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https://www.readbyqxmd.com/read/28820713/quality-testing-of-artemisinin-based-antimalarial-drugs-in-myanmar
#1
Suqin Guo, Myat Phone Kyaw, Lishan He, Myo Min, Xiangxue Ning, Wei Zhang, Baomin Wang, Liwang Cui
Artemisinin-based combination therapies are the frontline treatment of Plasmodium falciparum malaria. The circulation of falsified and substandard artemisinin-based antimalarials in Southeast Asia has been a major predicament for the malaria elimination campaign. To provide an update of this situation, we purchased 153 artemisinin-containing antimalarials, as convenience samples, in private drug stores from different regions of Myanmar. The quality of these drugs in terms of their artemisinin derivative content was tested using specific dipsticks for these artemisinin derivatives, as point-of-care devices...
July 31, 2017: American Journal of Tropical Medicine and Hygiene
https://www.readbyqxmd.com/read/28817228/isolation-of-the-new-antiplasmodial-butanolide-malleastrumolide-a-from-a-malleastrum-sp-meliaceae-from-madagascar
#2
Yongle Du, Alexander K Abedi, Ana Lisa Valenciano, Maria L Fernández-Murga, Maria B Cassera, Vincent E Rasamison, Wendy L Applequist, James S Miller, David G I Kingston
An extract of a Malleastrum sp. (Meliaceae) collected in Madagascar by the Madagascar International Cooperative Biodiversity Group was found to have antimalarial activity, with an IC50 value between 2.5 and 5 μg/mL. After purification by liquid-liquid partition, chromatography on a Diaion open column, C-18 SPE and C-18 reverse phase HPLC, the new butanolide malleastrumolide A was isolated. The structure of malleastrumolide A was determined by mass spectrometry, NMR and ECD. The double bond position was determined by cross-metathesis and mass spectrometry...
August 17, 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/28814579/hepatosplenic-schistosomiasis-playing-hide-and-seek-with-an-elusive-parasite
#3
Martin Baekby, Henning Glerup, Katrine Stribolt, Britta Tarp
A 27-year-old man of Eritrean origin presented with persistent left-sided abdominal pain. Initial investigation showed signs of liver fibrosis, portal hypertension and splenomegaly. A diagnosis of hepatosplenic schistosomiasis was suspected on grounds of elevated total IgE, grey area antischistosomiasis antibodies and the high endemic status of his native country. However, repeated microscopy of faecal and urine samples, as well as rectal biopsies, failed to demonstrate schistosomal eggs. Finally, the diagnosis of hepatosplenic schistosomiasis was established through demonstration of a Schistosoma mansoni egg in a liver biopsy taken in an attempt to clarify the cause of the above findings...
August 16, 2017: BMJ Case Reports
https://www.readbyqxmd.com/read/28813147/synthesis-and-evaluation-of-asymmetric-acyclic-nucleoside-bisphosphonates-as-inhibitors-of-plasmodium-falciparum-and-human-hypoxanthine-guanine-xanthine-phosphoribosyltransferase
#4
Petr Špaček, Dianne T Keough, Marina Chavchich, Martin Dracinsky, Zlatko Janeba, Lieve Naesens, Michael D Edstein, Luke W Guddat, Dana Hocková
Acyclic nucleoside bisphosphonates (ANbPs) have previously been shown to be good inhibitors of human hypoxanthine-guanine phosphoribosyltransferase (HGPRT) and Plasmodium falciparum (Pf) hypoxanthine-guanine-xanthine phosphoribosyltransferase (PfHGXPRT). Based on this scaffold, a new series of ANbPs was synthesized. One of these new ANbPs, [3-(guanine-9-yl)-2-((2-phosphonoethoxy)methyl)propoxy]methylphosphonic acid, exhibited Ki values of 6 and 70 nM for human HGPRT and Pf HGXPRT, respectively. These low Ki values were achieved by inserting an extra carbon atom in the linker connecting the N9 atom of guanine to one of the phosphonate groups...
August 16, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28812327/design-and-synthesis-of-terephthalic-acid-based-histone-deacetylase-inhibitors-with-dual-stage-anti-plasmodium-activity
#5
Katharina Stenzel, Ming Jang Chua, Sandra Duffy, Yevgeniya Antonova-Koch, Stephan Meister, Alexandra Hamacher, Matthias U Kassack, Elizabeth A Winzeler, Vicky M Avery, Thomas Kurz, Katherine T Andrews, Finn Kristian Hansen
In this work we aimed to develop parasite-selective HDAC inhibitors with activity against the disease-causing asexual blood stages of Plasmodium as well as causal prophylactic and/or transmission blocking properties. We report the design, synthesis and biological testing of a series of 13 terephthalic acid-based histone deacetylase inhibitors. All compounds showed low cytotoxicity against human embryonic kidney (HEK293) cells (IC50 8 - >51 µM), with 11 also having sub-micromolar in vitro activity against drug-sensitive (3D7) and multi-drug resistant (Dd2) asexual blood stage Plasmodium falciparum parasites (IC50 ~ 0...
August 15, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28810849/in-vitro-antiplasmodial-activity-and-prophylactic-potentials-of-extract-and-fractions-of-trema-orientalis-linn-stem-bark
#6
John Oludele Olanlokun, Oluwole Moses David, Anthony Jide Afolayan
BACKGROUND: Trema orientalis (T. orientalis Linn) has been used in the management of malaria in the western part of Nigeria and despite its application in ethnomedicine, there is dearth of scientific evidence to justify the acclaimed prophylactic antimalarial usage of the plant. The aim of this study is to assess the in vitro antiplasmodial cell-free assay and chemopreventive efficacy of the methanol extract of the stem bark of T. orientalis and its fractions as a prophylactic regimen for malaria prevention...
August 15, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28808396/catechin-isolated-from-garcinia-celebica-leaves-inhibit-plasmodium-falciparum-growth-through-the-induction-of-oxidative-stress
#7
Rizky Abdulah, Eka W Suradji, Anas Subarnas, Unang Supratman, Milyadi Sugijanto, Ajeng Diantini, Keri Lestari, Melisa I Barliana, Shinichiro Kawazu, Hiroshi Koyama
BACKGROUND: Resistance of antimalarial drugs to Plasmodium falciparum has become a major concern in malaria eradication. Although it is also affected by several socioeconomic factors, a new antiplasmodial agent is needed for a global malaria control program. OBJECTIVE: In this study, we attempted to uncover the antiplasmodial properties of Garcinia celebica, an Indonesian medicinal plant, along with the responsible compound and its possible mechanism. MATERIALS AND METHODS: The G...
July 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/28808258/hexahydroquinolines-are-antimalarial-candidates-with-potent-blood-stage-and-transmission-blocking-activity
#8
Manu Vanaerschot, Leonardo Lucantoni, Tao Li, Jill M Combrinck, Andrea Ruecker, T R Santha Kumar, Kelly Rubiano, Pedro E Ferreira, Giulia Siciliano, Sonia Gulati, Philipp P Henrich, Caroline L Ng, James M Murithi, Victoria C Corey, Sandra Duffy, Ori J Lieberman, M Isabel Veiga, Robert E Sinden, Pietro Alano, Michael J Delves, Kim Lee Sim, Elizabeth A Winzeler, Timothy J Egan, Stephen L Hoffman, Vicky M Avery, David A Fidock
Antimalarial compounds with dual therapeutic and transmission-blocking activity are desired as high-value partners for combination therapies. Here, we report the identification and characterization of hexahydroquinolines (HHQs) that show low nanomolar potency against both pathogenic and transmissible intra-erythrocytic forms of the malaria parasite Plasmodium falciparum. This activity translates into potent transmission-blocking potential, as shown by in vitro male gamete formation assays and reduced oocyst infection and prevalence in Anopheles mosquitoes...
August 14, 2017: Nature Microbiology
https://www.readbyqxmd.com/read/28808005/conformational-dynamics-of-1-deoxy-d-xylulose-5-phosphate-synthase-on-ligand-binding-revealed-by-h-d-exchange-ms
#9
Jieyu Zhou, Luying Yang, Alicia DeColli, Caren Freel Meyers, Natalia S Nemeria, Frank Jordan
The enzyme 1-deoxy-d-xylulose 5-phosphate synthase (DXPS) is a key enzyme in the methylerythritol 4-phosphate pathway and is a target for the development of antibiotics, herbicides, and antimalarial drugs. DXPS catalyzes the formation of 1-deoxy-d-xylulose 5-phosphate (DXP), a branch point metabolite in isoprenoid biosynthesis, and is also used in the biosynthesis of thiamin (vitamin B1) and pyridoxal (vitamin B6). Previously, we found that DXPS is unique among the superfamily of thiamin diphosphate (ThDP)-dependent enzymes in stabilizing the predecarboxylation intermediate, C2-alpha-lactyl-thiamin diphosphate (LThDP), which has subsequent decarboxylation that is triggered by d-glyceraldehyde 3-phosphate (GAP)...
August 14, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28807879/apigenin-induced-abcc1-mediated-efflux-of-glutathione-from-mature-erythrocytes-inhibits-the-proliferation-of-plasmodium-falciparum
#10
Ohud Fallatah, Elias Georges
Plasmodium falciparum infection of mature normal erythrocytes leads to heightened oxidative stress that is tolerated in normal but not in erythrocytes from sickle-cell, β-thalassemia, and glucose-6-phosphate dehydrogenase (G6PD) deficiency hosts. In this report, it was of interest to perturb the redox homeostasis of normal erythrocytes through drug-induced active efflux of glutathione via erythrocyte ABCC1 (member of the C- subfamily of the human ATP-binding cassette (ABC) transporters). To achieve this objective, we made use of apigenin, shown previously to activate ABCC1 glutathione efflux in mature erythrocytes...
August 11, 2017: International Journal of Antimicrobial Agents
https://www.readbyqxmd.com/read/28805984/self-medication-misuse-in-the-middle-east-a-systematic-literature-review
#11
REVIEW
Malak M Khalifeh, Nicholas D Moore, Pascale R Salameh
Regulations usually distinguish between prescription-only (POM) and over-the-counter (OTC) medicines. The former requires medical prescription; the latter are available for SM of common minor or easily treated ailments. However, in the Eastern Mediterranean countries, theoretical prescription medicines can easily be purchased without a prescription, as self-medication (SM) resulting in potential misuse and unnecessary risk for patients. The magnitude of this activity is uncertain. The aim of this article, therefore, is to undertake a comprehensive review to identify the different types of medicines that can easily be purchased as SM in Middle East and recognized as misused...
August 2017: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/28804611/antimalarial-evaluation-of-selected-medicinal-plant-extracts-used-in-iranian-traditional-medicine
#12
Mohammad Hossein Feiz Haddad, Hamidreza Mahbodfar, Zahra Zamani, Ali Ramazani
OBJECTIVES: In an attempt to discover new natural active extracts against malaria parasites, the present study evaluated the antiplasmodial properties of selected plants based on Iranian traditional medicine. MATERIALS AND METHODS: Ten plant species found in Iran were selected and collected based on the available literature about the Iranian traditional medicine. The methanolic extracts of these plants were investigated for in vitro antimalarial properties against chloroquine-sensitive (3D7) and multi-drug resistant (K1) strains of Plasmodium falciparum...
April 2017: Iranian Journal of Basic Medical Sciences
https://www.readbyqxmd.com/read/28800458/quinoline-hybrids-and-their-antiplasmodial-and-antimalarial-activities
#13
REVIEW
Yuan-Qiang Hu, Chuan Gao, Shu Zhang, Lei Xu, Zhi Xu, Lian-Shun Feng, Xiang Wu, Feng Zhao
Malaria, in particular infection with P. falciparum (the most lethal of the human malaria parasite species, responsible for nearly one million deaths every year), is one of the most devastating and common infectious disease throughout the world. Beginning with quinine, quinoline containing compounds have long been used in clinical treatment of malaria and remained the mainstays of chemotherapy against malaria. The emergence of P. falciparum strains resistant to almost all antimalarials prompted medicinal chemists and biologists to study their effective replacement with an alternative mechanism of action and new molecules...
July 27, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28796406/diarylpyrazole-ligated-dihydropyrimidine-hybrids-as-potent-non-classical-antifolates-and-their-efficacy-against-plasmodium-falciparum
#14
Jaimin D Bhatt, Chaitanya J Chudasama, Kanuprasad D Patel
A series of diarylpyrazole clubbed dihydropyrimidine derivatives (J1-J30) was synthesized under microwave-assisted heating conditions by employing Biginelli reaction methodology and utilizing triethylammonium acetate both as a catalyst and as reaction medium, leading towards a greener reaction pathway. The synthesized entities were screened for their antimalarial efficacy against a Plasmodium falciparum strain in vitro. The active entities (J9, J15, J21, J25, and J27) obtained out of the in vitro screening were further evaluated for their enzyme inhibitory potency against the Pf-DHFR enzyme in vitro as well as in silico using Glide...
August 10, 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/28795024/chemopreventive-effect-of-artesunate-in-1-2-dimethylhydrazine-induced-rat-colon-carcinogenesis
#15
Sazal Patyar, Rakesh Raman Patyar, Bikash Medhi, Krishan Lal Khanduja
Artesunate (ART) is a semisynthetic derivative of artemisinin. Artemisinin and its derivatives have shown profound cytotoxicity and antitumor activity in addition to antimalarial activity in various studies. As the in vivo chemopreventive efficacy of ART in colon carcinogenesis has not been investigated so far, the aim of the current study was to study the chemopreventive effect of ART in 1,2-dimethylhydrazine (DMH)-induced rat colon carcinogenesis. Animals were divided into four groups (n = 6): Group I - vehicle (1 mM ethylenediaminetetraacetic acid), Group II - DMH (20 mg/kg), Group III - DMH + 5-fluorouracil (81 mg/kg), Group IV - DMH + ART (6...
July 2017: Journal of Advanced Pharmaceutical Technology & Research
https://www.readbyqxmd.com/read/28789907/benzothiazole-analogues-synthesis-characterization-mo-calculations-with-pm6-and-dft-in-silico-studies-and-in-vitro-antimalarial-as-dhfr-inhibitors-and-antimicrobial-activities
#16
Sampark S Thakkar, Parth Thakor, Arabinda Ray, Hiren Doshi, Vasudev R Thakkar
Benzothiazole analogues are of interest due to their potential activity against malarial and microbial infections. In search of suitable antimicrobial and antimalarial agents, we report here the synthesis, characterization and biological activities of benzothiazole analogues (J 1-J 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...
July 29, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28776016/mechanistic-investigation-of-the-specific-anticancer-property-of-artemisinin-and-its-combination-with-aminolevulinic-acid-for-enhanced-anticolorectal-cancer-activity
#17
Jigang Wang, Jianbin Zhang, Yin Shi, Chengchao Xu, Chongjing Zhang, Yin Kwan Wong, Yew Mun Lee, Sanjeev Krishna, Yingke He, Teck Kwang Lim, Weiying Sim, Zi-Chun Hua, Han-Ming Shen, Qingsong Lin
The antimalarial artemisinin (ART) possesses anticancer activity, but its underlying mechanism remains largely unclear. Using a chemical proteomics approach with artemisinin-based activity probes, we identified over 300 specific ART targets. This reveals an anticancer mechanism whereby ART promiscuously targets multiple critical biological pathways and leads to cancer cell death. The specific cytotoxicity of ART against colorectal cancer (CRC) cells rather than normal colon epithelial cells is due to the elevated capacity of heme synthesis in the cancer cells...
July 26, 2017: ACS Central Science
https://www.readbyqxmd.com/read/28775291/antimalarial-troponoids-puberulic-acid-and-viticolins-divergent-synthesis-and-structure-activity-relationship-studies
#18
Goh Sennari, Ryo Saito, Tomoyasu Hirose, Masato Iwatsuki, Aki Ishiyama, Rei Hokari, Kazuhiko Otoguro, Satoshi Ōmura, Toshiaki Sunazuka
Divergent synthesis of antimalarial troponoids, including naturally occurring compounds, some of which were identified and isolated by our group, has been achieved utilizing the total synthetic route of puberulic acid. Structure-activity relationships of natural products and simple troponoids inspired us to explore more detailed properties of this class of compounds. Access to new derivatives was facilitated through intermediate compounds generated during the total synthesis of puberulic acid by a stepwise oxidation-aromatization sequence to provide 7-hydroxytropolones and bromination for conversion of the carboxylic acid moiety...
August 3, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28774427/synthesis-of-antimalarial-amide-analogues-based-on-the-plant-serrulatane-diterpenoid-3-7-8-trihydroxyserrulat-14-en-19-oic-acid
#19
Rohitesh Kumar, Sandra Duffy, Vicky M Avery, Rohan A Davis
A plant-derived natural product scaffold, 3,7,8-trihydroxyserrulat-14-en-19-oic acid (1) was isolated in high yield from the aerial parts of the endemic Australian desert plant Eremophila microtheca. This scaffold (1) was subsequently used in the generation of a series of new amide analogues via a one-pot mixed anhydride amidation using pivaloyl chloride. The structures of all analogues were characterized using MS, NMR, and UV data. The major serrulatane natural products (1-3), isolated from the plant extract, and all amide analogues (6-15) together with several pivaloylated derivatives of 3,7,8-trihydroxyserrulat-14-en-19-oic acid (16-18) were evaluated for their antimalarial activity against 3D7 (chloroquine sensitive) and Dd2 (chloroquine resistant) Plasmodium falciparum strains, and preliminary cytotoxicity data were also acquired using the human embryonic kidney cell line HEK293...
July 15, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28768914/dichotomous-mir-expression-and-immune-responses-following-primary-blood-stage-malaria
#20
Julie G Burel, Simon H Apte, Penny L Groves, Michelle J Boyle, Christine Langer, James G Beeson, James S McCarthy, Denise L Doolan
Clinical responses to infection or vaccination and the development of effective immunity are characterized in humans by a marked interindividual variability. To gain an insight into the factors affecting this variability, we used a controlled human infection system to study early immune events following primary infection of healthy human volunteers with blood-stage Plasmodium falciparum malaria. By day 4 of infection, a dichotomous pattern of high or low expression of a defined set of microRNAs (miRs) emerged in volunteers that correlated with variation in parasite growth rate...
August 3, 2017: JCI Insight
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