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https://www.readbyqxmd.com/read/28644986/designing-novel-inhibitors-against-histone-acetyltransferase-hat-%C3%A2-gcn5-of-plasmodium-falciparum
#1
Amarjeet Kumar, Krishanu Bhowmick, Kunwar Somesh Vikramdeo, Neelima Mondal, Naidu Subbarao, Suman Kumar Dhar
During active proliferation phase of intra-erythrocytic cycle, the genome of P. falciparum is regulated epigenetically and evolutionary conserved parasite-specific histone proteins are extensively acetylated. The reversible process of lysine acetylation, causing transcriptional activation and its deacetylation, causing transcriptional repression is regulated by balanced activities of HATs and HDACs. They are also known to regulate antigenic variations and gametocytic conversion in P. falciparum. These histone modifying enzymes have been identified as potential targets for development of anitmalarials in literature...
June 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28643446/artemisinin-as-an-anticancer-drug-recent-advances-in-target-profiling-and-mechanisms-of-action
#2
REVIEW
Yin Kwan Wong, Chengchao Xu, Karunakaran A Kalesh, Yingke He, Qingsong Lin, W S Fred Wong, Han-Ming Shen, Jigang Wang
Artemisinin and its derivatives (collectively termed as artemisinins) are among the most important and effective antimalarial drugs, with proven safety and efficacy in clinical use. Beyond their antimalarial effects, artemisinins have also been shown to possess selective anticancer properties, demonstrating cytotoxic effects against a wide range of cancer types both in vitro and in vivo. These effects appear to be mediated by artemisinin-induced changes in multiple signaling pathways, interfering simultaneously with multiple hallmarks of cancer...
June 23, 2017: Medicinal Research Reviews
https://www.readbyqxmd.com/read/28642094/investigation-of-the-component-in-artemisia-annua-l-leading-to-enhanced-antiplasmodial-potency-of-artemisinin-via-regulation-of-its-metabolism
#3
Tian-Yu Cai, Yun-Rui Zhang, Jian-Bo Ji, Jie Xing
ETHNOPHARMACOLOGICAL RELEVANCE: The chemical matrix of the herb Artemisia annua L. (A. annua), from which artemisinin (QHS) is isolated, can enhance both the bioavailability and efficacy of QHS. However, the exact mechanism of this synergism remains unknown. The biotransformation of QHS and potential "enzyme inhibitors" in plant matrix could be of great importance in understanding the improved efficacy of QHS in A. annua, which has been limited to the synergism with flavonoid components...
June 19, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28638769/deeper-insight-into-the-six-step-domino-reaction-of-aldehydes-with-malononitrile-and-evaluation-of-antiviral-and-antimalarial-activities-of-the-obtained-bicyclic-products
#4
Christina M Bock, Gangajji Parameshwarappa, Simon Bönisch, Walter Bauer, Corina Hutterer, Maria Leidenberger, Oliver Friedrich, Manfred Marschall, Barbara Kappes, Andreas Görling, Svetlana B Tsogoeva
The straightforward and efficient synthesis of complex aza- and carbobicyclic compounds, which are of importance for medicinal chemistry, is a challenge for modern chemical methodology. An unprecedented metal-free six-step domino reaction of aldehydes with malononitrile was presented in our previous study to provide, in a single operation, these bicyclic nitrogen-containing molecules. Presented here is a deeper investigation of this atom-economical domino process by extending the scope of aldehydes, performing post-modifications of domino products, applying bifunctional organocatalysts and comprehensive NMR studies of selected domino products...
June 2017: ChemistryOpen
https://www.readbyqxmd.com/read/28635544/heparin-new-life-for-an-old-drug
#5
Carlos Raúl Aláez-Versón, Elena Lantero, Xavier Fernàndez-Busquets
Heparin is one of the oldest drugs, which nevertheless remains in widespread clinical use as an inhibitor of blood coagulation. The history of its identification a century ago unfolded amid one of the most fascinating scientific controversies turning around the distribution of credit for its discovery. The composition, purification and structure-function relationship of this naturally occurring glycosaminoglycan regarding its classical role as anticoagulant will be dealt with before proceeding to discuss its therapeutic potential in, among other, inflammatory and infectious disease, cancer treatment, cystic fibrosis and Alzheimer's disease...
June 21, 2017: Nanomedicine
https://www.readbyqxmd.com/read/28635296/benzoxaborole-antimalarial-agents-part-5-lead-optimization-of-novel-amide-pyrazinyloxy-benzoxaboroles-and-identification-of-a-preclinical-candidate
#6
Yong-Kang Zhang, Jacob J Plattner, Eric E Easom, Robert Toms Jacobs, Denghui Guo, Yvonne R Freund, Pamela Berry, Vic Ciaravino, John C L Erve, Philip J Rosenthal, Brice Campo, Francisco-Javier Gamo, Laura M Sanz, Jianxin Cao
Carboxamide pyrazinyloxy benzoxaboroles were investigated with the goal to identify a molecule with satisfactory antimalarial activity, physicochemical properties, pharmacokinetic profile, in vivo efficacy, and safety profile. This optimization effort discovered 46, which met our target candidate profile. Compound 46 had excellent activity against cultured Plasmodium falciparum, and in vivo against P. falciparum and P. berghei in infected mice. It exhibited good PK properties in mouse, rat and dog. It was highly active against other eleven P...
June 21, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28634040/1-2-4-triazole-and-1-3-4-oxadiazole-analogues-synthesis-mo-studies-in-silico-molecular-docking-studies-antimalarial-as-dhfr-inhibitor-and-antimicrobial-activities
#7
Sampark S Thakkar, Parth Thakor, Hiren Doshi, Arabinda Ray
1,2,4-Triazole and 1,3,4-oxadiazole analogues are of interest due to their potential activity against microbial and malarial infections. In search of suitable antimicrobial and antimalarial compounds, we report here the synthesis, characterization and biological activities of 1,2,4-triazole and 1,3,4-oxadiazole analogues (SS 1-SS 10). The molecules were characterized by IR, mass, (1)H NMR, (13)C NMR and elemental analysis. The in vitro antimicrobial activity was investigated against pathogenic strains, the results were explained with the help of DFT and PM6 molecular orbital calculations...
May 27, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28629227/chemical-and-biological-studies-on-cichorium-intybus-l
#8
Dinara Satmbekova, Radhakrishnan Srivedavyasasri, Yerkebulan Orazbekov, Roza Omarova, Ubaidilla Datkhayev, Samir A Ross
Cichorium intybus L. (Asteraceae family) is a world-wide grown plant known as chicory. In traditional medicine, this plant is used as diuretic, anti-inflammatory, digestive, cardiotonic and liver tonic. Chromatographic purification of the supercritical fluid extract of aerial parts of C. intybus on silica gel column led to isolation of three compounds: new compound, 28β-hydroxytaraxasterol (I), and two known compounds usnic acid (II) and β-sitosterol (III). Purification of the ethanolic extract of aerial parts of this plant on silica gel column chromatography yielded four compounds: 1,3-dioleylglycerate (IV), sitoindoside II (V), 11β-13-dihydrolactucin (VI) and β-sitosterol-3-O-glucoside (VII)...
June 19, 2017: Natural Product Research
https://www.readbyqxmd.com/read/28625144/detection-of-poor-quality-artemisinin-based-combination-therapy-act-medicines-marketed-in-benin-using-simple-and-advanced-analytical-techniques
#9
Achille Yemoa, Védaste Habyalimana, Jérémie K Mbinze, Victoria Crickboom, Benjamin Muhigirwa, Agnès Ngoya, Pierre-Yves Sacré, Fernand Gbaguidi, Joëlle Quetin-Leclercq, Philippe Hubert, Roland D Marini
BACKGROUND: Poor quality antimalarial medicines still represent a threat to the public health, especially in Sub-Saharan Africa who bears a disproportionate share of the global burden of malaria. It is essential and urgent to strengthen mechanisms against counterfeit medicines. One of the approaches is regular market surveillance through quality controls. METHODS: 12 samples of artemether/lumefantrine were collected from formal and informal drug sellers in Cotonou (Benin) as well as additional other similar samples from Rwanda (13 samples) and from D...
June 15, 2017: Current Drug Safety
https://www.readbyqxmd.com/read/28621561/a-patent-review-of-two-fruitful-decades-1997-2016-of-isocoumarin-research
#10
Hidayat Hussain, Ivan R Green
Isocoumarins comprise a six-membered oxygen heterocycle (α-pyranone) along with one aromatic ring and are known to possess interesting biological properties. During the last two decade (1997-2016), isocoumarin chemistry has attracted attention due to its biological and pharmaceutical effects viz., anticancer, anti-diabetic, antibacterial, antimalarial, and fungicidal effects. Areas covered: This review covers the patents on the therapeutic activities of natural and synthetic isocoumarins over the last two decades (1997-2016)...
June 16, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28620060/hospitalizations-in-patients-with-systemic-lupus-erythematosus-in-an-academic-health-science-center
#11
Kaien Gu, Dafna D Gladman, Jiandong Su, Murray B Urowitz
OBJECTIVE: Hospitalization occurs in about 10% of patients with systemic lupus erythematosus (SLE) each year and accounts for most of the direct cost of SLE patient care. We aimed to determine the frequency of admissions of patients with SLE and describe their causes and outcomes. METHODS: We identified all hospitalizations at University Health Network in the periods 2011-2012 and 2013-2015 with an International Classification of Diseases, 10th ed. code of M32 (SLE)...
June 15, 2017: Journal of Rheumatology
https://www.readbyqxmd.com/read/28615849/in-vivo-antimalarial-activity-of-aqueous-leaf-and-bark-extracts-of-trema-orientalis-against-plasmodium-berghei-in-mice
#12
Oluwatoyosi Eniola Oyebola, Olajumoke Abimbola Morenikeji, Isaiah Oluwafemi Ademola
The control of malaria relies on the use of chemical antimalarial, but the development of resistance necessitates research into alternatives. Trema orientalis (L.) Blume is used in Nigerian folklore medicine for the treatment of malaria. This study investigates the in vivo antiplasmodial activity of aqueous leaf and bark extracts of T. orientalis in rodent model. Swiss Albino mice weighing 23-27 g were intraperitoneally infected with Plasmodium berghei. The lethal dose in mice was estimated to be greater than 5000 mg/kg based on toxicity signs and death...
June 2017: Journal of Parasitic Diseases: Official Organ of the Indian Society for Parasitology
https://www.readbyqxmd.com/read/28612497/pharmacotherapy-follow-up-role-in-active-malaria-surveillance-in-a-travel-medicine-centre-outside-the-transmission-area-in-brazil
#13
R S Pedro, P Brasil, A Pina-Costa, C R Machado, L S Damasceno, C T Daniel-Ribeiro, L Guaraldo
WHAT IS KNOWN AND OBJECTIVE: Malaria is a potentially severe disease, widespread in tropical and subtropical areas. Apart from parasite drug resistance, which receives the largest share of attention, several factors directly influence the response to antimalarial treatment such as incorrect doses, adverse drug events, lack of adherence to treatment, drug quality and drug-drug interactions. Pharmacotherapy follow-up can be used to monitor and improve the effectiveness of treatment, prevent drug-related problems and ensure patient safety...
June 13, 2017: Journal of Clinical Pharmacy and Therapeutics
https://www.readbyqxmd.com/read/28607017/high-accumulation-and-in-vivo-recycling-of-the-new-antimalarial-albitiazolium-rapidly-condemn-the-parasite-to-death
#14
Sharon Wein, Nicolas Taudon, Marjorie Maynadier, Christophe Tran Van Ba, Delphine Margout, Yann Bordat, Laurent Fraisse, Kai Wengelnik, Rachel Cerdan, Françoise Bressolle-Gomeni, Henri J Vial
Albitiazolium is the lead compound of bis-thiazolium choline analogues and exerts powerful in vitro and in vivo antimalarial activities. Here we provide new insight into the fate of albitiazolium in vivo in mice and how it exerts its pharmacological activity. We show that the drug exhibits a rapid and potent activity and has very favorable pharmacokinetic and pharmacodynamic properties. Pharmacokinetic studies in Plasmodium vinckei-infected mice indicated that albitiazolium rapidly and specifically accumulates to a great extent (cellular accumulation ratio > 150) in infected erythrocytes...
June 12, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28601510/synthesis-and-evaluation-of-symmetric-acyclic-nucleoside-bisphosphonates-as-inhibitors-of-the-plasmodium-falciparum-plasmodium-vivax-and-human-6-oxopurine-phosphoribosyltransferases-and-the-antimalarial-activity-of-their-prodrugs
#15
Petr Špaček, Dianne T Keough, Marina Chavchich, Martin Dračínský, Zlatko Janeba, Lieve Naesens, Michael D Edstein, Luke W Guddat, Dana Hocková
Two new series of symmetric acyclic nucleoside bisphosphonates (ANbPs) have been synthesised as potential inhibitors of the Plasmodium falciparum (Pf) and vivax (Pv) 6-oxopurine phosphoribosyltransferases. The structural variability between these symmetric ANbPs lies in the number of atoms in the two acyclic linkers connecting the N(9) atom of the purine base to each of two phosphonate groups and the branching point of the acyclic moiety relative to the purine base, which occurs at either the alpha or beta positions...
May 24, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28599096/proteases-as-antimalarial-targets-strategies-for-genetic-chemical-and-therapeutic-validation
#16
REVIEW
Edgar Deu
Malaria is a devastating parasitic disease affecting half of the world's population. The rapid emergence of resistance against new antimalarial drugs, including artemisinin-based therapies, has made the development of drugs with novel mechanisms of action extremely urgent. Proteases are enzymes proven to be well suited for target-based drug development due to our knowledge of their enzymatic mechanisms and active site structures. More importantly, Plasmodium proteases have been shown to be involved in a variety of pathways that are essential for parasite survival...
June 9, 2017: FEBS Journal
https://www.readbyqxmd.com/read/28597191/theoretical-analysis-of-the-binding-of-iron-iii-protoporphyrin-ix-to-4-methoxyacetophenone-thiosemicarbazone-via-dft-d3-mep-qtaim-nci-elf-and-lol-studies
#17
Nyiang Kennet Nkungli, Julius Numbonui Ghogomu
Thiosemicarbazones display diverse pharmacological properties, including antimalarial activities. Their pharmacological activities have been studied in depth, but little of this research has focused on their antimalarial mode of action. To elucidate this antimalarial mechanism, we investigated the nature of the interactions between iron(III) protoporphyrin IX (Fe(III)PPIX) and the thione-thiol tautomers of 4-methoxyacetophenone thiosemicarbazone (MAPTSC). Dispersion-corrected density functional theory (DFT-D3), the quantum theory of atoms in molecules (QTAIM), the noncovalent interaction (NCI) index, the electron localization function (ELF), the localized orbital locator (LOL), and thermodynamic calculations were employed in this work...
July 2017: Journal of Molecular Modeling
https://www.readbyqxmd.com/read/28595540/apicoplast-import-protein-tic20-a-promising-therapeutic-molecular-target-for-plasmodium-falciparum-an-insilico-approach-for-therapeutic-intervention
#18
Pavan C P K Srimath-Tirumala-Peddinti, Sandeep Solmon Kusuma, Deepthi Nammi, Nageswara Rao Reddy Neelapu
Malaria is a lethal disease causing mortality to over millions each year. Drug resistance in the malarial parasite encouraged to discover effective antimalarial drug targets and drugs. An objective of this current study is to identify drug targets for malarial parasite. Genes unique, non-homologous to humans and essential for parasite are identified using BLASTn by comparing genomes between parasite and host. Further open BLASTp was used to filter the targets specific to Plasmodium species and later were subjected to gene property analysis to identify 65 potential targets...
June 5, 2017: Infectious Disorders Drug Targets
https://www.readbyqxmd.com/read/28589322/comparison-of-systemic-lupus-erythematosus-sle-patients-managed-early-after-diagnosis-in-specialty-versus-community-care-clinics
#19
Roaa Aljohani, Dafna D Gladman, Jiandong Su, Murray B Urowitz
To compare management and outcomes of SLE patients treated in community clinics (Cc) with those treated in specialty clinic (Sc) within 10 years after SLE diagnosis. A single-center, matched cohort study design was used. We identified 54 SLE patients who were referred to a Sc from Cc within 5 years of SLE diagnosis, and 101 inception SLE patients who followed in a Sc. Patients in Cc were matched 1:2 based on gender, decade of SLE diagnosis, and age at diagnosis within 3 years with Sc patients. Disease characteristics, damage accumulation, death, cardiovascular (CVS) risk factors, and events were compared at 5 and 10 years of disease...
June 6, 2017: Clinical Rheumatology
https://www.readbyqxmd.com/read/28588941/physicochemical-equivalence-of-generic-antihypertensive-medicines-equimeds-protocol-for-a-quality-of-medicines-assessment
#20
Julie Redfern, Rufus Adesoji Adedoyin, Sandra Ofori, Raghupathy Anchala, Vamadevan S Ajay, Luciano De Andrade, Jose Zelaya, Harparkash Kaur, Dina Balabanova, Mahmoud U Sani
BACKGROUND: Prevention and optimal management of hypertension in the general population is paramount to the achievement of the World Heart Federation (WHF) goal of reducing premature cardiovascular disease (CVD) mortality by 25% by the year 2025 and widespread access to good quality antihypertensive medicines is a critical component for achieving the goal. Despite research and evidence relating to other medicines such as antimalarials and antibiotics, there is very little known about the quality of generic antihypertensive medicines in low-income and middle-income countries...
August 2016: BMJ Global Health
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