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https://www.readbyqxmd.com/read/28213434/malaria-during-pregnancy
#1
Michal Fried, Patrick E Duffy
One hundred and twenty-five million women in malaria-endemic areas become pregnant each year (see Dellicour et al. PLoS Med7: e1000221 [2010]) and require protection from infection to avoid disease and death for themselves and their offspring. Chloroquine prophylaxis was once a safe approach to prevention but has been abandoned because of drug-resistant parasites, and intermittent presumptive treatment with sulfadoxine-pyrimethamine, which is currently used to protect pregnant women throughout Africa, is rapidly losing its benefits for the same reason...
February 17, 2017: Cold Spring Harbor Perspectives in Medicine
https://www.readbyqxmd.com/read/28208619/akt-axis-mir-21-and-reck-play-pivotal-roles-in-dihydroartemisinin-killing-malignant-glioma-cells
#2
Ying-Ying Shao, Tao-Lan Zhang, Lan-Xiang Wu, He-Cun Zou, Shuang Li, Jin Huang, Hong-Hao Zhou
Dihydroartemisinin (DHA), a semi-synthetic derivative of artemisinin, is known to play important roles in inhibiting proliferation rate, inducing apoptosis, as well as hindering the metastasis and invasion of glioma cells, but the underlying mechanisms are still unclear so far. In this study, methyl thiazolyl tetrazolium (MTT), colony-forming, wound healing, invasion, and apoptosis assays were performed to investigate the effect of DHA on malignant glioma cells. Results showed that DHA induced apoptosis of malignant glioma cells through Protein Kinase B (AKT) axis, induced death of malignant glioma cells by downregulating miR-21, and inhibited the invasion of malignant glioma cells corresponding with up-regulation of the reversion-inducing-cysteine-rich protein with kazal motifs (RECK)...
February 10, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28195463/target-elucidation-by-co-crystal-structures-of-nadh-ubiquinone-oxidoreductase-of-plasmodium-falciparum-pfndh2-with-small-molecule-to-eliminate-drug-resistant-malaria
#3
Yiqing Yang, You Yu, Xiaolu Li, Jing Li, Yue Wu, Jie Yu, Jingpeng Ge, Zhenghui Huang, Lubin Jiang, Yu Rao, Maojun Yang
Drug-resistant malarial strains have been continuously emerging recently, which posts a great challenge for the global health. Therefore, new anti-malarial drugs with novel targeting mechanisms are urgently needed for fighting drug-resistant malaria. NADH-ubiquinone oxidoreductase of Plasmodium falciparum (PfNDH2) represents a viable target for anti-malarial drug development. However, the absence of structural information of PfNDH2 limited rational drug design and further development. Herein, we report high resolution crystal structures of the PfNDH2 protein for the first time in Apo-, NADH- and RYL-552 (a new inhibitor)-bound states...
February 14, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28193647/piperaquine-population-pharmacokinetics-and-cardiac-safety-in-cambodia
#4
Pattaraporn Vanachayangkul, Chanthap Lon, Michele Spring, Sommethy Sok, Winita Ta-Aksorn, Chanikarn Kodchakorn, Sut-Thang Pann, Soklyda Chann, Mali Ittiverakul, Sabaithip Sriwichai, Nillawan Buathong, Worachet Kuntawunginn, Mary So, Theng Youdaline, Erin Milner, Mariusz Wojnarski, Charlotte Lanteri, Jessica Manning, Satharath Prom, Mark Haigney, Louis Cantilena, David Saunders
Despite rising resistance, dihydroartemisinin-piperaquine (DP) remains a first line therapy for uncomplicated malaria in many parts of Cambodia. While generally well-tolerated as a 3-day regimen, compressed 2-day regimens were associated with treatment-limiting cardiac repolarization effects in a recent clinical trial. To better estimate the risks of piperaquine concentration on QT interval prolongation, we pooled data from 3 randomized clinical trials between 2010 and 2014 in northern Cambodia. A population pharmacokinetic model was developed to compare exposure-response relationships between 2-day (2DP) and 3-day (3DP) regimens while accounting for differences in regimen and sample collection times between studies...
February 13, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28189106/application-of-sequential-factorial-design-and-orthogonal-array-composite-design-oacd-to-study-combination-of-5-prostate-cancer-drugs
#5
Xiaolong Jia, Yiyang Li, Alok Sharma, Yulong Li, Guohai Xie, Guoyao Wang, Junhui Jiang, Yue Cheng, Xianting Ding
Prostate cancer is one of the most common cancers among men in the United States. It is also a major leading cause of cancer death among men of all races. In order to treat prostate cancer, drug combinations are often applied. Drug combinations target at different pathways of cells can potentially lead to higher efficacy and lower toxicity due to drug synergy. In this paper, we sequentially applied a two-level design and a follow-up orthogonal array composite design (OACD) to investigate combinations of five anti-cancer drugs, namely, doxorubicin, docetaxel, paclitaxel, cis-dichlorodiamine platinum and dihydroartemisinin...
February 4, 2017: Computational Biology and Chemistry
https://www.readbyqxmd.com/read/28187497/antiretroviral-therapy-with-efavirenz-accentuates-pregnancy-associated-reduction-of-dihydroartemisinin-piperaquine-exposure-during-malaria-chemoprevention
#6
Richard Kajubi, Liusheng Huang, Prasanna Jagannathan, Nona Chamankhah, Moses Were, Theodore Ruel, Catherine A Koss, Abel Kakuru, Norah Mwebaza, Moses Kamya, Diane Havlir, Grant Dorsey, Philip J Rosenthal, Francesca T Aweeka
Dihydroartemisinin (DHA)-piperaquine is promising for malaria chemoprevention in pregnancy. We assessed impacts of pregnancy and efavirenz-based antiretroviral therapy on exposure to DHA and piperaquine in pregnant Ugandan women. Intensive sampling was performed at 28 weeks gestation in 31 HIV-uninfected pregnant women, in 27 HIV-infected pregnant women receiving efavirenz, and in 30 HIV-uninfected non-pregnant women. DHA peak concentration and area under the concentration time curve (AUC0-8hr ) were 50% and 47% lower, respectively, and piperaquine AUC0-21d was 40% lower in pregnant women compared to non-pregnant women...
February 10, 2017: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28182780/farnesylthiosalicylic-acid-sensitizes-hepatocarcinoma-cells-to-artemisinin-derivatives
#7
Liping Wu, Yilin Pang, Guiqi Qin, Gaina Xi, Shengnan Wu, Xiaoping Wang, Tongsheng Chen
Dihydroartemisinin (DHA) and artesunate (ARS), two artemisinin derivatives, have efficacious anticancer activities against human hepatocarcinoma (HCC) cells. This study aims to study the anticancer action of the combination treatment of DHA/ARS and farnesylthiosalicylic acid (FTS), a Ras inhibitor, in HCC cells (Huh-7 and HepG2 cell lines). FTS pretreatment significantly enhanced DHA/ARS-induced phosphatidylserine (PS) externalization, Bak/Bax activation, mitochondrial membrane depolarization, cytochrome c release, and caspase-8 and -9 activations, characteristics of the extrinsic and intrinsic apoptosis...
2017: PloS One
https://www.readbyqxmd.com/read/28170391/haemolysis-in-g6pd-heterozygous-females-treated-with-primaquine-for-plasmodium-vivax-malaria-a-nested-cohort-in-a-trial-of-radical-curative-regimens
#8
Cindy S Chu, Germana Bancone, Kerryn A Moore, Htun Htun Win, Niramon Thitipanawan, Christina Po, Nongnud Chowwiwat, Rattanaporn Raksapraidee, Pornpimon Wilairisak, Aung Pyae Phyo, Lily Keereecharoen, Stéphane Proux, Prakaykaew Charunwatthana, François Nosten, Nicholas J White
BACKGROUND: Radical cure of Plasmodium vivax malaria with 8-aminoquinolines (primaquine or tafenoquine) is complicated by haemolysis in individuals with glucose-6-phosphate dehydrogenase (G6PD) deficiency. G6PD heterozygous females, because of individual variation in the pattern of X-chromosome inactivation (Lyonisation) in erythroid cells, may have low G6PD activity in the majority of their erythrocytes, yet are usually reported as G6PD "normal" by current phenotypic screening tests...
February 2017: PLoS Medicine
https://www.readbyqxmd.com/read/28154599/effect-of-stents-coated-with-artemisinin-or-dihydroartemisinin-in-a-porcine-coronary-restenosis-model
#9
Suyoung Jang, Myung Ho Jeong, Kyung Seob Lim, In Ho Bae, Jun-Kyu Park, Dae Sung Park, Jae Won Shim, Jung Ha Kim, Hyun Kuk Kim, Doo Sun Sim, Young Joon Hong, Youngkeun Ahn, Jung Chaee Kang
BACKGROUND AND OBJECTIVES: Artemisinin and dihydroartemisinin are drugs used to treat malaria. These drugs suppress inflammatory reactions. The aim of this study was to examine the anti-intima hyperplasia effect of a novel drug-eluting stent with artemisinin or dihydroartemisinin in a porcine coronary restenosis model. MATERIALS AND METHODS: Pigs were randomized into four groups; in the first, the coronary arteries (20 pigs, a total of 40 coronary arteries, with 10 coronary arteries in each group) was implanted with bare metal stents (BMS, n=10); the second group was given polymer-coated stents (PCS, n=10); the third group was treated with artemisinin-eluting stents (AES, n=10); and the fourth group was given dihydroartemisinin-eluting stents (DAES, n=10)...
January 2017: Korean Circulation Journal
https://www.readbyqxmd.com/read/28153004/efficacy-of-artemether-lumefantrine-artesunate-amodiaquine-and-dihydroartemisinin-piperaquine-for-treatment-of-uncomplicated-plasmodium-falciparum-malaria-in-angola-2015
#10
Mateusz M Plucinski, Pedro Rafael Dimbu, Aleixo Panzo Macaia, Carolina Miguel Ferreira, Claudete Samutondo, Joltim Quivinja, Marília Afonso, Richard Kiniffo, Eliane Mbounga, Julia S Kelley, Dhruviben S Patel, Yun He, Eldin Talundzic, Denise O Garrett, Eric S Halsey, Venkatachalam Udhayakumar, Pascal Ringwald, Filomeno Fortes
BACKGROUND: Recent anti-malarial resistance monitoring in Angola has shown efficacy of artemether-lumefantrine (AL) in certain sites approaching the key 90% lower limit of efficacy recommended for artemisinin-based combination therapy. In addition, a controversial case of malaria unresponsive to artemisinins was reported in a patient infected in Lunda Sul Province in 2013. METHODS: During January-June 2015, investigators monitored the clinical and parasitological response of children with uncomplicated Plasmodium falciparum infection treated with AL, artesunate-amodiaquine (ASAQ), or dihydroartemisinin-piperaquine (DP)...
February 2, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28151566/efficacy-of-artesunate-sulfadoxine-pyrimethamine-and-artemether-lumefantrine-and-dhfr-and-dhps-mutations-in-somalia-evidence-for%C3%A2-updating-the-malaria-treatment-policy
#11
Marian Warsame, Abdikarim Hussein Hassan, Abdillahi Mohamed Hassan, Abdulkadir Mohamed Arale, Ali Mohamed Jibril, Said Abdulkadir Mohamud, Amy Barrette, Abdikarim Yusuf Muse, Fahmi Essa Yusuf Rania A Nada, Jamal Ghilan Hefzullah Amran
OBJECTIVE: To determine the therapeutic efficacy of artesunate + sulfadoxine/pyrimethamine (AS + SP) and artemether + lumefantrine (AL), and to investigate the presence of molecular mutations associated with resistance, to inform national malaria treatment policy. METHODS: One-arm prospective studies were conducted in three study sites in Somalia in 2013 and 2015 to evaluate the efficacy of AS + SP and AL among patients with uncomplicated falciparum malaria. Outcomes included clinical and parasitological response over 28 days, and the presence of dihydrofolate reductase (dfhr) and dihydropteroate synthase (dhps) and mutations...
February 2, 2017: Tropical Medicine & International Health: TM & IH
https://www.readbyqxmd.com/read/28143417/early-rising-asexual-parasitaemia-in-nigerian-children-following-a-first-dose-of-artemisinin-based-combination-treatments-of-falciparum-malaria
#12
Akintunde Sowunmi, Kazeem Akano, Adejumoke I Ayede, Elsie O Adewoye, Godwin Ntadom, Bayo Fatunmbi, Grace O Gbotosho, Onikepe A Folarin, Christian T Happi
BACKGROUND: Early rising asexual parasitaemia (ERAP), initially defined as 'an increase in the parasite count over the baseline pre-treatment level during the first 24 h of treatment' of falciparum malaria with artemisinin derivatives is well documented, but there is no characterization of its risk factors, kinetics, molecular features or relationship to late-appearing anaemia (LAA) in acute falciparum malaria in African children following oral artemisinin-based combination therapies (ACTs)...
January 31, 2017: BMC Infectious Diseases
https://www.readbyqxmd.com/read/28137815/k13-propeller-mutations-in-plasmodium-falciparum-populations-in-malaria-endemic-regions-of-vietnam-from-2009-to-2016
#13
Nguyen Thuy-Nhien, Nguyen Kim Tuyen, Nguyen Thanh Tong, Tuong Vy, Ngo Viet Thanh, Huynh Thuy Van, Pham Huong-Thu, Huynh Hong Quang, Maciej F Boni, Christiane Dolecek, Jeremy Farrar, Guy E Thwaites, Olivo Miotto, Nicholas J White, Tran Tinh Hien
The spread of artemisinin resistant P. falciparum compromises the therapeutic efficacy of artemisinin combination therapies (ACT) and is considered the greatest threat to current global initiatives to control and eliminate malaria. This is particularly relevant for Vietnam, where dihydroartemisinin-piperaquine (DP) is the recommended ACT for P. falciparum The propeller domain gene of K13, a molecular marker of artemisinin resistance, was sequenced successfully in 1060 P. falciparum isolates collected at 3 malaria hotspots in Vietnam between 2009 and 2016...
January 30, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28122617/in-vitro-activity-of-anti-malarial-ozonides-against-an-artemisinin-resistant-isolate
#14
Fabian Baumgärtner, Joëlle Jourdan, Christian Scheurer, Benjamin Blasco, Brice Campo, Pascal Mäser, Sergio Wittlin
BACKGROUND: Recently published data suggest that artemisinin derivatives and synthetic peroxides, such as the ozonides OZ277 and OZ439, have a similar mode of action. Here the cross-resistance of OZ277 and OZ439 and four additional next-generation ozonides was probed against the artemisinin-resistant clinical isolate Plasmodium falciparum Cam3.I, which carries the K13-propeller mutation R539T (Cam3.I(R539T)). METHODS: The previously described in vitro ring-stage survival assay (RSA0-3h) was employed and a simplified variation of the original protocol was developed...
January 25, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28111262/dihydroartemisin-inhibits-glioma-invasiveness-via-a-ros-to-p53-to-%C3%AE-catenin-signaling
#15
Zhongyou Que, Ping Wang, Yi Hu, Yixue Xue, Xiaobai Liu, Chengbin Qu, Jun Ma, Yunhui Liu
Dihydroartemisinin(DHA) is the active metabolic derivative of artemisinin. DHA has potential therapeutic effects on glioma but the detailed mechanism is unclear. In this study, we investigated the role and the underlying mechanisms of DHA in its inhibition of glioma cells. U87 cells are wild-type p53 glioblastoma cells and U251 cells contain mutant p53. DHA inhibited the proliferation, migration and invasion of glioma cells in a dose-dependent manner. DHA promoted reactive oxygen species production and activated p53 in two glioma cell lines, U87 and U251...
January 19, 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/28105176/dihydroartemisinin-transiently-activates-the-jnk-sapk-signaling-pathway-in-endothelial-cells
#16
Fengyun Dong, Ju Han, Guoxian Jing, Xiaocui Chen, Suhua Yan, Longtao Yue, Zhiqun Cao, Xiaochun Liu, Guozhao Ma, Ju Liu
Artemisinin and its derivatives are well-known anti-malaria drugs and in the early stages of research for cancer treatment. Dihydroartemisinin (DHA), a more water-soluble derivative of artemisinin, has demonstrated strong anti-angiogenic activity. The purpose of the present study was to investigate the underlying molecular mechanisms of the effect of DHA on angiogenesis. Human umbilical vein endothelial cells (HUVECs) treated with DHA were examined for apoptosis and activation of the c-Jun N-terminal kinase (JNK) signaling pathway, one of the major mitogen-activated protein kinase cascades...
December 2016: Oncology Letters
https://www.readbyqxmd.com/read/28087910/-progress-on-anti-tumor-molecular-mechanisms-of-dihydroartemisinin
#17
Peng Cao, Dongjin Leng, Ying Li, Ziwei Zhang, Lei Liu, Xiaoyan Li
Artemisinin is an anti-malarial drug with poor water solubility and oral absorption; so a variety of derivatives based on the parent nucleus have been developed. Compared with artemisinin, dihydroartemisinin (DHA) has a stronger anti-malaria activity, and has the advantages of high metabolic rate and better water solubility. Recent studies have discovered that DHA has a good inhibitory effect on tumor cells, which is closely related to the peroxide bridge in its molecular structure. Since tumor cells need more Fe(3+) than normal cells, there are a large number of transferrin receptors on the tumor cell membrane...
May 25, 2016: Zhejiang da Xue Xue Bao. Yi Xue Ban, Journal of Zhejiang University. Medical Sciences
https://www.readbyqxmd.com/read/28086775/rapid-decline-in-the-susceptibility-of-plasmodium-falciparum-to-dihydroartemisinin-piperaquine-in-the-south-of-vietnam
#18
Ngo Viet Thanh, Nguyen Thuy-Nhien, Nguyen Thi Kim Tuyen, Nguyen Thanh Tong, Nguyen Thuy Nha-Ca, Le Thanh Dong, Huynh Hong Quang, Jeremy Farrar, Guy Thwaites, Nicholas J White, Marcel Wolbers, Tran Tinh Hien
BACKGROUND: Artemisinin resistant Plasmodium falciparum has emerged in the countries of the Greater Mekong sub-region posing a serious threat to global malaria elimination efforts. The relationship of artemisinin resistance to treatment failure has been unclear. METHODS: In annual studies conducted in three malaria endemic provinces in the south of Vietnam (Binh Phuoc, Ninh Thuan and Gia Lai) between 2011 and 2015, 489 patients with uncomplicated P. falciparum malaria were enrolled in detailed clinical, parasitological and molecular therapeutic response assessments with 42 days follow up...
January 13, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28072872/population-pharmacokinetic-properties-of-piperaquine-in-falciparum-malaria-an-individual-participant-data-meta-analysis
#19
Richard M Hoglund, Lesley Workman, Michael D Edstein, Nguyen Xuan Thanh, Nguyen Ngoc Quang, Issaka Zongo, Jean Bosco Ouedraogo, Steffen Borrmann, Leah Mwai, Christian Nsanzabana, Ric N Price, Prabin Dahal, Nancy C Sambol, Sunil Parikh, Francois Nosten, Elizabeth A Ashley, Aung Pyae Phyo, Khin Maung Lwin, Rose McGready, Nicholas P J Day, Philippe J Guerin, Nicholas J White, Karen I Barnes, Joel Tarning
BACKGROUND: Artemisinin-based combination therapies (ACTs) are the mainstay of the current treatment of uncomplicated Plasmodium falciparum malaria, but ACT resistance is spreading across Southeast Asia. Dihydroartemisinin-piperaquine is one of the five ACTs currently recommended by the World Health Organization. Previous studies suggest that young children (<5 y) with malaria are under-dosed. This study utilised a population-based pharmacokinetic approach to optimise the antimalarial treatment regimen for piperaquine...
2017: PLoS Medicine
https://www.readbyqxmd.com/read/28070879/a-review-of-pharmacogenetics-of-antimalarials-and-associated-clinical-implications
#20
REVIEW
Hazem Elewa, Kyle John Wilby
Genetic variability in drug-metabolizing enzymes and drug transporters is known to influence the pharmacokinetics of many drugs. Antimalarial drugs are a class of agents known to utilize metabolic and elimination pathways prone to genetic variation. This paper aims to review the genetic variants affecting antimalarial medications and discuss their clinical implications. Data were identified for the genes coding for the cytochrome P450 (CYP) enzymes: CYP2C8, CYP2C19, CYP2A6, CYP2D6, CYP2B6, and the P-glycoprotein drug transporter...
January 9, 2017: European Journal of Drug Metabolism and Pharmacokinetics
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