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Artemisinin

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https://www.readbyqxmd.com/read/28726171/qsar-modeling-docking-and-admet-studies-for-exploration-of-potential-anti-malarial-compounds-against-plasmodium-falciparum
#1
Tabish Qidwai
Development of resistance in the Plasmodium falciparum to Artemisinin, the most effective anti-malarial compound, threatens malaria elimination tactics. To gain more efficacious Artemisinin derivatives, QSAR modeling and docking was performed. In the present study, 2D-QSAR model and molecular docking were used to evaluate the Artemisinin compounds and to reveal their binding modes and structural basis of inhibitory activity. Moreover, ADMET-related descriptors have been calculated to predict the pharmacokinetic properties of the effective compounds...
December 2016: In Silico Pharmacology
https://www.readbyqxmd.com/read/28724415/identification-and-characterization-of-the-antiplasmodial-activity-of-hsp90-inhibitors
#2
Claribel Murillo-Solano, Chunmin Dong, Cecilia G Sanchez, Juan C Pizarro
BACKGROUND: The recent reduction in mortality due to malaria is being threatened by the appearance of Plasmodium falciparum parasites that are resistant to artemisinin in Southeast Asia. To limit the impact of resistant parasites and their spread across the world, there is a need to validate anti-malarial drug targets and identify new leads that will serve as foundations for future drug development programmes targeting malaria. Towards that end, the antiplasmodial potential of several Hsp90 inhibitors was characterized...
July 19, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28724354/novel-plasmodium-falciparum-metabolic-network-reconstruction-identifies-shifts-associated-with-clinical-antimalarial-resistance
#3
Maureen A Carey, Jason A Papin, Jennifer L Guler
BACKGROUND: Malaria remains a major public health burden and resistance has emerged to every antimalarial on the market, including the frontline drug, artemisinin. Our limited understanding of Plasmodium biology hinders the elucidation of resistance mechanisms. In this regard, systems biology approaches can facilitate the integration of existing experimental knowledge and further understanding of these mechanisms. RESULTS: Here, we developed a novel genome-scale metabolic network reconstruction, iPfal17, of the asexual blood-stage P...
July 19, 2017: BMC Genomics
https://www.readbyqxmd.com/read/28723328/artemisinin-resistant-plasmodium-falciparum-in-africa
#4
LETTER
Feng Lu, Richard Culleton, Jun Cao
No abstract text is available yet for this article.
July 20, 2017: New England Journal of Medicine
https://www.readbyqxmd.com/read/28723327/artemisinin-resistant-plasmodium-falciparum-in-africa
#5
LETTER
(no author information available yet)
New England Journal of Medicine, Volume 377, Issue 3, Page 305-306, July 2017.
July 20, 2017: New England Journal of Medicine
https://www.readbyqxmd.com/read/28722611/phase-2a-open-label-4-escalating-dose-randomized-multicenter-study-evaluating-the-safety-and-activity-of-ferroquine-ssr97193-plus-artesunate-versus-amodiaquine-plus-artesunate-in-african-adult-men-with-uncomplicated-plasmodium-falciparum-malaria
#6
Christian Supan, Ghyslain Mombo-Ngoma, Maryvonne Kombila, Carmen L Ospina Salazar, Jana Held, Bertrand Lell, Cathy Cantalloube, Elhadj Djeriou, Bernhards Ogutu, John Waitumbi, Nekoye Otsula, Duncan Apollo, Mark E Polhemus, Peter G Kremsner, Douglas S Walsh
Artemisinin-based combination therapies are recommended as first-line agents for treating uncomplicated Plasmodium falciparum malaria. Ferroquine, a 4-aminoquinolone, is a novel long-acting combination partner for fast-acting drugs like artesunate (AS). We did a small phase 2a, multicenter, open-label, safety-focused dose-ranging randomized study of ferroquine at three African hospitals: two Gabonese and one Kenyan. We recruited adult men with symptomatic uncomplicated P. falciparum monoinfection. Four escalating doses of ferroquine (100, 200, 400, and 600 mg) were assessed in sequence, versus an amodiaquine comparator...
May 30, 2017: American Journal of Tropical Medicine and Hygiene
https://www.readbyqxmd.com/read/28719312/molecular-epidemiology-of-malaria-in-cameroon-and-c%C3%A3-te-d-ivoire-xxxi-kelch-13-propeller-sequences-in-plasmodium-falciparum-isolates-before-and-after-implementation-of-artemisinin-based-combination-therapy
#7
Joseph Allico Djaman, Dagnogo Olefongo, Aristide Berenger Ako, Jocelyne Roman, Vincent Foumane Ngane, Leonardo K Basco, Rachida Tahar
Artemisinin-resistant malaria has not been reported from Africa, but resistance can possibly spread from Asia or arise independently in Africa. The emergence of artemisinin resistance in Africa can be monitored by molecular assay of Kelch 13 (K13) propeller sequences. A total of 251 archived DNA samples of Plasmodium falciparum isolates collected in 2002, 2003, and 2006 in Yaounde, Cameroon, and 47 samples collected in 2006 and 2013 in Abidjan, Côte d'Ivoire, were analyzed for K13-propeller sequence polymorphism...
July 2017: American Journal of Tropical Medicine and Hygiene
https://www.readbyqxmd.com/read/28719180/heterologous-expression-purification-and-functional-analysis-of-plasmodium-falciparum-phosphatidylinositol-3-kinase
#8
Matthew Hassett, Anna Sternberg, Bryce Riegel, Craig J Thomas, Paul David Roepe
The Plasmodium falciparum malarial parasite genome appears to encode one and only one phosphatidylinositol 3'-kinase (PI3K) and sequence analysis suggests that the enzyme is a "class III" or "Vps34" type PI3K. The PfVps34 has generated excitement as a possible druggable target and potentially a key target of artemisinin-based antimalarials. In this study, we optimize the PfVps34 gene for heterologous expression in yeast, purify the protein to homogeneity, use a recently validated quantitative assay for phosphatidylinositol 3'-phosphate (PI3P) production from phosphatidylinositol (PI) (Hassett et al...
July 18, 2017: Biochemistry
https://www.readbyqxmd.com/read/28714338/antiplasmodial-prenylated-flavanonols-from-tephrosia-subtriflora
#9
Lois M Muiva-Mutisya, Yoseph Atilaw, Matthias Heydenreich, Andreas Koch, Hoseah M Akala, Agnes C Cheruiyot, Matthew L Brown, Beatrice Irungu, Faith A Okalebo, Solomon Derese, Charles Mutai, Abiy Yenesew
The CH2Cl2/MeOH (1:1) extract of the aerial parts of Tephrosia subtriflora afforded a new flavanonol, named subtriflavanonol (1), along with the known flavanone spinoflavanone B, and the known flavanonols MS-II (2) and mundulinol. The structures were elucidated by the use of NMR spectroscopy and mass spectrometry. The absolute configuration of the flavanonols was determined based on quantum chemical ECD calculations. In the antiplasmodial assay, compound 2 showed the highest activity against chloroquine-sensitive Plasmodium falciparum reference clones (D6 and 3D7), artemisinin-sensitive isolate (F32-TEM) as well as field isolate (KSM 009) with IC50 values 1...
July 16, 2017: Natural Product Research
https://www.readbyqxmd.com/read/28711439/updates-on-k13-mutant-alleles-for-artemisinin-resistance-in-plasmodium-falciparum
#10
REVIEW
Myo Thura Zaw, Nor Amalina Emran, Zaw Lin
BACKGROUND: In the fight against malaria caused by Plasmodium falciparum, the successes achieved by artemisinin were endangered by resistance of the parasites to the drug. Whole genome sequencing approach on artemisinin resistant parasite line discovered k13 gene associated with drug resistance. In vitro and in vivo studies indicated mutations in the k13 gene were linked to the artemisinin resistance. METHODOLOGY: The literatures published after April, 2015 up to December, 2016 on k13 mutant alleles for artemisinin resistance in Plasmodium falciparum and relevant literatures were comprehensively reviewed...
June 29, 2017: Journal of Microbiology, Immunology, and Infection, Wei Mian Yu Gan Ran za Zhi
https://www.readbyqxmd.com/read/28708672/artemisinin-disrupts-androgen-responsiveness-of-human-prostate-cancer-cells-by-stimulating-the-26s-proteasome-mediated-degradation-of-the-androgen-receptor-protein
#11
Andrea M Steely, Jamin A Willoughby, Shyam N Sundar, Vasiliki I Aivaliotis, Gary L Firestone
Androgen receptor (AR) expression and activity is highly linked to the development and progression of prostate cancer and is a target of therapeutic strategies for this disease. We investigated whether the antimalarial drug artemisinin, which is a sesquiterpene lactone isolated from the sweet wormwood plant Artemisia annua, could alter AR expression and responsiveness in cultured human prostate cancer cell lines. Artemisinin treatment induced the 26S proteasome-mediated degradation of the receptor protein, without altering AR transcript levels, in androgen-responsive LNCaP prostate cancer cells or PC-3 prostate cancer cells expressing exogenous wild-type AR...
July 13, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28707601/potential-role-of-natural-compounds-as-anti-angiogenic-agents-in-cancer
#12
Muthu K Shanmugam, Sudha Warrier, Alan Prem Kumar, Gautam Sethi, Frank Arfuso
BACKGROUND: Neovascularization, also known as angiogenesis, is the process of capillary sprouting from pre-existing blood vessels. This physiological process is a hallmark event in normal embryonic development as blood vessels generally supply both oxygen and nutrients to the cells of the body. Any disruption in this process can lead to the development of various chronic diseases, including cancer. In cancer, aberrant angiogenesis plays a prominent role in maintaining sustained tumor growth to malignant phenotypes and promoting metastasis...
July 12, 2017: Current Vascular Pharmacology
https://www.readbyqxmd.com/read/28693890/artemisinin-and-chinese-medicine-as-tu-science
#13
Jia-Chen Fu
The story of discovery of artemisinin highlights the diversity of scientific values across time and space. Resituating artemisinin research within a broader temporal framework allows us to understand how Chinese drugs like qinghao came to articulate a space for scientific experimentation and innovation through its embodiment of alternating clusters of meanings associated with tu and yang within scientific discourse. Tu science, which was associated with terms like native, Chinese, local, rustic, mass, and crude, articulated a radical vision of science in the service of socialist revolutionary ideals...
July 7, 2017: Endeavour
https://www.readbyqxmd.com/read/28689867/ex-vivo-activity-of-proveblue-a-methylene-blue-against-field-isolates-of-plasmodium-falciparum-in-dakar-senegal-from-2013-2015
#14
Bécaye Fall, Marylin Madamet, Silman Diawara, Sébastien Briolant, Khalifa Ababacar Wade, Gora Lo, Aminata Nakoulima, Mansour Fall, Raymond Bercion, Mame Bou Kounta, Rémi Amalvict, Nicolas Benoit, Mamadou Wague Gueye, Bakary Diatta, Boubacar Wade, Bruno Pradines
Resistance to most antimalarial drugs has spread from Southeast Asia to Africa. Accordingly, new therapies to use with artemisinin-based combination therapy (triple ACT) are urgently needed. Proveblue, a methylene blue preparation, was found to exhibit antimalarial activity against Plasmodium falciparum strains in vitro. Proveblue has synergistic effects when used in combination with dihydroartemisinin, and has been shown to significantly reduce or prevent cerebral malaria in mice. The objectives of the current study were to evaluate the in vitro baseline susceptibility of clinical field isolates to Proveblue, compare its activity with that of other standard antimalarial drugs and define the patterns of cross-susceptibility between Proveblue and conventional antimalarial drugs...
July 6, 2017: International Journal of Antimicrobial Agents
https://www.readbyqxmd.com/read/28688800/protein-degradation-systems-as-antimalarial-therapeutic-targets
#15
REVIEW
Caroline L Ng, David A Fidock, Matthew Bogyo
Artemisinin (ART)-based combination therapies are the most efficacious treatment of uncomplicated Plasmodium falciparum malaria. Alarmingly, P. falciparum strains have acquired resistance to ART across much of Southeast Asia. ART creates widespread protein and lipid damage inside intraerythrocytic parasites, necessitating macromolecule degradation. The proteasome is the main engine of Plasmodium protein degradation. Indeed, proteasome inhibition and ART have shown synergy in ART-resistant parasites. Moreover, ubiquitin modification is associated with altered parasite susceptibility to multiple antimalarials...
July 5, 2017: Trends in Parasitology
https://www.readbyqxmd.com/read/28687086/ivermectin-susceptibility-and-sporontocidal-effect-in-greater-mekong-subregion-anopheles
#16
Kevin C Kobylinski, Ratawan Ubalee, Alongkot Ponlawat, Chanyapat Nitatsukprasert, Siriporn Phasomkulsolsil, Thanaporn Wattanakul, Joel Tarning, Kesara Na-Bangchang, Patrick W McCardle, Silas A Davidson, Jason H Richardson
BACKGROUND: Novel vector control methods that can directly target outdoor malaria transmission are urgently needed in the Greater Mekong Subregion (GMS) to accelerate malaria elimination and artemisinin resistance containment efforts. Ivermectin mass drug administration (MDA) to humans has been shown to effectively kill wild Anopheles and suppress malaria transmission in West Africa. Preliminary laboratory investigations were performed to determine ivermectin susceptibility and sporontocidal effect in GMS Anopheles malaria vectors coupled with pharmacokinetic models of ivermectin at escalating doses...
July 7, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28686181/how-can-synergism-of-traditional-medicines-benefit-from-network-pharmacology
#17
REVIEW
Haidan Yuan, Qianqian Ma, Heying Cui, Guancheng Liu, Xiaoyan Zhao, Wei Li, Guangchun Piao
Many prescriptions of traditional medicines (TMs), whose efficacy has been tested in clinical practice, have great therapeutic value and represent an excellent resource for drug discovery. Research into single compounds of TMs, such as artemisinin from Artemisia annua L., has achieved great success; however, it has become evident that a TM prescription (which frequently contains various herbs or other components) has a synergistic effect in effecting a cure or reducing toxicity. Network pharmacology targets biological networks and analyzes the links among drugs, targets, and diseases in those networks...
July 7, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28683750/use-of-malaria-rapid-diagnostic-tests-by-community-health-workers-in-afghanistan-cluster-randomised-trial
#18
Toby Leslie, Mark Rowland, Amy Mikhail, Bonnie Cundill, Barbara Willey, Asif Alokozai, Ismail Mayan, Anwar Hasanzai, Sayed Habibullah Baktash, Nader Mohammed, Molly Wood, Habib-U-Rahman Rahimi, Baptiste Laurent, Cyril Buhler, Christopher J M Whitty
BACKGROUND: The World Health Organisation (WHO) recommends parasitological diagnosis of malaria before treatment, but use of malaria rapid diagnostic tests (mRDTs) by community health workers (CHWs) has not been fully tested within health services in south and central Asia. mRDTs could allow CHWs to diagnose malaria accurately, improving treatment of febrile illness. METHODS: A cluster randomised trial in community health services was undertaken in Afghanistan. The primary outcome was the proportion of suspected malaria cases correctly treated for polymerase chain reaction (PCR)-confirmed malaria and PCR negative cases receiving no antimalarial drugs measured at the level of the patient...
July 7, 2017: BMC Medicine
https://www.readbyqxmd.com/read/28683649/in-vitro-and-in-vivo-delivery-of-artemisinin-loaded-pcl-peg-pcl-micelles-and-its-pharmacokinetic-study
#19
Hamidreza Kheiri Manjili, Hojjat Malvandi, Mir Sajjad Mousavi, Elahe Attari, Hossein Danafar
Artemisinin (ART) is a natural anti-malarial sesquiterpene lactone with anticancer properties, but its application is limited because of its low water solubility. To increase the bioavailability and water solubility of ART, we synthesized three series of poly (ɛ-caprolactone)-poly (ethylene glycol)-poly (ɛ-caprolactone) (PCL-PEG-PCL) tri-block copolymers. The structure of the copolymers was characterized by HNMR, FTIR, DSC and GPC techniques. ART was encapsulated inside micelles by a nanoprecipitation method which leading to the formation of ART/PCL-PEG-PCL micelles...
July 7, 2017: Artificial Cells, Nanomedicine, and Biotechnology
https://www.readbyqxmd.com/read/28680367/cost-effectiveness-analysis-of-malaria-interventions-using-disability-adjusted-life-years-a-systematic-review
#20
REVIEW
Resign Gunda, Moses John Chimbari
BACKGROUND: Malaria continues to be a public health problem despite past and on-going control efforts. For sustenance of control efforts to achieve the malaria elimination goal, it is important that the most cost-effective interventions are employed. This paper reviews studies on cost-effectiveness of malaria interventions using disability-adjusted life years. METHODS: A review of literature was conducted through a literature search of international peer-reviewed journals as well as grey literature...
2017: Cost Effectiveness and Resource Allocation: C/E
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