search for species of Annonaceae used traditionally to treat malaria and fever were carried out. This family contains 2,100 species in 123 genera. We e

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Hoppe, Heinrich C., Donelly A. van Schalkwyk, Ursula I. M. Wiehart, Sandra A. Meredith, Joanne Egan, and Brandon W. Weber. "Antimalarial Quinolines and Artemisinin Inhibit Endocytosis in Plasmodium falciparum." Antimicrobial Agents and Chemotherapy 48, no. 7 (2004): 2370–78. http://dx.doi.org/10.1128/aac.48.7.2370-2378.2004.

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ABSTRACT Endocytosis is a fundamental process of eukaryotic cells and fulfills numerous functions, most notably, that of macromolecular nutrient uptake. Malaria parasites invade red blood cells and during their intracellular development endocytose large amounts of host cytoplasm for digestion in a specialized lysosomal compartment, the food vacuole. In the present study we have examined the effects of artemisinin and the quinoline drugs chloroquine and mefloquine on endocytosis in Plasmodium falciparum. By using novel assays we found that mefloquine and artemisinin inhibit endocytosis of macro

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Oboh, Mary Aigbiremo, Daouda Ndiaye, Hiasindh Ashmi Antony, et al. "Status of Artemisinin Resistance in Malaria Parasite Plasmodium falciparum from Molecular Analyses of the Kelch13 Gene in Southwestern Nigeria." BioMed Research International 2018 (October 3, 2018): 1–5. http://dx.doi.org/10.1155/2018/2305062.

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Evolution and spread of malaria parasite Plasmodium falciparum capable of evading antimalarials are the prime concern to malaria control. The currently effective drug, artemisinin (ART), is under threat due to detection of ART-resistant P. falciparum parasites in the Southeast Asian countries. It has been shown that amino acid (AA) mutations at the P. falciparum Kelch13 (Pfk13) gene provide resistance to ART. Nigeria, a part of the Sub-Saharan Africa, is highly endemic to malaria, contributing quite significantly to malaria, and resistance to chloroquine (CQ) and sulfadoxine-pyrimethamine (SP)

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van Pelt-Koops, J. C., H. E. Pett, W. Graumans, et al. "The Spiroindolone Drug Candidate NITD609 Potently Inhibits Gametocytogenesis and Blocks Plasmodium falciparum Transmission to Anopheles Mosquito Vector." Antimicrobial Agents and Chemotherapy 56, no. 7 (2012): 3544–48. http://dx.doi.org/10.1128/aac.06377-11.

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ABSTRACTThe global malaria agenda has undergone a reorientation from control of clinical cases to entirely eradicating malaria. For that purpose, a key objective is blocking transmission of malaria parasites from humans to mosquito vectors. The new antimalarial drug candidate NITD609 was evaluated for its transmission-reducing potential and compared to a few established antimalarials (lumefantrine, artemether, primaquine), using a suite ofin vitroassays. By the use of a microscopic readout, NITD609 was found to inhibit the early and late development ofPlasmodium falciparumgametocytesin vitroin

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McCarthy, James S., Louise Marquart, Silvana Sekuloski, et al. "Linking Murine and Human Plasmodium falciparum Challenge Models in a Translational Path for Antimalarial Drug Development." Antimicrobial Agents and Chemotherapy 60, no. 6 (2016): 3669–75. http://dx.doi.org/10.1128/aac.02883-15.

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Effective progression of candidate antimalarials is dependent on optimal dosing in clinical studies, which is determined by a sound understanding of pharmacokinetics and pharmacodynamics (PK/PD). Recently, two important translational models for antimalarials have been developed: the NOD/SCID/IL2Rγ−/−(NSG) model, whereby mice are engrafted with noninfected andPlasmodium falciparum-infected human erythrocytes, and the induced blood-stage malaria (IBSM) model in human volunteers. The antimalarial mefloquine was used to directly measure the PK/PD in both models, which were compared to previously p

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Ducati, Rodrigo G., Hilda A. Namanja-Magliano, Rajesh K. Harijan, et al. "Genetic resistance to purine nucleoside phosphorylase inhibition in Plasmodium falciparum." Proceedings of the National Academy of Sciences 115, no. 9 (2018): 2114–19. http://dx.doi.org/10.1073/pnas.1525670115.

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Plasmodium falciparum causes the most lethal form of human malaria and is a global health concern. The parasite responds to antimalarial therapies by developing drug resistance. The continuous development of new antimalarials with novel mechanisms of action is a priority for drug combination therapies. The use of transition-state analog inhibitors to block essential steps in purine salvage has been proposed as a new antimalarial approach. Mutations that reduce transition-state analog binding are also expected to reduce the essential catalytic function of the target. We have previously reported

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Ling, Liqin, Maruthi Mulaka, Justin Munro, et al. "Genetic ablation of the mitoribosome in the malaria parasite Plasmodium falciparum sensitizes it to antimalarials that target mitochondrial functions." Journal of Biological Chemistry 295, no. 21 (2020): 7235–48. http://dx.doi.org/10.1074/jbc.ra120.012646.

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The mitochondrion of malaria parasites contains several clinically validated drug targets. Within Plasmodium spp., the causative agents of malaria, the mitochondrial DNA (mtDNA) is only 6 kb long, being the smallest mitochondrial genome among all eukaryotes. The mtDNA encodes only three proteins of the mitochondrial electron transport chain and ∼27 small, fragmented rRNA genes having lengths of 22–195 nucleotides. The rRNA fragments are thought to form a mitochondrial ribosome (mitoribosome), together with ribosomal proteins imported from the cytosol. The mitoribosome of Plasmodium falciparum

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Gadalla, Nahla B., Ishag Adam, Salah-Eldin Elzaki, et al. "Increasedpfmdr1Copy Number and Sequence Polymorphisms in Plasmodium falciparum Isolates from Sudanese Malaria Patients Treated with Artemether-Lumefantrine." Antimicrobial Agents and Chemotherapy 55, no. 11 (2011): 5408–11. http://dx.doi.org/10.1128/aac.05102-11.

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ABSTRACTMolecular markers for surveillance ofPlasmodium falciparumresistance to current antimalarials are sorely needed. A 28-day efficacy study of artemether-lumefantrine in eastern Sudan identified 5 treatment failures among 100 evaluable patients; 9 further individuals were parasite positive by PCR during follow-up. Polymorphisms inpfatpase6andpfmdr1were evaluated by DNA sequencing. One individual carried parasites with a novelpfmdr1polymorphism (F1044L).pfmdr1gene amplification in parasites prior to treatment occurred in three individuals who had recurrent infection during follow-up.

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Songsungthong, Warangkhana, Supasak Kulawonganunchai, Alisa Wilantho, et al. "The Plasmodium berghei RC strain is highly diverged and harbors putatively novel drug resistance variants." PeerJ 5 (October 5, 2017): e3766. http://dx.doi.org/10.7717/peerj.3766.

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Background The current first line drugs for treating uncomplicated malaria are artemisinin (ART) combination therapies. However, Plasmodium falciparum parasites resistant to ART and partner drugs are spreading, which threatens malaria control efforts. Rodent malaria species are useful models for understanding antimalarial resistance, in particular genetic variants responsible for cross resistance to different compounds. Methods The Plasmodium berghei RC strain (PbRC) is described as resistant to different antimalarials, including chloroquine (CQ) and ART. In an attempt to identify the genetic

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Biddau, Marco, and Lilach Sheiner. "Targeting the apicoplast in malaria." Biochemical Society Transactions 47, no. 4 (2019): 973–83. http://dx.doi.org/10.1042/bst20170563.

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Abstract Malaria continues to be one of the leading causes of human mortality in the world, and the therapies available are insufficient for eradication. Severe malaria is caused by the apicomplexan parasite Plasmodium falciparum. Apicomplexan parasites, including the Plasmodium spp., are descendants of photosynthetic algae, and therefore they possess an essential plastid organelle, named the apicoplast. Since humans and animals have no plastids, the apicoplast is an attractive target for drug development. Indeed, after its discovery, the apicoplast was found to host the target pathways of som

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Duez, Julien, John P. Holleran, Papa Alioune Ndour, et al. "Splenic Retention of Plasmodium falciparum Gametocytes To Block the Transmission of Malaria." Antimicrobial Agents and Chemotherapy 59, no. 7 (2015): 4206–14. http://dx.doi.org/10.1128/aac.05030-14.

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ABSTRACTPlasmodium falciparumis transmitted from humans toAnophelesmosquito vectors via the sexual erythrocytic forms termed gametocytes. Erythrocyte filtration through microsphere layers (microsphiltration) had shown that circulating gametocytes are deformable. Compounds reducing gametocyte deformability would induce their splenic clearance, thus removing them from the blood circulation and blocking malaria transmission. The hand-made, single-sample prototype for microsphiltration was miniaturized to a 96-well microtiter plate format, and gametocyte retention in the microsphere filters was qu

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Rodrigues Henriques, Juan Ricardo, and Neira Gamboa de Domínguez. "Modulation of the oxidative stress in malaria infection by clotrimazole." Brazilian Journal of Pharmaceutical Sciences 48, no. 3 (2012): 519–28. http://dx.doi.org/10.1590/s1984-82502012000300019.

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Antimycotic clotrimazole (CTZ) has demonstrated remarkable activity against Plasmodium falciparum in vitro and in vivo. Hemoglobin degradation by Plasmodium parasites makes amino acids available for protein synthesis, inducing oxidative stress in infected cells and producing free heme. These events represent biochemical targets for potential antimalarials. In this study, we have tested the ability of CTZ to modify the oxidative status in Plasmodium berghei-infected erythrocytes. After hemolysis, activities of superoxide dismutase (SOD), catalase (CAT), glutathione cycle and NADPH+H+-producing

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Locher, Christopher P., Peter C. Ruben, Jiri Gut, and Philip J. Rosenthal. "5HT1A Serotonin Receptor Agonists Inhibit Plasmodium falciparum by Blocking a Membrane Channel." Antimicrobial Agents and Chemotherapy 47, no. 12 (2003): 3806–9. http://dx.doi.org/10.1128/aac.47.12.3806-3809.2003.

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ABSTRACT Toidentify new leads for the treatment of Plasmodium falciparum malaria, we screened a panel of serotonin (5-hydroxytryptamine [5HT]) receptor agonists and antagonists and determined their effects on parasite growth. The 5HT1A receptor agonists 8-hydroxy-N-(di-n-propyl)-aminotetralin (8-OH-DPAT), 2,5-dimethoxy-4-iodoamphetamine, and 2,5-dimethoxy-4-bromophenylethylamine inhibited the growth of P. falciparum in vitro (50% inhibitory concentrations, 0.4, 0.7, and 1.5 μM, respectively). In further characterizing the antiparasitic effects of 8-OH-DPAT, we found that this serotonin recepto

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Khim, Nimol, Christiane Bouchier, Marie-Thérèse Ekala, et al. "Countrywide Survey Shows Very High Prevalence of Plasmodium falciparum Multilocus Resistance Genotypes in Cambodia." Antimicrobial Agents and Chemotherapy 49, no. 8 (2005): 3147–52. http://dx.doi.org/10.1128/aac.49.8.3147-3152.2005.

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ABSTRACT Cambodia is located in an area of resistance to multiple antimalarials and has been the first country to implement the systematic use of an artesunate-mefloquine combination as first-line treatment for Plasmodium falciparum malaria. Little is known, however, about the prevalence of resistance mutations within the natural parasite populations, impeding rational drug policy in this context. Using direct sequencing of PCR products, we have analyzed sequence polymorphism of the dihydrofolate reductase-thymidylate synthase, dihydropteroate synthetase, and multidrug resistance 1 genes in a

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Heppner, DG, PE Hallaway, GJ Kontoghiorghes, and JW Eaton. "Antimalarial properties of orally active iron chelators." Blood 72, no. 1 (1988): 358–61. http://dx.doi.org/10.1182/blood.v72.1.358.358.

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Abstract The appearance of widespread multiple drug resistance in human malaria has intensified the search for new antimalarial compounds. Metal chelators, especially those with high affinity for iron, represent one presently unexploited class of antimalarials. Unfortunately the use of previously identified chelators as antimalarials has been precluded by their toxicity and, in the case of desferrioxamine, the necessity for parenteral administration. The investigators now report that a new class of orally active iron chelators, namely the derivatives of alpha- ketohydroxypyridines (KHPs), are

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Heppner, DG, PE Hallaway, GJ Kontoghiorghes, and JW Eaton. "Antimalarial properties of orally active iron chelators." Blood 72, no. 1 (1988): 358–61. http://dx.doi.org/10.1182/blood.v72.1.358.bloodjournal721358.

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The appearance of widespread multiple drug resistance in human malaria has intensified the search for new antimalarial compounds. Metal chelators, especially those with high affinity for iron, represent one presently unexploited class of antimalarials. Unfortunately the use of previously identified chelators as antimalarials has been precluded by their toxicity and, in the case of desferrioxamine, the necessity for parenteral administration. The investigators now report that a new class of orally active iron chelators, namely the derivatives of alpha- ketohydroxypyridines (KHPs), are potent an

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Sharma, Shilpi, Shailendra Kumar Sharma, Rahul Modak, Krishanpal Karmodiya, Namita Surolia, and Avadhesha Surolia. "Mass Spectrometry-Based Systems Approach for Identification of Inhibitors of Plasmodium falciparum Fatty Acid Synthase." Antimicrobial Agents and Chemotherapy 51, no. 7 (2007): 2552–58. http://dx.doi.org/10.1128/aac.00124-07.

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ABSTRACT The emergence of strains of Plasmodium falciparum resistant to the commonly used antimalarials warrants the development of new antimalarial agents. The discovery of type II fatty acid synthase (FAS) in Plasmodium distinct from the FAS in its human host (type I FAS) opened up new avenues for the development of novel antimalarials. The process of fatty acid synthesis takes place by iterative elongation of butyryl-acyl carrier protein (butyryl-ACP) by two carbon units, with the successive action of four enzymes constituting the elongation module of FAS until the desired acyl length is ob

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SEGURADO, Aluisio Augusto Cotrim, Silvia Maria DI SANTI, and Mario SHIROMA. "In vivo and in vitro Plasmodium falciparum Resistance to Chloroquine, Amodiaquine and Quinine in the Brazilian Amazon." Revista do Instituto de Medicina Tropical de São Paulo 39, no. 2 (1997): 85–90. http://dx.doi.org/10.1590/s0036-46651997000200004.

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In order to study the chemoresistance of Plasmodium falciparum to commonly used antimalarial drugs in Brazil the authors have studied ten patients with falciparum malaria, acquired in the Brazilian Amazon region. Patients were submitted to in vivo study of drug sensitivity, after chemotherapy with either 4-aminoquinolines (chloroquine or amodiaquine) or quinine. Adequate drug absorption was confirmed by standard urine excretion tests for antimalarials. Eight patients could be followed up to 28 days. Among these in vivo resistance (R I and R II responses) was seen in all patients who received 4

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Choudhary, Amit, Manish Sinha, Arti Devi, Shammy Jindal, and Kamya Goyal. "A Review on Antimalarial 1,2,4-Trioxane Derivatives." Journal of Drug Delivery and Therapeutics 10, no. 4-s (2020): 240–53. http://dx.doi.org/10.22270/jddt.v10i4-s.4268.

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Malaria in recent years becomes a major health hitch globally due to the surfacing of multidrug-resistant strains of Plasmodium falciparum parasite. In recent times, artemisinin (ART)-based drugs and combination therapies become the drugs of preference for the treatment and prophylaxis of resistant P. falciparum malaria. Endoperoxide compounds natural, semi-synthetic or synthetic signifying a massive number of antimalarial agents which possess a wide structural miscellany with needed antimalarial effectiveness against resistant P. falciparum malaria. The 1,2,4-trioxane ring system deficient th

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Crandall, Ian, Jeffrey Charuk, and Kevin C. Kain. "Nonylphenolethoxylates as Malarial Chloroquine Resistance Reversal Agents." Antimicrobial Agents and Chemotherapy 44, no. 9 (2000): 2431–34. http://dx.doi.org/10.1128/aac.44.9.2431-2434.2000.

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ABSTRACT Malaria-associated morbidity and mortality are increasing because of widespread resistance to one of the safest and least expensive antimalarials, chloroquine. The availability of an inexpensive agent that is capable of reversing chloroquine resistance would have a major impact on malaria treatment worldwide. The interaction of nonylphenolethoxylates (NPEs, commercially available synthetic surfactants) with drug-resistant Plasmodium falciparum was examined to determine if NPEs inhibited the growth of the parasites and if NPEs could sensitize resistant parasites to chloroquine. NPEs in

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Chhim, Srean, Patrice Piola, Tambri Housen, Vincent Herbreteau, and Bunkea Tol. "Malaria in Cambodia: A Retrospective Analysis of a Changing Epidemiology 2006–2019." International Journal of Environmental Research and Public Health 18, no. 4 (2021): 1960. http://dx.doi.org/10.3390/ijerph18041960.

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Background: In Cambodia, malaria persists with changing epidemiology and resistance to antimalarials. This study aimed to describe how malaria has evolved spatially from 2006 to 2019 in Cambodia. Methods: We undertook a secondary analysis of existing malaria data from all government healthcare facilities in Cambodia. The epidemiology of malaria was described by sex, age, seasonality, and species. Spatial clusters at the district level were identified with a Poisson model. Results: Overall, incidence decreased from 7.4 cases/1000 population in 2006 to 1.9 in 2019. The decrease has been drastic

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Parkinson, Christopher J., Geoffrey W. Birrell, Marina Chavchich, et al. "Development of pyridyl thiosemicarbazones as highly potent agents for the treatment of malaria after oral administration." Journal of Antimicrobial Chemotherapy 74, no. 10 (2019): 2965–73. http://dx.doi.org/10.1093/jac/dkz290.

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AbstractObjectivesDrug resistance exists to all current and investigational antimalarial drug classes. Consequently, we have set out to develop chemically and mechanistically discrete antimalarials. Here we report on the development of thiosemicarbazone (TSC) antimalarials, with TSC3 as the most advanced lead.MethodsThiosemicarbazones were generated through simple condensation reactions of thiosemicarbazides and ketones. TSC3 was selected and tested for in vitro antimalarial activities against MDR Plasmodium falciparum lines using the [3H]hypoxanthine growth assay, in vitro cytotoxicity agains

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Morozova, L. F., A. V. Kondrashin, E. V. Stepanova, et al. "In vivo effectiveness of the inhibitors of telomerase against malaria parasites." Infekcionnye bolezni 18, no. 4 (2020): 127–32. http://dx.doi.org/10.20953/1729-9225-2020-4-127-132.

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One of the most dangerous causative agents of malaria is Plasmodium falciparum, transmitted by various Anopheline mosquitoes. Due to widespread drug resistance to practically all antimalarials, novel and effective drugs to manage this important disease are urgently required. In this study we evaluated the antimalarial activity of a series of 14 compounds from the inhibitors of the telomerase group. For in vivo studies we used P. berghei strain NK 65 in white unbread mice. The most antimalarial activity was shown by Imatinib, Phosphazide and Imetelstat. We found that Imatinib is the most potent

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Akompong, Thomas, Saliha Eksi, Kim Williamson, and Kasturi Haldar. "Gametocytocidal Activity and Synergistic Interactions of Riboflavin with Standard Antimalarial Drugs against Growth of Plasmodium falciparum In Vitro." Antimicrobial Agents and Chemotherapy 44, no. 11 (2000): 3107–11. http://dx.doi.org/10.1128/aac.44.11.3107-3111.2000.

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ABSTRACT Our previous studies have shown that riboflavin has activity against Plasmodium falciparum asexual-stage parasites in vitro. In the present study we examine the gametocytocidal activity of riboflavin and the interaction of riboflavin with some commonly used antimalarial drugs against the asexual forms of P. falciparum in vitro. The addition of riboflavin to P. falciparum cultures killed gametocytes at all stages, even those at late stages (III to V), which are not affected by many of the commonly used antimalarials. Combinations of riboflavin with mefloquine, pyrimethamine, and quinin

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Peters, W. "The problem of drug resistance in malaria." Parasitology 90, no. 4 (1985): 705–15. http://dx.doi.org/10.1017/s003118200005232x.

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The resistance in human malaria is mainly of practical importance in relation to Plasmodium falciparum. Strains resistant not only to chloroquine but also to dihydrofolate reductase inhibitors, and even to potentiating combinations of these with sulphonamides or sulphones, are appearing in an ever increasing geographical area which now includes tropical Africa and India. Few new drugs are available or foreseen for the near future, mefloquine and artemisinine being the leading contenders. It is vital that all measures possible should be taken to protect such new compounds, their deployment in t

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Lucumi, Edinson, Claire Darling, Hyunil Jo, et al. "Discovery of Potent Small-Molecule Inhibitors of Multidrug-Resistant Plasmodium falciparum Using a Novel Miniaturized High-Throughput Luciferase-Based Assay." Antimicrobial Agents and Chemotherapy 54, no. 9 (2010): 3597–604. http://dx.doi.org/10.1128/aac.00431-10.

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ABSTRACT Malaria is a global health problem that causes significant mortality and morbidity, with more than 1 million deaths per year caused by Plasmodium falciparum. Most antimalarial drugs face decreased efficacy due to the emergence of resistant parasites, which necessitates the discovery of new drugs. To identify new antimalarials, we developed an automated 384-well plate screening assay using P. falciparum parasites that stably express cytoplasmic firefly luciferase. After initial optimization, we tested two different types of compound libraries: known bioactive collections (Library of Ph

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N., Raghu Murthy, and Seema Rai. "Analysis of clinical profile and prescription pattern of malaria in a tertiary care hospital in Karnataka, India." International Journal of Basic & Clinical Pharmacology 8, no. 8 (2019): 1744. http://dx.doi.org/10.18203/2319-2003.ijbcp20193136.

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Background: Malaria is one of the leading causes of morbidity and mortality in developing countries like India. Plasmodium falciparum and Plasmodium vivax are the commonest species implicated for an increased incidence of malaria in India. The pattern of disease, signs, and symptoms vary from place to place, region to region due to demographic variations. The current study was undertaken to study the differences in the clinical profile of malaria, particularly signs and symptoms, complications and response to treatment in malaria.Methods: A retrospective, single center, surveillance study was

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