keyword
MENU ▼
Read by QxMD icon Read
search

antimalarial activity

keyword
https://www.readbyqxmd.com/read/27908538/antimalarial-activity-of-novel-4-aminoquinolines-active-against-drug-resistant-strains
#1
Srinivasarao Kondaparla, Awakash Soni, Ashan Manhas, Kumkum Srivastava, Sunil K Puri, S B Katti
In the present study we have synthesized a new class of 4-aminoquinolines and evaluated against Plasmodium falciparum in vitro (3D7-sensitive strain & K1-resistant strain) and Plasmodium yoelii in vivo (N-67 strain). Among the series, eleven compounds (5, 6, 7, 8, 9, 11, 12, 13, 14, 15 and 21) showed superior antimalarial activity against K1 strain as compared to CQ. In addition, all these analogues showed 100% suppression of parasitemia on day 4 in the in vivo mouse model against N-67 strain when administered orally...
November 23, 2016: Bioorganic Chemistry
https://www.readbyqxmd.com/read/27904956/some-nontoxic-metal-based-drugs-for-selected-prevalent-tropical-pathogenic-diseases
#2
REVIEW
Saliu A Amolegbe, Caroline A Akinremi, Sheriff Adewuyi, Amudat Lawal, Mercy O Bamigboye, Joshua A Obaleye
Metal coordination of bioorganic compounds from both natural and synthetic products is not only gaining recognition in drug design and medicinal inorganic chemistry research, also they are being considered in the improvement of the bioactivity of drugs. What is done in this paper is a review of recent advances in the study of coordination-driven drug delivery, i.e., metal-based drugs (MBDs). The role of some late first row transition metal ions namely Fe, Cu and Zn in the biological activities of metallodrugs such as antimalarials and antimicrobials are highlighted...
November 30, 2016: Journal of Biological Inorganic Chemistry: JBIC
https://www.readbyqxmd.com/read/27896925/design-synthesis-and-in-vitro-antiplasmodial-activity-of-some-bisquinolines-against-chloroquine-resistant-strain
#3
Srinivasarao Kondaparla, Pooja Agarwal, Kumkum Srivastava, Sunil K Puri, S B Katti
A series of novel bisquinoline compounds comprising, N(1) -(7-chloroquinolin-4-yl) ethane-1,2-diamine and 7-chloro-N-(2-(piperazin-1-yl)ethyl)quinolin-4-amine connected with 7-chloro-4-aminoquinoline containing various amino acids is described. We have bio-evaluated the compounds against both chloroquine-sensitive (3D7) and chloroquine-resistant (K1) strains of Plasmodium falciparum in vitro. Among the series, compounds 4 and 7 exhibited 1.8 and 10.6 fold superior activity as compared to chloroquine (CQ) (IC50 = 0...
November 29, 2016: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/27896581/secondary-metabolites-of-endophytic-xylaria-species-with-potential-applications-in-medicine-and-agriculture
#4
REVIEW
Martha Lydia Macías-Rubalcava, Rosa Elvira Sánchez-Fernández
Fungal endophytes are important sources of bioactive secondary metabolites. The genus Xylaria Hill (ex Schrank, 1789, Xylariaceae) comprises various endophytic species associated to both vascular and non vascular plants. The secondary metabolites produced by Xylaria species include a variety of volatile and non-volatile compounds. Examples of the former are sesquiterpenoids, esters, and alcohols, among others; and of the latter we find terpenoids, cytochalasins, mellein, alkaloids, polyketides, and aromatic compounds...
January 2017: World Journal of Microbiology & Biotechnology
https://www.readbyqxmd.com/read/27895526/development-of-a-simple-and-specific-direct-competitive-elisa-for-the-determination-of-artesunate-using-an-anti-artesunate-polyclonal-antiserum
#5
Yoshinori Mitsui
BACKGROUND: Since artesunate (ART) became a vital component of artemisinin (ARM)-based combination therapies for the treatment for malaria, counterfeit ART drugs have spread in regions of Southeast Asia and Africa. The consumption of counterfeit ART drugs has resulted in the death of many patients. Thus, evaluating the quality of ART drugs is needed. There are several methods for quantitating the ART content in tablets, the most common being a high-performance liquid chromatography. However, that method is hampered by the need for expensive equipment and a rather time-consuming process of extraction...
2016: Tropical Medicine and Health
https://www.readbyqxmd.com/read/27890637/antiplasmodial-activity-of-heinsia-crinita-rubiaceae-and-identification-of-new-iridoids
#6
P Tshisekedi Tshibangu, P Mutwale Kapepula, M J Kabongo Kapinga, A Tujibikila Mukuta, Dibungi T Kalenda, Alembert T Tchinda, Ange A Mouithys-Mickalad, O Jansen, E Cieckiewicz, M Tits, L Angenot, M Frédérich
ETHNOPHARMACOLOGICAL RELEVANCE: Heinsia crinita is used in traditional medicine for the treatment of febrile illness and erectile dysfunction. Its stem bark powder is found in some peripheral markets in the Democratic Republic of the Congo (DRC) as a remedy against malaria. Investigations were conducted on crude extracts of leaves, fruits and stem barks in view to validate their use and to determine which plant part possesses the best antiplasmodial properties. MATERIALS AND METHODS: Different plant parts were extracted with methanol, ethanol and dichloromethane...
November 24, 2016: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/27889529/antiviral-activities-of-selected-antimalarials-against-dengue-virus-type-2-and-zika-virus
#7
Anuradha Balasubramanian, Tadahisa Teramoto, Amol A Kulkarni, Apurba K Bhattacharjee, Radhakrishnan Padmanabhan
In a previous study, twelve antimalarial compounds, amodiaquine (AQ) and derivatives, were shown to have potent anti-dengue viral (DENV) activity by using the stable DENV2 Renilla luciferase reporter replicon expressing BHK-21 cells, infectivity (plaque), and the qRT-PCR assays. In this study, we performed molecular modeling on these compounds to determine their stereo-electronic properties required for optimal antiviral activity. Based on the similarity of calculated stereo-electronic profiles, specifically the electrostatic potential profiles of the compounds, and in silico screening of related compounds from literature, we identified three additional compounds, Quinacrine (QC), Mefloquine (MQ), and GSK369796...
November 23, 2016: Antiviral Research
https://www.readbyqxmd.com/read/27886049/alkynyl-containing-peptides-of-marine-origin-a-review
#8
REVIEW
Qiu-Ye Chai, Zhen Yang, Hou-Wen Lin, Bing-Nan Han
Since the 1990s, a number of terminal alkynyl residue-containing cyclic/acyclic peptides have been identified from marine organisms, especially cyanobacteria and marine mollusks. This review has presented 66 peptides, which covers over 90% marine peptides with terminal alkynyl fatty acyl units. In fact, more than 90% of these peptides described in the literature are of cyanobacterial origin. Interestingly, all the linear peptides featured with terminal alkyne were solely discovered from marine cyanobacteria...
November 23, 2016: Marine Drugs
https://www.readbyqxmd.com/read/27884822/a-framework-for-remission-in-sle-consensus-findings-from-a-large-international-task-force-on-definitions-of-remission-in-sle-doris
#9
Ronald van Vollenhoven, Alexandre Voskuyl, George Bertsias, Cynthia Aranow, Martin Aringer, Laurent Arnaud, Anca Askanase, Petra Balážová, Eloisa Bonfa, Hendrika Bootsma, Dimitrios Boumpas, Ian Bruce, Ricard Cervera, Ann Clarke, Cindy Coney, Nathalie Costedoat-Chalumeau, László Czirják, Ronald Derksen, Andrea Doria, Thomas Dörner, Rebecca Fischer-Betz, Ruth Fritsch-Stork, Caroline Gordon, Winfried Graninger, Noémi Györi, Frédéric Houssiau, David Isenberg, Soren Jacobsen, David Jayne, Annegret Kuhn, Veronique Le Guern, Kirsten Lerstrøm, Roger Levy, Francinne Machado-Ribeiro, Xavier Mariette, Jamil Missaykeh, Eric Morand, Marta Mosca, Murat Inanc, Sandra Navarra, Irmgard Neumann, Marzena Olesinska, Michelle Petri, Anisur Rahman, Ole Petter Rekvig, Jozef Rovensky, Yehuda Shoenfeld, Josef Smolen, Angela Tincani, Murray Urowitz, Bernadette van Leeuw, Carlos Vasconcelos, Anne Voss, Victoria P Werth, Helena Zakharova, Asad Zoma, Matthias Schneider, Michael Ward
OBJECTIVES: Treat-to-target recommendations have identified 'remission' as a target in systemic lupus erythematosus (SLE), but recognise that there is no universally accepted definition for this. Therefore, we initiated a process to achieve consensus on potential definitions for remission in SLE. METHODS: An international task force of 60 specialists and patient representatives participated in preparatory exercises, a face-to-face meeting and follow-up electronic voting...
November 24, 2016: Annals of the Rheumatic Diseases
https://www.readbyqxmd.com/read/27880887/de-novo-lead-optimization-of-triazine-derivatives-identifies-potent-antimalarials
#10
Ashutosh Shandilya, Nasimul Hoda, Sameena Khan, Ehtesham Jameel, Jitendra Kumar, B Jayaram
Malaria is a life-threatening disease caused by Plasmodium parasites among which Plasmodium falciparum is the most deadly. Due to the widespread resistance of the current antimalarial drugs, intense research efforts are focused on identification of new and potent antimalarials. We report here, a structure based drug discovery strategy for design of a series of effective and novel triazine based antimalarials. The X-ray structure of P. falciparum methyl transferase (PfPMT) is used as a target as it is unique to the parasite...
November 13, 2016: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/27872647/antimalarial-properties-of-aqueous-crude-extracts-of-gynostemma-pentaphyllum-and-moringa-oleifera-leaves-in-combination-with-artesunate-in-plasmodium-berghei-infected-mice
#11
Voravuth Somsak, Preeyanuch Borkaew, Chokdee Klubsri, Kittiyaporn Dondee, Panatda Bootprom, Butsarat Saiphet
Due to the emergence and spread of malaria parasite with resistance to antimalarial drugs, discovery and development of new, safe, and affordable antimalarial are urgently needed. In this respect, medicinal plant extracts are targets to optimize antimalarial actions and restore efficacy of standard antimalarial drugs. The present study was aimed at determining the antimalarial activities of Gynostemma pentaphyllum and Moringa oleifera leaf extracts in combination with artesunate against Plasmodium berghei-infected mice...
2016: Journal of Tropical Medicine
https://www.readbyqxmd.com/read/27867276/ursolic-acid-a-natural-pentacylcic-triterpene-from-ochrosia-elliptica-and-its-role-in-the-management-of-certain-neglected-tropical-diseases
#12
Rola M Labib, Sherif S Ebada, Fadia S Youssef, Mohamed L Ashour, Samir A Ross
BACKGROUND: Leishmaniasis and African trypanosomiasis are recognized as the leading causes of mortality and morbidity with the greatest prevalence in the developing countries. They affect more than one billion of the poorest people on the globe. OBJECTIVE: To find a cheap, affordable, safe, and efficacious antileshmanial and antitrypanosomal natural drug and to elucidate its probable mode of action. MATERIALS AND METHODS: Phytochemical investigation of the non-polar fraction of the methanol extract of leaves of Ochrosia elliptica Labill...
October 2016: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/27867026/artemisinin-and-its-derivatives-in-treating-protozoan-infections-beyond-malaria
#13
REVIEW
Cecilia Shi Ni Loo, Nelson Siu Kei Lam, Deying Yu, Xin-Zhuan Su, Fangli Lu
Many parasitic protozoan diseases continue to rank among the world's greatest global health problems, which are also common among poor populations. Currently available drugs for treatment present drawbacks, urging the need for more effective, safer, and cheaper drugs. Artemisinin (ART) and its derivatives are some of the most important classes of antimalarial agents originally derived from Artemisia annua L. However, besides the outstanding antimalarial and antischistosomal activities, ART and its derivatives also possess activities against other parasitic protozoa...
November 17, 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/27865644/bioactivity-of-topologically-confined-gramicidin-a-dimers
#14
Kirtikumar B Jadhav, Claudia Stein, Oliwia Makarewicz, Gabriele Pradel, Roman J Lichtenecker, Holger Sack, Stefan H Heinemann, Hans-Dieter Arndt
The d-/l-peptide gramicidin A (gA) is well known as a pivotal ion channel model and shows a broad spectrum of bioactivities such as antibiosis, antimalarial activity, as well as hemolysis. We applied inter-chain disulfide bonds to constrain the conformational freedom of gA into parallel and antiparallel dimeric topologies. Albeit the constructs were not found to be monoconformational, CD- and IR-spectroscopic studies suggested that this strategy indeed restricted the conformational space of the d-/l-peptide construct, and that β-helical secondary structures prevail...
November 9, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27863116/a-quinacrine-analogue-selective-against-gastric-cancer-cells-insights-from-biochemical-and-biophysical-studies
#15
Paula Gomes, Ana Gomes, Iva Fernandes, Cátia Teixeira, Nuno Mateus, M João Sottomayor
One of the earliest synthetic antimalarial drugs, quinacrine, was recently reported as interesting for the treatment of acute myeloid leukemia. Inspired by this and similar findings, we evaluated a set of quinacrine analogues against three different cancer cell lines (MKN-28, Caco-2 and MCF-7) and one normal human cell line (HFF-1). All the compounds, previously developed by us as dual-stage antimalarial leads, displayed antiproliferative activity, with one of the set (4b) standing out as selective towards the gastric cancer cell line MKN-28...
November 14, 2016: ChemMedChem
https://www.readbyqxmd.com/read/27859683/s2k-guideline-for-treatment-of-cutaneous-lupus-erythematosus
#16
Annegret Kuhn, Elisabeth Aberer, Zsuzsanna Bata-Csörgő, Marzia Caproni, Andreas Dreher, Camille Frances, Regine Gläser, Hans-Wilhelm Klötgen, Aysche Landmann, Branka Marinovic, Filippa Nyberg, Rodica Olteanu, Annamari Ranki, Jacek C Szepietowski, Beatrix Volc-Platzer
Cutaneous lupus erythematosus (CLE) is a rare inflammatory autoimmune disease with heterogeneous subtypes. To date, no therapeutic agents have been licensed specifically for patients with this disease entity and topical and systemic drugs are mostly used "off-label". The aim of the present guideline was to achieve a broad consensus on treatment strategies for patients with CLE by a European subcommittee, guided by the European Dermatology Forum (EDF) and supported by the European Academy of Dermatology and Venereology (EADV)...
November 15, 2016: Journal of the European Academy of Dermatology and Venereology: JEADV
https://www.readbyqxmd.com/read/27857147/molecular-mechanism-of-action-of-antimalarial-benzoisothiazolones-species-selective-inhibitors-of-the-plasmodium-spp-mep-pathway-enzyme-ispd
#17
Kathryn E Price, Christopher M Armstrong, Leah S Imlay, Dana M Hodge, C Pidathala, Natalie J Roberts, Jooyoung Park, Marwa Mikati, Raman Sharma, Alexandre S Lawrenson, Niraj H Tolia, Neil G Berry, Paul M O'Neill, Audrey R Odom John
The methylerythritol phosphate (MEP) pathway is an essential metabolic pathway found in malaria parasites, but absent in mammals, making it a highly attractive target for the discovery of novel and selective antimalarial therapies. Using high-throughput screening, we have identified 2-phenyl benzo[d]isothiazol-3(2H)-ones as species-selective inhibitors of Plasmodium spp. 2-C-methyl-D-erythritol-4-phosphate cytidyltransferase (IspD), the third catalytic enzyme of the MEP pathway. 2-Phenyl benzo[d]isothiazol-3(2H)-ones display nanomolar inhibitory activity against P...
November 18, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27847337/herb-drug-interaction-of-andrographis-paniculata-nees-extract-and-andrographolide-on-pharmacokinetic-and-pharmacodynamic-of-naproxen-in-rats
#18
Aishwarya Balap, Sathiyanarayanan Lohidasan, Arulmozhi Sinnathambi, Kakasaheb Mahadik
ETHNOPHARMACOLOGICAL RELEVANCE: Andrographis paniculata Nees (Acanthacae) have broad range of pharmacological effects such as hepatoprotective, antifertility, antimalarial, antidiabetic, suppression of various cancer cells and anti-inflammatory properties and is widely used medicinal plant in the traditional Unani and Ayurvedic medicinal systems. Andrographolide (AN) is one of the active constituent of the Andrographis paniculata Nees extract (APE). They have been found in many traditional herbal formulations in India and proven to be effective as anti-inflammatory drug...
November 12, 2016: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/27845882/antiplasmodial-activity-of-the-ethanolic-root-bark-extract-of-icacina-senegalensis-in-mice-infected-by-plasmodium-berghei
#19
Godwin C Akuodor, David-Oku Essien, Julie A Nkorroh, Augustine D Essien, Effiong E Nkanor, Mercy N Ezeunala, Kingsley C Chilaka
BACKGROUND: The root of Icacina senegalensis is used for the treatment of malaria and related conditions in southeastern Nigeria. METHODS: To establish its efficacy, the ethanolic root bark extract was investigated as antiplasmodial agent against Plasmodium berghei in mice. A 4-day suppressive test and the curative effect against established infection models of antiplasmodial studies were used. RESULTS: The root bark extract of I. senegalensis (50, 100, and 200 mg/kg) exhibited a significant (p<0...
November 15, 2016: Journal of Basic and Clinical Physiology and Pharmacology
https://www.readbyqxmd.com/read/27842542/asymptomatic-only-at-first-sight-malaria-infection-among-schoolchildren-in-highland-rwanda
#20
Kevin C Sifft, Dominik Geus, Caritas Mukampunga, Jean Claude Mugisha, Felix Habarugira, Kira Fraundorfer, Claude Bayingana, Jules Ndoli, Irenee Umulisa, Corine Karema, George von Samson-Himmelstjerna, Toni Aebischer, Peter Martus, Augustin Sendegeya, Jean Bosco Gahutu, Frank P Mockenhaupt
BACKGROUND: Plasmodium infection and malaria in school children are increasingly recognized as a relevant public health problem, but data on actual prevalence and health consequences are insufficient. The present study from highland southern Rwanda aimed at estimating infection prevalence among children attending school, at identifying associated factors and at assessing the clinical consequences of these infections. METHODS: In a survey including 12 schools in the Huye district of Rwanda, 1089 children aged 6-10 years were clinically and anthropometrically examined, malaria parasites were diagnosed by microscopy and PCR, haemoglobin concentrations were measured, and socio-economic and behavioural parameters as well as medical histories were obtained...
November 14, 2016: Malaria Journal
keyword
keyword
43150
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"