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Dihydroartemisinin

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https://www.readbyqxmd.com/read/29193867/improved-safety-margin-for-embryotoxicity-in-rats-for-the-new-endoperoxide-artefenomel-oz439-as-compared-to-artesunate
#1
Robert L Clark, Tammye L Edwards, Monica Longo, Joseph Kinney, Don K Walker, Jon Rhodes, Sally A Clode, Thomas Rückle, Timothy Wells, Nicole Andenmatten, Anna Christine Huber
BACKGROUND: Combination medicines including an artemisinin are the mainstay of antimalarial therapy. Artemisinins are potent embryotoxicants in animal species due to their trioxane moiety. METHODS: As part of its development, the new synthetic trioxolane antimalarial artefenomel (OZ439) was tested in rat whole embryo culture and in rat embryo-fetal toxicity studies with dosing throughout organogenesis or with a single dose on Gestational Day (GD) 12. The single-dose studies included groups treated with artesunate to allow a direct comparison of the embryotoxicity of the two antimalarials and included toxicokinetics hematology and histological examination of embryos...
November 28, 2017: Birth Defects Research
https://www.readbyqxmd.com/read/29193726/dihydroartemisinin-up-regulates-ve-cadherin-expression-in-human-renal-glomerular-endothelial-cells
#2
Liqun Li, Xiaocui Chen, Fengyun Dong, Qiang Liu, Caiqing Zhang, Dongmei Xu, Thaddeus D Allen, Ju Liu
The antimalarial agent dihydroartemisinin (DHA) has been shown to be anti-inflammatory. In this study, we found that DHA increased the expression of the junctional protein vascular endothelial (VE)-cadherin in human renal glomerular endothelial cells. In addition, DHA inhibited TGF-β RI-Smad2/3 signalling and its downstream effectors SNAIL and SLUG, which repress VE-cadherin gene transcription. Correspondingly, DHA decreased the binding of SNAIL and SLUG to the VE-cadherin promoter. Together, our results suggest an effect of DHA in regulating glomerular permeability by elevation of VE-cadherin expression...
November 29, 2017: Journal of Cellular and Molecular Medicine
https://www.readbyqxmd.com/read/29152657/dihydroartemisinin-treatment-exhibits-antitumor-effects-in-glioma-cells-through-induction-of-apoptosis
#3
Chun-Hua Xu, Yue Liu, Li-Min Xiao, Chang-Gui Guo, Su-Yue Zheng, Er-Ming Zeng, Dong-Hai Li
The present study aimed to investigate the effect of dihydroartemisinin on the proliferation of chemotherapy‑resistant C6 rat glioma cells. The results revealed that incubation of C6 glioma cells with a range of dihydroartemisinin concentrations for 48 h led to a significant (P<0.02) reduction in the cell number. There was a ‑0.8-fold reduction in the cell count following treatment with 20 µM dihydroartemisinin when compared with the control cultures. Analysis of DNA synthesis using bromodeoxyuridine (BrdU) staining demonstrated a reduction in the BrdU‑labeling index (LI) following treatment with 20 µM dihydroartemisinin...
October 19, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/29139274/-dihydroartemisinin-inhibits-proliferation-of-pancreatic-cancer-jf-305-cells-by-regulating-expression-of-apoptosis-related-proteins-and-production-of-reactive-oxygen-species
#4
Ya-Wei Li, Wei Zhang, Na Xu, Yan Li, Hong Zhang, Shi-Jie Lv, Wen-He Zhu
To investigate the effect of dihydroartemisinin on apoptosis of human pancreatic cancer cell line JF-305 and the role of reactive oxygen species(ROS) in the apoptosis of JF-305 cells induced by dihydroartemisinin. MTT assays were used to detect effect of different concentrations of dihydroartemisinin on cells proliferation of JF-305 lines. Cell cycle was detected by flow cytometry, and the apoptotic morphology was observed by Hoechst 333258 fluorescence staining. Annexin V fluorescence staining was used to detect the apoptosis changes of JF-305 cells, while DCFH-DA was used to detect the changes of ROS during apoptosis process...
August 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/29136776/dihydroartemisinin-inhibits-er-stress-mediated-mitochondrial-pathway-to-attenuate-hepatocyte-lipoapoptosis-via-blocking-the-activation-of-the-pi3k-akt-pathway
#5
Xingran Chen, Mianli Bian, Chenxi Zhang, Jun Kai, Zhen Yao, Huanhuan Jin, Chunfeng Lu, Jiangjuan Shao, Anping Chen, Feng Zhang, Shizhong Zheng
Alcoholic liver disease (ALD), characterized by accumulation of fatty acids in liver cells, is usually caused by Chronic alcohol consumption. Our previous study has identified that DA protects against alcoholic liver injury in alcohol-fed rats through alleviating hepatocyte steatosis. It has emerged that saturated fatty acids could provoke endoplasmic reticulum (ER) stress and apoptosis in hepatocytes. This study was aimed to explore the impact of DA on ALD and further elaborate the underlying mechanisms. Results demonstrated that DA attenuates alcoholic liver injury in mice...
November 7, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29128513/dihydroartemisinin-induced-caspase-dependent-apoptosis-through-inhibiting-the-specificity-protein-1-pathway-in-hepatocellular-carcinoma-sk-hep-1-cells
#6
Eunji Im, Changhwan Yeo, Hyo-Jeong Lee, Eun-Ok Lee
AIMS: Dihydroartemisinin (DHA) is a semi-synthetic derivative of artemisinin, well known for a safe and effective first-line antimalarial agent. This study investigated whether and how DHA induces apoptosis focusing on the specificity protein 1 (Sp1) pathway in hepatocellular carcinoma (HCC) SK-Hep-1 cells. MAIN METHODS: The cell viability was evaluated by MTT assay. Cell cycle analysis was performed after PI staining by flow cytometry system. Apoptosis was confirmed by DAPI staining and by detecting cytoplasmic histone-associated-DNA-fragments using a cell death detection ELISA(PLUS) kit...
November 8, 2017: Life Sciences
https://www.readbyqxmd.com/read/29114376/dihydroartemisinin-induces-apoptosis-in-human-bladder-cancer-cell-lines-through-reactive-oxygen-species-mitochondrial-membrane-potential-and-cytochrome-c-pathway
#7
Farhad Poupel, Mahmoud Aghaei, Ahmad Movahedian, Seyyed Mehdi Jafari, Mohammad Keyvanloo Shahrestanaki
Background: Dihydroartemisinin (DHA) is a semisynthetic derivative of artemisinin and has antiproliferative effect. However, such effects of DHA have not yet been revealed for bladder cancer cells. Methods: We used as bladder cancer cell lines to examine the effect of DHA on the cell viability, cell apoptosis, and monitoring of mitochondrial membrane potential (ΔΨm) changes. Furthermore, the effect of DHA on the reactive oxygen species (ROS) production and cytochrome c release were also detected...
2017: International Journal of Preventive Medicine
https://www.readbyqxmd.com/read/29110709/the-prevalence-incidence-and-prevention-of-plasmodium-falciparum-infections-in-forest-rangers-in-bu-gia-map-national-park-binh-phuoc-province-vietnam-a-pilot-study
#8
Do Hung Son, Nguyen Thuy-Nhien, Lorenz von Seidlein, Truong Le Phuc-Nhi, Ngo Thi Phu, Nguyen Thi Kim Tuyen, Nguyen Huyen Tran, Nguyen Van Dung, Bui Van Quan, Nicholas P J Day, Arjen M Dondorp, Nicholas J White, Guy E Thwaites, Tran Tinh Hien
BACKGROUND: Prophylaxis for high-risk populations, such as forest workers, could be one component for malaria elimination in the Greater Mekong Sub-region. A study was conducted to assess the malaria incidence in forest rangers and the feasibility of malaria prophylaxis for rangers sleeping in forest camps. METHODS: Forest rangers deployed in the Bu Gia Map National Park, Vietnam were invited to participate in the study. Plasmodium infections were cleared using presumptive treatment, irrespective of malaria status, with a 3-day course dihydroartemisinin/piperaquine (DP) and a 14-day course of primaquine...
November 6, 2017: Malaria Journal
https://www.readbyqxmd.com/read/29102180/synthesis-anticancer-evaluation-and-pharmacokinetic-study-of-novel-10-o-phenyl-ethers-of-dihydroartemisinin
#9
Shenglin Luan, Hang Zhong, Xuan Zhao, Jinyu Yang, Yongkui Jing, Dan Liu, Linxiang Zhao
Twenty hybrid compounds, tethering dihydroartemisinin (DHA) with diaryl-pyrazoline/diaryl-pyrazole through ether linkage, were synthesized based on hybridization strategy and assessed for their anticancer activity. The representative compound 6f exhibited significantly elevated antiproliferative activity compared with DHA against a panel of cancer cell lines. Unexpected sensitivity of 6f in Adriamycin-resistant MCF-7 cells (MCF-7/Adr) inspired subsequent research on anticancer activity of these DHA derivatives against breast cancer cell lines...
December 1, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29096671/community-led-responses-for-elimination-core-a-study-protocol-for-a-community-randomized-controlled-trial-assessing-the-effectiveness-of-community-level-reactive-focal-drug-administration-for-reducing-plasmodium-falciparum-infection-prevalence-and-incidence
#10
Daniel J Bridges, John M Miller, Victor Chalwe, Hawela Moonga, Busiku Hamainza, Rick Steketee, Kafula Silumbe, Jenala Nyangu, David A Larsen
BACKGROUND: Zambia is pushing for, and has made great strides towards, the elimination of malaria transmission in Southern Province. Reactive focal test and treat (RFTAT) using rapid diagnostic tests and artemether-lumefantrine (AL) has been key in making this progress. Reactive focal drug administration (RFDA) using dihydroartemisinin-piperaquine (DHAP), may be superior in accelerating clearance of the parasite reservoir in humans due to the provision of enhanced chemoprophylactic protection of at-risk populations against new infections...
November 2, 2017: Trials
https://www.readbyqxmd.com/read/29065172/concomitant-nevirapine-impacts-pharmacokinetic-exposure-to-the-antimalarial-artemether-lumefantrine-in-african-children
#11
Liusheng Huang, Vincent Carey, Jane C Lindsey, Florence Marzan, David Gingrich, Bobbie Graham, Linda Barlow-Mosha, Phionah K Ssemambo, Portia Kamthunzi, Sharon Nachman, Sunil Parikh, Francesca T Aweeka
BACKGROUND: The antiretroviral drug nevirapine and the antimalarial artemisinin-based combination therapy artemether-lumefantrine are commonly co-administered to treat malaria in the context of HIV. Nevirapine is a known inhibitor of cytochrome P450 3A4, which metabolizes artemether and lumefantrine. To address the concern that the antiretroviral nevirapine impacts the antimalarial artemether-lumefantrine pharmacokinetics, a prospective non-randomized controlled study in children presenting with uncomplicated malaria and HIV in sub-Saharan Africa was carried out...
2017: PloS One
https://www.readbyqxmd.com/read/29062913/safety-and-effectiveness-of-mass-drug-administration-to-accelerate-elimination-of-artemisinin-resistant-falciparum-malaria-a-pilot-trial-in-four-villages-of-eastern-myanmar
#12
Jordi Landier, Ladda Kajeechiwa, May Myo Thwin, Daniel M Parker, Victor Chaumeau, Jacher Wiladphaingern, Mallika Imwong, Olivo Miotto, Krittaya Patumrat, Jureeporn Duanguppama, Dominique Cerqueira, Benoit Malleret, Laurent Rénia, Suphak Nosten, Lorenz von Seidlein, Clare Ling, Stéphane Proux, Vincent Corbel, Julie A Simpson, Arjen M Dondorp, Nicholas J White, François H Nosten
Background: Artemisinin and partner drug-resistant falciparum malaria is expanding over the Greater Mekong Sub-region (GMS). Eliminating falciparum malaria in the GMS while drugs still retain enough efficacy could prevent global spread of antimalarial resistance. Eliminating malaria rapidly requires targeting the reservoir of asymptomatic parasite carriers. This pilot trial aimed to evaluate the acceptability, safety, feasibility and effectiveness of mass-drug administration (MDA) in reducing malaria in four villages in Eastern Myanmar...
2017: Wellcome Open Research
https://www.readbyqxmd.com/read/29061778/anticancer-activity-of-artemisinin-and-its-derivatives
#13
REVIEW
Silvia Slezakova, Jana Ruda-Kucerova
Artemisinin is an extract from the plant Artemisia annua. With its semi-synthetic derivatives, they form a group of well-known and efficacious antimalarial drugs. Recent studies have documented the potential anticancer effect of artemisinin and its derivatives (ARTs). This review summarizes results of preclinical studies, documenting mechanisms of anticancer actions of ARTs and clinical studies focused mainly on efficacy, safety and dose-ranging of ARTs as anticancer chemotherapeutics. The main mechanisms of action of ARTs is the production of reactive oxygen species, inhibition of cell cycle in G0/G1 phase, induction of apoptosis and inhibition of angiogenesis...
November 2017: Anticancer Research
https://www.readbyqxmd.com/read/29061746/a-new-water-dispersible-paediatric-formulation-of-dihydroartemisinin-piperaquine-for-the-treatment-of-uncomplicated-plasmodium-falciparum-malaria-in-african-infants-efficacy-and-tolerability-outcomes-of-a-phase-ii-randomized-open-label-multicenter-study
#14
Nicola Gargano, Lola Madrid, Giovanni Valentini, Umberto D'Alessandro, Tinto Halidou, Sodiomon Sirima, Antoinette Tshefu, Ali Mtoro, Samwel Gesase, Quique Bassat
Artemisinin combination therapies are considered the mainstay of malaria treatment, but paediatric friendly formulations for the treatments of infants are scarce. We aimed to evaluate the efficacy and safety of a new dispersible tablet formulation of dihydroartemisinin/piperaquine phosphate (DHA/PQP) in comparison to the marketed tablet (Eurartesim®) in the treatment of infants with uncomplicated P. falciparum malaria.Reported here are the results of a large phase II, randomized, open label, multicenter trial conducted in African infants (6-12 months of age) from Mozambique, Burkina Faso, The Gambia, DR-Congo and Tanzania...
October 23, 2017: Antimicrobial Agents and Chemotherapy
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
#15
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
#16
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
#17
REVIEW
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 efficacy. 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)...
November 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
#18
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
#19
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 antiapoptotic MCL-1 to promote viability and are resistant to BH3-mimetic agents such as navitoclax (ABT-263) that target BCL-2, BCL-XL, and BCL-W. However, the survival of most normal blood cells and other cell types is 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
#20
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
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