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https://www.readbyqxmd.com/read/28728995/a-mechanistic-model-quantifies-artemisinin-induced-parasite-growth-retardation-in-blood-stage-plasmodium-falciparum-infection
#1
Pengxing Cao, Nectarios Klonis, Sophie Zaloumis, David S Khoury, Deborah Cromer, Miles P Davenport, Leann Tilley, Julie A Simpson, James M McCaw
Falciparum malaria is a major parasitic disease causing widespread morbidity and mortality globally. Artemisinin derivatives-the most effective and widely-used antimalarials that have helped reduce the burden of malaria by 60% in some areas over the past decade-have recently been found to induce growth retardation of blood-stage Plasmodium falciparum when applied at clinically relevant concentrations. To date, no model has been designed to quantify the growth retardation effect and to predict the influence of this property on in vivo parasite killing...
July 18, 2017: Journal of Theoretical Biology
https://www.readbyqxmd.com/read/28728898/kbe009-an-antimalarial-bestatin-like-inhibitor-of-the-plasmodium-falciparum-m1-aminopeptidase-discovered-in-an-ugi-multicomponent-reaction-derived-peptidomimetic-library
#2
Jorge González-Bacerio, Sarah El Chamy Maluf, Yanira Méndez, Isel Pascual, Isabelle Florent, Pollyana M S Melo, Alexandre Budu, Juliana C Ferreira, Ernesto Moreno, Adriana K Carmona, Daniel G Rivera, Maday Alonso Del Rivero, Marcos L Gazarini
Malaria is a global human parasitic disease mainly caused by the protozoon Plasmodium falciparum. Increased parasite resistance to current drugs determines the relevance of finding new treatments against new targets. A novel target is the M1 alanyl-aminopeptidase from P. falciparum (PfA-M1), which is essential for parasite development in human erythrocytes and is inhibited by the pseudo-peptide bestatin. In this work, we used a combinatorial multicomponent approach to produce a library of peptidomimetics and screened it for the inhibition of recombinant PfA-M1 (rPfA-M1) and the in vitro growth of P...
July 4, 2017: Bioorganic & Medicinal Chemistry
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/28720134/in-vitro-antioxidant-and-antimalarial-activities-of-leaves-pods-and-bark-extracts-of-acacia-nilotica-l-del
#4
Muhammad Bilal Sadiq, Pattamon Tharaphan, Kesinee Chotivanich, Joel Tarning, Anil Kumar Anal
BACKGROUND: The emergence of drug resistant malaria is threatening our ability to treat and control malaria in the Southeast Asian region. There is an urgent need to develop novel and chemically diverse antimalarial drugs. This study aimed at evaluating the antimalarial and antioxidant potentials of Acacia nilotica plant extracts. METHODS: The antioxidant activities of leaves, pods and bark extracts were determined by standard antioxidant assays; reducing power capacity, % lipid peroxidation inhibition and ferric reducing antioxidant power assay...
July 18, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28719294/molecular-markers-for-sensitive-detection-of-plasmodium-falciparum-asexual-stage-parasites-and-their-application-in-a-malaria-clinical-trial
#5
Fitsum G Tadesse, Kjerstin Lanke, Issa Nebie, Jodie A Schildkraut, Bronner P Gonçalves, Alfred B Tiono, Robert Sauerwein, Chris Drakeley, Teun Bousema, Sanna R Rijpma
Plasmodium falciparum parasite life stages respond differently to antimalarial drugs. Sensitive stage-specific molecular assays may help to examine parasite dynamics at microscopically detectable and submicroscopic parasite densities in epidemiological and clinical studies. In this study, we compared the performance of skeleton-binding protein 1 (SBP1), ring-infected erythrocyte surface antigen, Hyp8, ring-exported protein 1 (REX1), and PHISTb mRNA for detecting ring-stage trophozoite-specific transcripts using quantitative reverse transcriptase polymerase chain reaction...
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
#6
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/28712788/antimalarial-agent-artesunate-protects-concanavalin-a-induced-autoimmune-hepatitis-in-mice-by-inhibiting-inflammatory-responses
#7
Xin Zhao, MingJiang Liu, JinGui Li, ShaoJie Yin, YangYang Wu, AnYuan Wang
The anti-malarial drug artesunate (ARS) has been shown to possess anti-inflammatory activity. Its effect on autoimmune hepatitis remains unclear. Concanavalin A (Con A)-induced hepatitis was used in this study to reveal the potential action of ARS and the related mechanism. Mice were pretreated with ARS followed by Con A challenge. Con A caused obvious hepatic injury with higher levels of liver enzymes, elevated pro-inflammatory cytokines and activation of nuclear factor-κB (NF-κB) and mitogen activated protein kinase (MAPK) signaling pathways...
July 13, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28710808/the-application-of-physiologically-based-pharmacokinetic-modelling-to-assess-the-impact-of-antiretroviral-mediated-drug-drug-interactions-on-piperaquine-antimalarial-therapy-during-pregnancy
#8
Olusola Olafuyi, Michael Coleman, Raj K S Badhan
Antimalarial therapy during pregnancy poses important safety concerns due to potential teratogenicity and maternal physiological and biochemical changes during gestation. Piperaquine (PQ) has gained interest for use in pregnancy in response to increasing resistance towards sulfadoxine-pyrimethamine in sub-Saharan Africa. Co-infection with HIV is common in many developing countries, however, little is known about the impact of anti-retroviral (ARV) mediated drug-drug interaction (DDI) on PQ pharmacokinetics during pregnancy...
July 14, 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28709400/broad-range-potential-of-asphodelus-microcarpus-leaves-extract-for-drug-development
#9
Amalia Di Petrillo, Antonella Fais, Francesca Pintus, Celestino Santos-Buelga, Ana M González-Paramás, Vincenzo Piras, Germano Orrù, Antonello Mameli, Enzo Tramontano, Aldo Frau
BACKGROUND: Many plants have been used in traditional medicine for their antibacterial, antifungal, antiprotozoal, antiviral, antidiarrhoeal, analgesic, antimalarial, antioxidant, anti-inflammatory and anticancer activities. In order to find novel antimicrobial and antiviral agents, the aim of the present study was the evaluation of the antibacterial and antibiofilm susceptibility of Asphodelus microcarpus leaves extract. Moreover, the antiviral activity and the phytochemical composition of the active extract were also determined...
July 14, 2017: BMC Microbiology
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
#10
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/28705498/-hepatonephritis-during-the-treatment-of-malaria-by-the-therapeutic-combinations-from-a-pharmacovigilance-database
#11
Mamadou Kamagaté, Check Oumar Diallo, David Meless, Thérèse Daubrey-Potey, Augustine Kakou, Éric Balayssac, Kanga Sita N'zue, Jean Claude Yavo, Henri Die-Kakou
INTRODUCTION: Prior studies have shown an association between the onset of hepatonephritis and the use of arteminisin-based combination therapy (ACT) during the treatment of uncomplicated malaria. The objective of this study was to identify the risk factors of hepatonephritis occurrence because of the uncertainty regarding the appearance and the aggravation of this syndrome. METHODS: A case-non case study was carried out on 428 notifications of pharmacovigilance extracted from the database of the clinical pharmacology department of the teaching hospital of Cocody from 2008 to 2012...
April 6, 2017: Thérapie
https://www.readbyqxmd.com/read/28697223/treatment-of-annular-elastolytic-giant-cell-granuloma-with-topical-tretinoin
#12
Aubrey Wagenseller, Cecilia Larocca, Neelam A Vashi
<p>Annular elastolytic giant cell granuloma, also known as actinic granuloma, is a rare skin condition with a chronic course that is often resistant to treatment. Literature is sparse, and only a handful of case reports are available to guide treatment decisions. Typical first line treatment options include topical and intralesional steroids, topical pimecrolimus, and cryotherapy. Resistant cases have been treated with cyclosporine, systemic steroids, antimalarials, and oral retinoids. In particular, acitretin and isotretinoin have shown success in three cases...
July 1, 2017: Journal of Drugs in Dermatology: JDD
https://www.readbyqxmd.com/read/28696697/development-of-a-potent-inhibitor-of-the-plasmodium-proteasome-with-reduced-mammalian-toxicity
#13
Gregory M LaMonte, Jehad Almaliti, Betsaida Bibo-Verdugo, Lena Keller, Bing Yu Zou, Jennifer Yang, Yevgeniya Antonova-Koch, Pamela Orjuela-Sanchez, Colleen A Boyle, Edgar Vigil, Lawrence Wang, Gregory M Goldgof, Lena Gerwick, Anthony J O'Donoghue, Elizabeth A Winzeler, William H Gerwick, Sabine Ottilie
Naturally derived chemical compounds are the foundation of much of our pharmacopeia, especially in anti-proliferative and anti-infective drug classes. Here, we report that a naturally-derived molecule called carmaphycin B, is a potent inhibitor against both the asexual and sexual blood stages of malaria infection. Using a combination of in silico molecular docking and in vitro directed evolution in a well-characterized drug-sensitive yeast model, we determined that these compounds target the β5 subunit of the proteasome...
July 11, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28695837/a-case-of-cerebral-malaria-managed-by-erythrocyte-exchange
#14
Gürsel Ersan, Işıl Köse, Fatma Liv, Bengü Gireniz Tatar, Şükran Köse
Plasmodium falciparum may cause serious and sometimes even fatal cerebral malaria. Cerebral malaria is a disease characterized by alterations in consciousness and epileptic attacks; therefore, it requires a rapid evaluation and quick intervention. It may progress to a fatal outcome despite administering targeted therapeutic interventions. There are studies indicating that erythrocyte exchange (erythrocytapheresis) can be a treatment modality for managing severe malaria patients. In this case report, the successful management of a cerebral malaria patient by the combination of antimalarial drug therapy and erythrocyte exchange is presented...
June 2017: Türkiye Parazitolojii Dergisi
https://www.readbyqxmd.com/read/28694195/hemoglobins-emerging-roles-in-mental-disorders-metabolical-genetical-and-immunological-aspects
#15
REVIEW
Meric A Altinoz, Bahri Ince
Hemoglobin (Hb) expression in the central nervous system is recently shown. Cooccurences of mental disorders (mainly bipolar disorder (BD) and tic disorders) with β- or α-thalassemia trait or erythrocytosis were witnessed, which may be due to peripheral or central hypoxia/hyperoxia or haplotypal gene interactions. β-Globin genes reside at 11p15.5 close to tyrosine hydroxylase, dopamine receptor DRD4 and Brain Derived Neurotrophic Factor, which involve in psychiatric diseases. α-Globin genes reside at 16p13...
July 8, 2017: International Journal of Developmental Neuroscience
https://www.readbyqxmd.com/read/28690382/qsar-based-predictive-modeling-for-anti-malarial-molecules
#16
Deepak R Bharti, Andrew M Lynn
Malaria is a predominant infectious disease, with a global footprint, but especially severe in developing countries in the African subcontinent. In recent years, drug-resistant malaria has become an alarming factor, and hence the requirement of new and improved drugs is more crucial than ever before. One of the promising locations for antimalarial drug target is the apicoplast, as this organelle does not occur in humans. The apicoplast is associated with many unique and essential pathways in many Apicomplexan pathogens, including Plasmodium...
2017: Bioinformation
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
#17
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/28689414/the-effects-of-quinoline-and-non-quinoline-inhibitors-on-the-kinetics-of-lipid-mediated-%C3%AE-hematin-crystallization
#18
Sharne-Mare Fitzroy, Johandie Gildenhuys, Tania Olivier, Ndivhuwo Olga Tshililo, David Kuter, Katherine Allison de Villiers
The throughput of a biomimetic lipid-mediated assay used to investigate the effects of inhibitors on the kinetics of β-hematin formation has been optimized through the use of 24-well microplates. The rate constant for β-hematin formation mediated by monopalmitoyl-rac-glycerol was reduced from 0.17 ± 0.04 min-1 previously measured in Falcon tubes to 0.019 ± 0.002 min-1 in the optimized assay. While this necessitated longer incubation times, transferring aliquots from multiple 24-well plates to a single 96-well plate for final absorbance measurements actually improved the overall turnaround time per inhibitor...
July 10, 2017: Langmuir: the ACS Journal of Surfaces and Colloids
https://www.readbyqxmd.com/read/28689253/effect-of-arteether-and-pyrimethamine-coadministration-on-the-pharmacokinetic-and-pharmacodynamic-profile-of-ormeloxifene
#19
Abhisheak Sharma, Swati Jaiswal, Mahendra Shukla, Jawahar Lal
The study was intended to investigate the effect of concomitant administration of antimalarial drug (pyrimethamine or arteether) on pharmacokinetic and post coitus contraceptive efficacy of ormeloxifene in female Sprague-Dawley rats. A serial sampling technique coupled with LC-MS/MS detection was utilized for quantification of ormeloxifene in plasma samples collected from female rats treated with ormeloxifene only and ormeloxifene with pyrimethamine or arteether. Coitus-proven female rats were utilized to investigate the effect of pyrimethamine or arteether coadministration on contraceptive efficacy of ormeloxifene by investigating the presence or absence of implantations and status of corpora lutea on day 10 post coitum...
July 8, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28688800/protein-degradation-systems-as-antimalarial-therapeutic-targets
#20
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
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