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Dihydroartemisinin

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https://www.readbyqxmd.com/read/29039344/mini-review-analysis-of-artemether-and-dihydroartemisinin-by-high-performance-high-liquid-chromatography-in-biological-fluids-issues-and-solutions
#1
Shabana Ali, Nusrat Jafery, Kulsoom Farhat, Akbar Waheed
Artemether-Lumefantrine is the most widely recommended antimalarial combination used to treat millions of patients suffering from malaria. Artemether undergoes rapid metabolism and gets converted to its active metabolite dihydroartemisisn. Drug analysis is a vital aspect to evaluate drugs in research. There are a number of methods available for the determination of artemether in biological fluids. These methods include HPLC based UV detection, GS-MS, HPLC-ECD and HPLC-MS/MS. This article reviews different methods for the determination of artemether in the biological fluids...
July 2017: Pakistan Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29033794/dihydroartemisinin-exerts-anti-tumor-activity-by-inducing-mitochondrion-and-endoplasmic-reticulum-apoptosis-and-autophagic-cell-death-in-human-glioblastoma-cells
#2
Chengbin Qu, Jun Ma, Xiaobai Liu, Yixue Xue, Jian Zheng, Libo Liu, Jing Liu, Zhen Li, Lei Zhang, Yunhui Liu
Glioblastoma (GBM) is the most advanced and aggressive form of gliomas. Dihydroartemisinin (DHA) has been shown to exhibit anti-tumor activity in various cancer cells. However, the effect and molecular mechanisms underlying its anti-tumor activity in human GBM cells remain to be elucidated. Our results proved that DHA treatment significantly reduced cell viability in a dose- and time-dependent manner by CCK-8 assay. Further investigation identified that the cell viability was rescued by pretreatment either with Z-VAD-FMK, 3-methyladenine (3-MA) or in combination...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/29027504/pharmacokinetic-considerations-for-use-of-artemisinin-based-combination-therapies-against-falciparum-malaria-in-different-ethnic-populations
#3
Sri Riyati Sugiarto, Timothy M E Davis, Sam Salman
Artemisinin-based combination therapy (ACT) is used extensively as first-line treatment for uncomplicated falciparum malaria. There has been no rigorous assessment of the potential for racial/ethnic differences in the pharmacokinetic properties of ACTs that might influence their pharmacokinetic properties. Areas covered: A comprehensive literature search was performed that identified 72 publications in which the geographical origin of the patients could be ascertained and the key pharmacokinetic parameters maximum drug concentration (Cmax), area under the plasma concentration-time curve (AUC) and elimination half-life (t½β) were available for one or more of the five WHO-recommended ACTs (artemether-lumefantrine, artesunate-amodiaquine, artesunate-mefloquine, dihydroartemisinin-piperaquine and artesunate-sulfadoxine-pyrimethamine)...
October 13, 2017: Expert Opinion on Drug Metabolism & Toxicology
https://www.readbyqxmd.com/read/28993326/a-dynamic-stress-model-explains-the-delayed-drug-effect-in-artemisinin-treatment-of-plasmodium-falciparum
#4
Pengxing Cao, Nectarios Klonis, Sophie Zaloumis, Con Dogovski, Stanley C Xie, Sompob Saralamba, Lisa J White, Freya J I Fowkes, Leann Tilley, Julie A Simpson, James M McCaw
Artemisinin resistance constitutes a major threat to the continued success of control programs for malaria, particularly in light of developing resistance to partner drugs. Improving our understanding of how artemisinin-based drugs act and how resistance manifests is essential for the optimisation of dosing regimens and the development of strategies to prolong the lifespan of current first-line treatment options. Recent short drug-pulse in vitro experiments have shown that the parasite killing rate depends not only on drug concentration but also the exposure time, challenging the standard pharmacokinetic-pharmacodynamic(PK-PD) paradigm in which the killing rate depends only on drug concentration...
October 9, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28974549/modulation-of-navitoclax-sensitivity-by-dihydroartemisinin-mediated-mcl-1-repression-in-bcr-abl-b-lineage-acute-lymphoblastic-leukemia
#5
Amit Budhraja, Meghan E Turnis, Michelle L Churchman, Anisha Kothari, Xue Yang, Haiyan Xu, Ewa Kaminska, John C Panetta, David Finkelstein, Charles G Mullighan, Joseph T Opferman
PURPOSE: BCR-ABL+ B-ALL leukemic cells are highly dependent on the expression of endogenous anti-apoptotic MCL-1 to promote viability and are resistant to BH3-mimetic agents such as navitoclax (ABT-263) that targets BCL-2, BCL-XL, and BCL-W. However, the survival of most normal blood cells and other cell types are also dependent on Mcl-1. Despite the requirement for MCL-1 in these cell types, initial reports of MCL-1-specific BH3-mimetics have not described any overt toxicities associated with single-agent use, but these agents are still early in clinical development...
October 3, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/28971859/sustained-ex-vivo-susceptibility-of-plasmodium-falciparum-to-artemisinin-derivatives-but-increasing-tolerance-to-act-partner-quinolines-in-the-gambia
#6
Alfred Amambua-Ngwa, Joseph Okebe, Haddijatou Mbye, Sukai Ceesay, Fatima El-Fatouri, Fatou Joof, Nyang Haddy, Janha Ramatoulie, Muna Affara, Abdullahi Ahmad, Olimatou Kolly, Davis Nwakanma, Umberto D'Alessandro
Antimalarial interventions have yielded significant decline in malaria prevalence in The Gambia, where Artemether-Lumefantrine (AL) has been used as first line antimalarial for a decade. Clinical Plasmodium falciparum isolates collected from 2012 to 2015 were analysed ex vivo for antimalarial susceptibility and genotyped for drug resistance markers (pfcrt K76T, pfmdr1-86-184 and 1246 and pfk13) and microsatellite variation. Additionally, allele frequencies of SNPs from other drug resistance-associated genes were compared from genomic sequence datasets from 2008 (n=79) and 2014 (n=168)...
October 2, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28968782/impact-of-intermittent-preventive-treatment-during-pregnancy-on-plasmodium-falciparum-drug-resistance-mediating-polymorphisms-in-uganda
#7
Melissa D Conrad, Daniel Mota, Marissa Foster, Stephen Tukwasibwe, Jennifer Legac, Patrick Tumwebaze, Meghan Whalen, Abel Kakuru, Patience Nayebare, Erika Wallender, Diane V Havlir, Prasanna Jagannathan, Liusheng Huang, Francesca Aweeka, Moses R Kamya, Grant Dorsey, Philip J Rosenthal
Background: In a recent trial of intermittent preventive treatment in pregnancy (IPTp) in Uganda, dihydroartemisinin-piperaquine (DP) was superior to sulfadoxine-pyrimethamine (SP) in preventing maternal and placental malaria. Methods: We compared genotypes using sequencing, fluorescent microsphere, and qPCR assays at loci associated with drug resistance in Plasmodium falciparum isolated from subjects receiving DP or SP. Results: Considering aminoquinoline resistance, DP was associated with increased prevalences of mutations at pfmdr1 N86Y, pfmdr1 Y184F, and pfcrt K76T compared to SP (64...
August 22, 2017: Journal of Infectious Diseases
https://www.readbyqxmd.com/read/28964258/measuring-ex-vivo-drug-susceptibility-in-plasmodium-vivax-isolates-from-cambodia
#8
Suwanna Chaorattanakawee, Chanthap Lon, Soklyda Chann, Kheang Heng Thay, Nareth Kong, Yom You, Siratchana Sundrakes, Chatchadaporn Thamnurak, Sorayut Chattrakarn, Chantida Praditpol, Kritsanai Yingyuen, Mariusz Wojnarski, Rekol Huy, Michele D Spring, Douglas S Walsh, Jaymin C Patel, Jessica Lin, Jonathan J Juliano, Charlotte A Lanteri, David L Saunders
BACKGROUND: While intensive Plasmodium falciparum multidrug resistance surveillance continues in Cambodia, relatively little is known about Plasmodium vivax drug resistance in Cambodia or elsewhere. To investigate P. vivax anti-malarial susceptibility in Cambodia, 76 fresh P. vivax isolates collected from Oddar Meanchey (northern Cambodia) in 2013-2015 were assessed for ex vivo drug susceptibility using the microscopy-based schizont maturation test (SMT) and a Plasmodium pan-species lactate dehydrogenase (pLDH) ELISA...
September 30, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28934730/dihydroartemisinin-and-curcumin-synergistically-induce-apoptosis-in-skov3-cells-via-upregulation-of-mir-124-targeting-midkine
#9
Jiaojiao Zhao, Yuchen Pan, Xiujun Li, Xuefang Zhang, Yaxian Xue, Tingting Wang, Shuli Zhao, Yayi Hou
BACKGROUND/AIM: Women with advanced ovarian carcinoma are less likely to receive platinum-based chemotherapy and surgery due to a greater risk of cytotoxicity and poorer outcomes. We attempted to improve a promising therapy against ovarian cancer by using a combination of dihydroartemisinin (DHA) and curcumin (Cur). METHODS: Human ovarian cancer SKOV3 cells were treated with DHA, Cur alone, or a combination of both. The viability of SKOV3 cells was measured by Cell Counting Kit-8 (CCK-8) and a colony formation assay...
September 21, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28934264/profiling-molecular-factors-associated-with-pyknosis-and-developmental-arrest-induced-by-an-opioid-receptor-antagonist-and-dihydroartemisinin-in-plasmodium-falciparum
#10
Hiroko Asahi, Shin-Ichi Inoue, Mamoru Niikura, Keisuke Kunigo, Yutaka Suzuki, Fumie Kobayashi, Fujiro Sendo
Malaria continues to be a devastating disease, largely caused by Plasmodium falciparum infection. We investigated the effects of opioid and cannabinoid receptor antagonists on the growth of intraerythrocytic P. falciparum. The delta opioid receptor antagonist 7-benzylidenenaltrexone (BNTX) and the cannabinoid receptor antagonists rimonaband and SR144528 caused growth arrest of the parasite. Notably BNTX and the established antimalarial drug dihydroartemisinin induced prominent pyknosis in parasite cells after a short period of incubation...
2017: PloS One
https://www.readbyqxmd.com/read/28931241/association-of-a-novel-mutation-in-the-plasmodium-falciparum-chloroquine-resistance-transporter-with-decreased-piperaquine-sensitivity
#11
Sonia Agrawal, Kara A Moser, Lindsay Morton, Michael P Cummings, Ankita Parihar, Ankit Dwivedi, Amol C Shetty, Elliott F Drabek, Christopher G Jacob, Philipp P Henrich, Christian M Parobek, Krisada Jongsakul, Rekol Huy, Michele D Spring, Charlotte A Lanteri, Suwanna Chaorattanakawee, Chanthap Lon, Mark M Fukuda, David L Saunders, David A Fidock, Jessica T Lin, Jonathan J Juliano, Christopher V Plowe, Joana C Silva, Shannon Takala-Harrison
Background: Amplified copy number in the plasmepsin II/III genes within Plasmodium falciparum has been associated with decreased sensitivity to piperaquine. To examine this association and test whether additional loci might also contribute, we performed a genome-wide association study of ex vivo P. falciparum susceptibility to piperaquine. Methods: Plasmodium falciparum DNA from 183 samples collected primarily from Cambodia was genotyped at 33716 genome-wide single nucleotide polymorphisms (SNPs)...
August 15, 2017: Journal of Infectious Diseases
https://www.readbyqxmd.com/read/28931236/a-molecular-assay-to-quantify-male-and-female-plasmodium-falciparum-gametocytes-results-from-2-randomized-controlled-trials-using-primaquine-for-gametocyte-clearance
#12
RANDOMIZED CONTROLLED TRIAL
Will Stone, Patrick Sawa, Kjerstin Lanke, Sanna Rijpma, Robin Oriango, Maureen Nyaurah, Paul Osodo, Victor Osoti, Almahamoudou Mahamar, Halimatou Diawara, Rob Woestenenk, Wouter Graumans, Marga van de Vegte-Bolmer, John Bradley, Ingrid Chen, Joelle Brown, Giulia Siciliano, Pietro Alano, Roly Gosling, Alassane Dicko, Chris Drakeley, Teun Bousema
Background: Single low-dose primaquine (PQ) reduces Plasmodium falciparum infectivity before it impacts gametocyte density. Here, we examined the effect of PQ on gametocyte sex ratio as a possible explanation for this early sterilizing effect. Methods: Quantitative reverse-transcription polymerase chain reaction assays were developed to quantify female gametocytes (targeting Pfs25 messenger RNA [mRNA]) and male gametocytes (targeting Pf3D7_1469900 mRNA) in 2 randomized trials in Kenya and Mali, comparing dihydroartemisinin-piperaquine (DP) alone to DP with PQ...
August 15, 2017: Journal of Infectious Diseases
https://www.readbyqxmd.com/read/28923866/changing-antimalarial-drug-sensitivities-in-uganda
#13
Stephanie A Rasmussen, Frida G Ceja, Melissa D Conrad, Patrick K Tumwebaze, Oswald Byaruhanga, Thomas Katairo, Samuel L Nsobya, Philip J Rosenthal, Roland A Cooper
Dihydroartemisinin-piperaquine (DP) has demonstrated excellent efficacy for the treatment and prevention of malaria in Uganda. However, resistance to both components of this regimen has emerged in Southeast Asia. The efficacy of artemether-lumefantrine, the first-line regimen to treat malaria in Uganda, has also been excellent, but continued pressure may select for parasites with decreased sensitivity to lumefantrine. To gain insight into current drug sensitivity patterns, ex vivo sensitivities were assessed and genotypes previously associated with altered drug sensitivity were characterized for 58 isolates collected in Tororo, Uganda from subjects presenting in 2016 with malaria from the community or as part of a clinical trial comparing DP chemoprevention regimens...
September 18, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28895080/population-pharmacokinetic-and-pharmacodynamic-modeling-of-artemisinin-resistance-in-southeast-asia
#14
Jesmin Lohy Das, Arjen M Dondorp, Francois Nosten, Aung Pyae Phyo, Warunee Hanpithakpong, Pascal Ringwald, Pharath Lim, Nicholas J White, Mats O Karlsson, Martin Bergstrand, Joel Tarning
Orally administered artemisinin-based combination therapy is the first-line treatment against uncomplicated P. falciparum malaria worldwide. However, the increasing prevalence of artemisinin resistance is threatening efforts to treat and eliminate malaria in Southeast Asia. This study aimed to characterize the exposure-response relationship of artesunate in patients with artemisinin sensitive and resistant malaria infections. Patients were recruited in Pailin, Cambodia (n = 39), and Wang Pha, Thailand (n = 40), and received either 2 mg/kg/day of artesunate mono-therapy for 7 consecutive days or 4 mg/kg/day of artesunate monotherapy for 3 consecutive days followed by mefloquine 15 and 10 mg/kg for 2 consecutive days...
September 11, 2017: AAPS Journal
https://www.readbyqxmd.com/read/28883394/a-thiol-probe-for-measuring-unfolded-protein-load-and-proteostasis-in-cells
#15
Moore Z Chen, Nagaraj S Moily, Jessica L Bridgford, Rebecca J Wood, Mona Radwan, Trevor A Smith, Zhegang Song, Ben Zhong Tang, Leann Tilley, Xiaohong Xu, Gavin E Reid, Mahmoud A Pouladi, Yuning Hong, Danny M Hatters
When proteostasis becomes unbalanced, unfolded proteins can accumulate and aggregate. Here we report that the dye, tetraphenylethene maleimide (TPE-MI) can be used to measure cellular unfolded protein load. TPE-MI fluorescence is activated upon labelling free cysteine thiols, normally buried in the core of globular proteins that are exposed upon unfolding. Crucially TPE-MI does not become fluorescent when conjugated to soluble glutathione. We find that TPE-MI fluorescence is enhanced upon reaction with cellular proteomes under conditions promoting accumulation of unfolded proteins...
September 7, 2017: Nature Communications
https://www.readbyqxmd.com/read/28854635/partner-drug-resistance-and-population-substructuring-of-artemisinin-resistant-plasmodium-falciparum-in-cambodia
#16
Christian M Parobek, Jonathan B Parr, Nicholas F Brazeau, Chanthap Lon, Suwanna Chaorattanakawee, Panita Gosi, Eric J Barnett, Lauren D Norris, Steven R Meshnick, Michele D Spring, Charlotte A Lanteri, Jeffrey A Bailey, David L Saunders, Jessica T Lin, Jonathan J Juliano
Plasmodium falciparum in western Cambodia has developed resistance to artemisinin and its partner drugs, causing frequent treatment failure. Understanding this evolution can inform the deployment of new therapies. We investigated the genetic architecture of 78 falciparum isolates using whole-genome sequencing, correlating results to in vivo and ex vivo drug resistance and exploring the relationship between population structure, demographic history, and partner drug resistance. Principle component analysis, network analysis and demographic inference identified a diverse central population with three clusters of clonally expanding parasite populations, each associated with specific K13 artemisinin resistance alleles and partner drug resistance profiles which were consistent with the sequential deployment of artemisinin combination therapies in the region...
June 1, 2017: Genome Biology and Evolution
https://www.readbyqxmd.com/read/28800035/the-anti-malarial-drug-artesunate-attenuates-cardiac-injury-in-a-rodent-model-of-myocardial-infarction
#17
Areeg I Khan, Amar Kapoor, Jianmin Che, Lukas Martin, Mara Rogazzo, Thomas Mercier, Laurent Decosterd, Massimo Collino, Christoph Thiemermann
Ischaemic heart disease remains the leading cause of morbidity and mortality in the Western world. Artesunate is the WHO-recommended drug of choice for complicated malaria (with organ failure). The administration of high doses of artesunate is safe in healthy volunteers (up to 8 mg/kg i.v) and patients with severe malaria (2.4 mg/kg i.v). We investigated the effects of artesunate (1 mg/kg) or its active metabolite dihydroartemisinin (DHA; 0.1 mg/kg) in a model of transient myocardial ischaemia/reperfusion (I/R) and evaluated the mechanism of action of the observed cardioprotective effects of artesunate and DHA...
August 9, 2017: Shock
https://www.readbyqxmd.com/read/28774303/comparison-of-anti-malarial-drugs-efficacy-in-the-treatment-of-uncomplicated-malaria-in-african-children-and-adults-using-network-meta-analysis
#18
Solange Whegang Youdom, Rachida Tahar, Leonardo K Basco
BACKGROUND: Artemisinin-based combination therapy (ACT) and novel drug combinations are available and used in African countries to treat uncomplicated malaria. Network meta-analysis methods are rarely and poorly applied for the comparison of their efficacies. This method was applied on a set of randomized controlled trials to illustrate its usefulness. METHODS: A literature review available in Pubmed was conducted in July 2016. Eligible studies, conducted in sub-Saharan Africa, published between 2002 and 2016, focused on randomized controlled trials of at least two artemisinin-based combinations to treat uncomplicated malaria in children and adults...
August 3, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28751747/synergistic-blending-of-high-valued-heterocycles-inhibits-growth-of-plasmodium-falciparum-in-culture-and-p-berghei-infection-in-mouse-model
#19
Prashant Kumar, Angela O Achieng, Vinoth Rajendran, Prahlad C Ghosh, Brajendra K Singh, Manmeet Rawat, Douglas J Perkins, Prakasha Kempaiah, Brijesh Rathi
A series of phthalimide analogues, novelized with high-valued bioactive scaffolds was synthesized by means of click-chemistry under non-conventional microwave heating and evaluated as noteworthy growth inhibitors of Plasmodium falciparum (3D7 and W2) in culture. Analogues 6a, 6h and 6 u showed highest activity to inhibit the growth of the parasite with IC50 values in submicromolar range. Structure-activity correlation indicated the necessity of unsubstituted triazoles and leucine linker to obtain maximal growth inhibition of the parasite...
July 27, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28738892/challenges-to-replace-act-as-first-line-drug
#20
Aung Pyae Phyo, Lorenz von Seidlein
The spread of artemisinin and partner drug resistance through Asia requires changes in first-line therapy. The traditional modus has been the replacement of one first-line anti-malarial regimen with another. The number of anti-malarial drug candidates currently in development may have given false confidence in the expectation that resistance to artemisinin-based combination therapy (ACT) can be solved with a switch to the next anti-malarial drug regimen. A number of promising anti-malarial drug regimens did not succeed in becoming first-line drugs due to safety concerns or rapid development of resistance...
July 24, 2017: Malaria Journal
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