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antimalarial activity

Jing Li, Chao Zhang, Muxin Gong, Manyuan Wang
Currently, the most effective antimalarial is artemisinin, which is extracted from the leaves of medicinal herb Artemisia annua L. (A. annua). Previous studies showed that the complex chemical matrix of A. annua could enhance both the bioavailability and efficacy of artemisinin. The present study aims to evaluate the efficacy and pharmacokinetic properties of a combination therapy based on artemisinin and 3 components from A. annua with high content (arteannuin B, arteannuic acid, and scopoletin). In vivo antimalarial activity was assessed following a 4-day treatment in murine malaria models (Plasmodium yoelii and Plasmodium berghei)...
April 15, 2018: Phytotherapy Research: PTR
Peter J Sadler, Prinessa Chellan, Vicky Avery, Sandra Duffy, James Triccas, Gayathri Nagalingam, Christina Tam, Luisa Cheng, Jenny Liu, Kirkwood Land, Guy Clarkson, Isolda Romero
Fourteen novel arene RuII, and cyclopentadienyl (Cpx) RhIII and IrIII complexes containing an N,N'-chelated pyridylimino- or quinolylimino ligand functionalized with the antimalarial drug sulfadoxine have been synthesized and characterized, including three by x-ray crystallography. Rhodium and iridium complexes exhibited potent antiplasmodial activity with IC50 values of 0.10 - 2.0 µM in either all, or one of the three Plasmodium falciparum assays (3D7 chloroquine sensitive, Dd2 chloroquine resistant and NF54 sexual late stage gametocytes), but were only moderately active towards Trichomonas vaginalis...
April 13, 2018: Chemistry: a European Journal
Guo-Fei Qin, Xu-Li Tang, Yan-Ting Sun, Xiang-Chao Luo, Jing Zhang, Leen van Ofwegen, Ping-Jyun Sung, Ping-Lin Li, Guo-Qiang Li
Three new sesquiterpenoids (sinuketal ( 1 ), sinulins A and B ( 2 and 3 )) and two new cembranoids (sinulins C and D ( 4 and 5 )), as well as eight known sesquiterpenoids ( 6–13 ) and eight known cembranoids ( 14–21 ), were isolated from the Xisha soft coral Sinularia sp. Their structures were elucidated by extensive spectroscopic analysis. Compound 1 possesses an unprecedented isopropyl-branched bicyclo [6.3.0] undecane carbon skeleton with unique endoperoxide moiety, and a plausible biosynthetic pathway of it was postulated...
April 13, 2018: Marine Drugs
Mariáurea Matias Sarandy, Lyvia Lopes Miranda, Luciana Schulthais Altoé, Rômulo Dias Novaes, Virgínia Vinha Zanuncio, João Paulo Viana Leite, Reggiani Vilela Gonçalves
Natural substances are used in folk medicines to treat injuries. Strychnos pseudoquina has scarring, antipyretic, and antimalarial actions. The present study aimed to analyze the effect of S. pseudoquina on cutaneous wound healing in rats. The S. pseudoquina extract was submitted to phytochemical prospection. The levels of flavonoids and total phenolic compounds in the extract were 50.7 mg/g and 2.59 mg/g, respectively. Thirty Wistar rats were individualized in cages with food and water ad libitum (registration no...
2018: PloS One
Helen Byomire Ndagije, Victoria Nambasa, Leonard Manirakiza, Donna Kusemererwa, Dan Kajungu, Sten Olsson, Niko Speybroeck
INTRODUCTION: Uganda has rapidly increased access to antimalarial medicines in an effort to address the huge malaria disease burden. Pharmacovigilance information is important to guide policy decisions. OBJECTIVES: The purpose of this study was to establish the burden of adverse drug reactions (ADRs) and associated risk factors for developing ADRs to artemisinin-based antimalarial treatment in Uganda. METHODS: An active follow-up study was conducted between April and July 2017 in a cohort of patients receiving treatment for uncomplicated malaria in the Iganga, Mayuge, and Kampala districts...
April 7, 2018: Drug Safety: An International Journal of Medical Toxicology and Drug Experience
Yinneth Victoria Rodríguez, Maria Helena Arias, José Octavio García, Eric Deharo, Giovanny Garavito
ETHNOPHARMACOLOGICAL RELEVANCE: In the Leticia-Amazonas area, Uitoto indigenous people use a preparation of Curarea toxicofera (Wedd) Barneby & Krukoff (Menispermaceae) combined with prescribed medications to prevent and treat malaria. AIM OF STUDY: To determine the in vitro and in vivo antiplasmodial activity of traditional preparations of Curarea toxicofera alone and in combination with classical antimalarials. MATERIAL AND METHODS: The traditional preparation was evaluated in vitro against P...
April 4, 2018: Journal of Ethnopharmacology
Hangjun Ke, Swati Dass, Joanne M Morrisey, Michael W Mather, Akhil B Vaidya
The phylum Apicomplexa contains a group of protozoan causing diseases in humans and livestock. Plasmodium spp. , the causative agent of malaria, contains a mitochondrion that is very divergent from that of their hosts. The malarial mitochondrion is a clinically validated target for the antimalarial drug atovaquone, which specifically blocks the electron transfer activity of the bc1 complex of the mitochondrial electron transport chain (mtETC). Most mtETC proteins are nuclear-encoded and imported from the cytosol, but three key protein subunits are encoded in the Plasmodium mitochondrial genome: cyt b, COXI, and COXIII...
April 6, 2018: Journal of Biological Chemistry
Eric Yu, Hari P R Mangunuru, Nakul S Telang, Caleb J Kong, Jenson Verghese, Stanley E Gilliland Iii, Saeed Ahmad, Raymond N Dominey, B Frank Gupton
Numerous synthetic methods for the continuous preparation of fine chemicals and active pharmaceutical ingredients (API's) have been reported in recent years resulting in a dramatic improvement in process efficiencies. Herein we report a highly efficient continuous synthesis of the antimalarial drug hydroxychloroquine (HCQ). Key improvements in the new process include the elimination of protecting groups with an overall yield improvement of 52% over the current commercial process. The continuous process employs a combination of packed bed reactors with continuous stirred tank reactors for the direct conversion of the starting materials to the product...
2018: Beilstein Journal of Organic Chemistry
Nittiya Chowchaikong, Sirinun Nilwarangkoon, Surat Laphookhieo, Chantra Tanunyutthawongse, Ramida Watanapokasin
Colorectal cancer, which is the third most common type of cancer diagnosed in both men and women, is the leading cause of cancer-related deaths worldwide. Cowanin is a pure compound extracted from Garcinia cowa Roxb., a tree species present in Thailand, Malaysia and Myanmar. The crude extract has been demonstrated to have antitumor activity, inflammation induction, antibacterial activity, anti-inflammatory activity and antimalarial activity. In the present study, the effects of cowanin on apoptosis induction and on the apoptosis-related and mitogen-activated protein kinase (MAPK) pathways were investigated in the LoVo human colorectal cancer cell line...
April 3, 2018: International Journal of Oncology
Wiwied Ekasari, Tutik Sri Wahyuni, Heny Arwaty, Nindya T Putri
Background: The preliminary study on antimalarial activity of the ethanol extract of Cassia spectabilis leaves against Plasmodium berghei has been carried out by in vivo experiment. It was demonstrated that ethanol extract of C. spectabilis leaves could inhibit growth of rodent malaria parasite P. berghei by 59.29 % (at a dose of 100 mg/kg bodyweight). However, further investigation is required to determine an effective dose of the administered extract for a higher inhibitory effect and increasing effectiveness of the extract...
2018: African Journal of Infectious Diseases
Abdel J Njouendou, Fanny F Fombad, Maeghan O'Neill, Denis Zofou, Chuck Nutting, Patrick C Ndongmo, Arnaud J Kengne-Ouafo, Timothy G Geary, Charles D Mackenzie, Samuel Wanji
BACKGROUND: Co-infection with loiasis remains a potential problem in control programs targeting filarial infections. The effects of many anti-parasitic drugs often administered to Loa loa infected people are not well documented. This study compared the in vitro activity of several of these drugs on the viability of L. loa microfilariae (mf). METHODS: Human strain L. loa mf were isolated from baboon blood using iso-osmotic Percoll gradient, and cultured in RPMI 1640/10% FBS with antimalarial drugs (mefloquine, amodiaquine, artesunate, chloroquine and quinine), anthelmintics (ivermectin, praziquantel, flubendazole and its reduced and hydrolyzed metabolites), two potential trypanocidal agents (fexinidazole and Scynexis-7158) and the anticancer drug imatinib...
April 4, 2018: Parasites & Vectors
Ari D Johnson, Oumar Thiero, Caroline Whidden, Belco Poudiougou, Djoumé Diakité, Fousséni Traoré, Salif Samaké, Diakalia Koné, Ibrahim Cissé, Kassoum Kayentao
The majority of the world's population lives in urban areas, and regions with the highest under-five mortality rates are urbanising rapidly. This 7-year interrupted time series study measured early access to care and under-five mortality over the course of a proactive community case management (ProCCM) intervention in periurban Mali. Using a cluster-based, population-weighted sampling methodology, we conducted independent cross-sectional household surveys at baseline and at 12, 24, 36, 48, 60, 72 and 84 months later in the intervention area...
2018: BMJ Global Health
Anita Wnętrzak, Katarzyna Makyła-Juzak, Anna Chachaj-Brekiesz, Ewelina Lipiec, Nuria Vila Romeu, Patrycja Dynarowicz-Latka
Cyclosporin A (CsA), a hydrophobic peptide, mainly known for its immunosuppressant properties, has shown a broad range of biological activities, including antimalarial action. Since CsA was found to be active on membrane level, it was subjected for investigations involving membrane models. Our former studies on interactions between CsA and different membrane lipids using Langmuir monolayer technique indicated its affinity for sphingomyelin (SM). Inspired by this finding we have extended our experiments on multicomponent systems and performed systematic investigations of CsA behavior towards artificial membranes containing different mutual proportion of sphingomyelin and cholesterol (Chol)...
March 26, 2018: Colloids and Surfaces. B, Biointerfaces
Denise Diedrich, Andreia C Wildner, Thayse F Silveira, Gloria N S Silva, Francine Dos Santos, Vanessa Petry do Canto, Grace Gosmann, Ana Maria Bergold, Aline R Zimmer, Paulo A Netz, Simone C B Gnoatto
Malaria is one of the most significant infectious diseases that affect poor populations in tropical areas throughout the world. Plants have been shown to be a good source for the development of new antimalarial chemotherapeutic agents, as shown for the discovery of quinine and artemisinin derivatives. Our research group has been working with semisynthetic triterpene derivatives that show potential antimalarial activity toward different strains of Plasmodium falciparum by specifically modulating calcium pathways in the parasite...
March 28, 2018: Chemico-biological Interactions
Himangini, Dharam Pal Pathak, Vidushi Sharma, Sachin Kumar
Coumarin containing pyrazoline derivatives have been synthesized and tested as inhibitors of in vitro development of a chloroquine-sensitive (MRC-02) and chloroquine-resistant (RKL-2) strain of Plasmodium falciparum and in vivo Plasmodium berghei malaria. Docking study was also done on cysteine protease falcipain-2 which showed that the binding pose of C-14 molecule and epoxysuccinate, inhibitor of falcipain-2, binds in the similar pattern. The most active antimalarial compound was 3-(1-benzoyl-5-(4-flurophenyl)-4,5-dihydro-1H-pyrazol-3yl)-7-(diethyamino)-2H-chromen-2-one C-14, with an IC50 of 4...
March 22, 2018: Bioorganic & Medicinal Chemistry Letters
Jose Maria Bueno, Felix Calderon, Jesús Chicharro, Juan Carlos de la Rosa, Beatriz Diaz, Jorge Fernandez, Jose M Fiandor, María Teresa Fraile, Mercedes Garcia, Esperanza Herreros, Adolfo García-Pérez, Milagros Lorenzo, Araceli Mallo, Margarita Puente, Anas Saadeddin, Santiago Ferrer, Iñigo Angulo-Barturen, Jeremy N Burrows, María Luisa Leon
Malaria is still one of the most prevalent parasitic infection in the world with half of the world's population at risk of malaria. The effectiveness of current antimalarial therapy is under continuous threat through the spread of resistant Plasmodium strains, even to the most recent class of antimalarial drugs (ACT: artemisinin-combination-therapies). As a consequence, there is still an urgent requirement for new antimalarial drugs. We previously reported the identification of 4(1H)-pyridones as a novel series with potent antimalarial activity...
March 28, 2018: Journal of Medicinal Chemistry
Waqas Khan Kayani, Bushra Hafeez Kiani, Erum Dilshad, Bushra Mirza
Artemisinin and its analogues are naturally occurring most effective antimalarial secondary metabolites. These compounds also possess activity against various types of cancer cells, schistosomiasis, and some viral diseases. Artemisinin and its derivatives (A&D) are found in very low amounts in the only natural source i.e. Artemisia plant. To meet the global needs, plant sources have been exploited for the enhanced production of these natural products because their chemical synthesis is not profitable. The generally adopted approaches include non-transgenic (tissue and cell cultures) and transgenic together with the cell, tissue, and whole transgenic plant cultures...
March 27, 2018: World Journal of Microbiology & Biotechnology
Li Lang, Qian Hu, Jingyuan Wang, Zehui Liu, Jin Huang, Weiqiang Lu, Ying Huang
Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) is a promising drug target for antimalarial chemotherapy. In our continuous efforts to develop more potent PfDHODH inhibitors, a unique library of active ingredients from traditional Chinese medicine (TCM) has been collected and was screened in this study. Through the initial screening, we found that coptisine, a natural alkaloid from TCM Coptidis Rhizoma, was a novel and potent inhibitor of PfDHODH with an IC50 value of 1.83 ± 0.08 μM. At the same time, enzyme kinetic analysis using Lineweaver-Burk plot indicated that coptisine is an uncompetitive inhibitor for PfDHODH...
March 27, 2018: Chemical Biology & Drug Design
Joanna Gallay, Sylvain Prod'hom, Thomas Mercier, Carine Bardinet, Dany Spaggiari, Emilie Pothin, Thierry Buclin, Blaise Genton, Laurent Arthur Decosterd
In epidemiological studies, antimalarials measurements in blood represent the best available marker of drugs exposure at population level, an important driver for the emergence of drug resistance. We have developed a liquid chromatography-tandem mass spectrometry method (LC-MS/MS) for the simultaneous quantification of 7 frequently used antimalarials (amodiaquine, chloroquine, quinine, sulfadoxine, pyrimethamine, mefloquine, lumefantrine) and 2 active metabolites (N-desethyl-amodiaquine, desbutyl-lumefantrine) in 10-μl dried blood spots (DBS)...
February 3, 2018: Journal of Pharmaceutical and Biomedical Analysis
Alessandra Vallone, Sarah D'Alessandro, Simone Brogi, Margherita Brindisi, Giulia Chemi, Gloria Alfano, Stefania Lamponi, Soon Goo Lee, Joseph M Jez, Karin J M Koolen, Koen J Dechering, Simona Saponara, Fabio Fusi, Beatrice Gorelli, Donatella Taramelli, Silvia Parapini, Reto Caldelari, Giuseppe Campiani, Sandra Gemma, Stefania Butini
Therapies addressing multiple stages of Plasmodium falciparum life cycle are highly desirable for implementing malaria elimination strategies. MMV019918 (1, 1-[5-(4-bromo-2-chlorophenyl)furan-2-yl]-N-[(piperidin-4-yl)methyl]methanamine) was selected from the MMV Malaria Box for its dual activity against both asexual stages and gametocytes. In-depth structure-activity relationship studies and cytotoxicity evaluation led to the selection of 25 for further biological investigation. The potential transmission blocking activity of 25 versus P...
March 10, 2018: European Journal of Medicinal Chemistry
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