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https://www.readbyqxmd.com/read/29035245/in-vivo-and-in-vitro-models-for-scanning-drug-substances-in-malaria-prestudy
#1
Ahmet Özbilgin, İbrahim Çavuş, Alicem Nuraydın, Tuğba Kaya
OBJECTIVE: The Wolrd Health Organization (WHO) encourages all countries to investigate antimalarial drug substances derived from herbal sources with the slogan "Hunt of the Next Artemisinin" due to the emergence of resistant strains of Plasmodium species to artemisinin. In the broad and simple sense, it was planned to help guide the young researchers set in-vitro and in-vivo models of malaria in order to be used in drug research and active ingredient studies. METHODS: In-vitro study, young Plasmodium berghei trophozoites were removed from the liquid nitrogen tank and resuspended in appropriate conditions, followed by incubation with chloroquine and tetracycline at concentrations of 0...
September 2017: Türkiye Parazitolojii Dergisi
https://www.readbyqxmd.com/read/29026393/in-vitro-investigation-of-clofazimine-analogues-for-antiplasmodial-cytotoxic-and-pro-oxidative-activities
#2
E M Makgatho, E F Mbajiorgu
BACKGROUND: Tetramethyl-piperidine-substituted, B4119 and B4158 have been shown to exhibit antiplasmodial activity. OBJECTIVES: The in vitro antiplasmodial, cytotoxic and oxidative activities of clofazimine and its analogues, all TMP (tetramethylpiperidyl)-substituted phenazines except B669, were evaluated in this study. METHODS: The antiplasmodial activity of the compounds against RB-1 and pfUP10 laboratory strains of Plasmodium falciparum was investigated by flow cytometry...
March 2017: African Health Sciences
https://www.readbyqxmd.com/read/29024590/efficient-synthesis-of-1-9-substituted-benzo-h-1-6-naphthyridin-2-1h-ones-and-evaluation-of-their-plasmodium-falciparum-gametocytocidal-activities
#3
Hao Li, Wei Sun, Xiuli Huang, Xiao Lu, Paresma Patel, Myunghoon Kim, Meghan Orr, Richard Fisher, Takeshi Tanaka, John McKew, Anton Simeonov, Philip Sanderson, Wei Zheng, Kimberly Willamson, Wenwei Huang
A novel three-component, two-step, one-pot nucleophilic aromatic substitution (SNAr)-intramolecular cyclization-Suzuki coupling reaction was developed for the synthesis of benzo[h][1,6]naphthyridin-2(1H)-ones (Torins). Based on the new efficiently convergent synthetic route, a library of Torin analogs was synthesized. The antimalarial activities of these compounds were evaluated against asexual parasites using a growth inhibition assay and gametocytes using a viability assay.
October 12, 2017: ACS Combinatorial Science
https://www.readbyqxmd.com/read/28990918/impact-evaluation-of-malaria-control-interventions-on-morbidity-and-all-cause-child-mortality-in-rwanda-2000-2010
#4
Erin Eckert, Lia S Florey, Jon Eric Tongren, S René Salgado, Alphonse Rukundo, Jean Pierre Habimana, Emmanuel Hakizimana, Kaendi Munguti, Noella Umulisa, Monique Mulindahabi, Corine Karema
The impressive decline in child mortality that occurred in Rwanda from 1996-2000 to 2006-2010 coincided with a period of rapid increase of malaria control interventions such as indoor residual spraying (IRS); insecticide-treated net (ITN) distribution and use, and improved malaria case management. The impact of these interventions was examined through ecological correlation analysis, and robust decomposition analysis of contextual factors on all-cause child mortality. Child mortality fell 61% during the evaluation period and prevalence of severe anemia in children 6-23 months declined 71% between 2005 and 2010...
September 2017: American Journal of Tropical Medicine and Hygiene
https://www.readbyqxmd.com/read/28990331/antimalarial-and-antileishmanial-activities-of-phytophenolics-and-their-synthetic-analogues
#5
Masanori Morimoto, Charles L Cantrell, Shabana Khan, Babu L Tekwani, Stephen O Duke
Thirty-seven phytophenolics and their synthetic analogues were evaluated for activity against two protozoal pathogens, Leishmania donovani and Plasmodium falciparum (D6 and W2 clones), respectively. 4,6-Dimethoxyaurone demonstrated the highest activity with IC50 values of 13.2 μM and 16.9 μM against L. donovani and P. falciparum (W2 clone), respectively, without undesired cytotoxicity against VERO cells. The moiety having two benzene rings was critical to maintain the antiprotozoal activities based on the observation that both coumaranones and chromones were inactive while other test compounds, including coumarans and aurones, remained active...
October 9, 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/28988153/synthesis-and-antimalarial-evaluation-of-artesunate-polyamine-and-trioxolane-polyamine-conjugates
#6
A Norrie Pearce, Marcel Kaiser, Brent R Copp
A series of artesunate-polyamine and trioxolane-polyamine conjugates have been prepared. The conjugates were evaluated for antimalarial activity towards the K1 dual drug resistant and NF54 chloroquine-sensitive strains of Plasmodium falciparum (Pf) and for cytotoxicity towards the rat myoblast cell line L6. (Bis)-Boc-(bis)-artesunate-polyamine and (tetra)-artesunate-polyamine conjugates exhibited potent in vitro activity towards both strains of Pf, with IC50 values in the range of 0.3-1.1 nM, comparable to the parent artesunate...
September 22, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28970217/lupus-low-disease-activity-state-is-associated-with-a-decrease-in-damage-progression-in-caucasian-patients-with-sle-but-overlaps-with-remission
#7
Margherita Zen, Luca Iaccarino, Mariele Gatto, Francesca Saccon, Maddalena Larosa, Anna Ghirardello, Leonardo Punzi, Andrea Doria
OBJECTIVE: To evaluate the prevalence, duration and effect on damage accrual of the 'Lupus Low Disease Activity State' (LLDAS) in a monocentric cohort of patients with systemic lupus erythematosus (SLE). METHODS: We studied 293 Caucasian patients with SLE during a 7-year follow-up period. Disease activity was assessed by SLE Disease Activity Index 2000 (SLEDAI-2K) and SELENA-SLEDAI physician global assessment (PGA), and damage by Systemic Lupus International Collaborating Clinics/American College of Rheumatology Damage Index (SDI)...
September 26, 2017: Annals of the Rheumatic Diseases
https://www.readbyqxmd.com/read/28968015/-mutagenicity-genotoxicity-and-gene-expression-of-rad51c-xiap-p53-and-nrf2-induced-by-antimalarial-extracts-of-plants-collected-from-the-middle-vaup%C3%A3-s-region-colombia
#8
Claudia Viviana Barbosa, Carlos Enrique Muskus, Luz Yaneth Orozco, Adriana Pabón
INTRODUCTION: Due to Plasmodium resistance to antimalarial drugs, it is important to find new therapeutic alternatives for malaria treatment and control. Based on the knowledge of Colombian indigenous communities, we collected extracts of plants with potential antimalarial effects from the middle Vaupés region. OBJECTIVE: To evaluate the mutagenic and genotoxic effects, as well as the gene expression of Rad51C, Xiap, P53 and Nrf2 induced by four ethanolic extracts with antimalarial activity (R001, T002, T015 and T028)...
September 1, 2017: Biomédica: Revista del Instituto Nacional de Salud
https://www.readbyqxmd.com/read/28967737/asymmetric-cycloaddition-and-cyclization-reactions-catalyzed-by-chiral-n-n-dioxide-metal-complexes
#9
Xiaohua Liu, Haifeng Zheng, Yong Xia, Lili Lin, Xiaoming Feng
Catalytic asymmetric cycloadditions and cascade cyclizations are a major focus for the enantioselective construction of chiral carbo- and heterocycles. A number of chiral Lewis acids and organocatalysts have been designed for such reactions. The development of broadly applicable catalysts bearing novel chiral backbones to meet the demands of various applications is an ongoing challenge. Approximately 10 years ago, we introduced a group of conformationally flexible C2-symmetric N,N'-dioxide amide compounds, which represent a new class of privileged ligands...
October 2, 2017: Accounts of Chemical Research
https://www.readbyqxmd.com/read/28961865/comparison-of-the-susceptibility-of-plasmodium-knowlesi-and-plasmodium-falciparum-to-antimalarial-agents
#10
Donelly A van Schalkwyk, Robert W Moon, Benjamin Blasco, Colin J Sutherland
Background: The simian malaria parasite Plasmodium knowlesi is now a well-recognized pathogen of humans in South-East Asia. Clinical infections appear adequately treated with existing drug regimens, but the evidence base for this practice remains weak. The availability of P. knowlesi cultures adapted to continuous propagation in human erythrocytes enables specific studies of in vitro susceptibility of the species to antimalarial agents, and could provide a surrogate system for testing investigational compounds against Plasmodium vivax and other non- Plasmodium falciparum infections that cannot currently be propagated in vitro ...
August 30, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/28960224/platinum-ii-chloroquine-complexes-are-antimalarial-agents-against-blood-and-liver-stages-by-impairing-mitochondrial-function
#11
Taís S Macedo, Wilmer Villarreal, Camila C Couto, Diogo R M Moreira, Maribel Navarro, Marta Machado, Miguel Prudêncio, Alzir A Batista, Milena B P Soares
Chloroquine is an antimalarial agent with strong activity against the blood stage of Plasmodium infection, but with low activity against the parasite's liver stage. In addition, the resistance to chloroquine limits its clinical use. The discovery of new molecules possessing multistage activity and overcoming drug resistance is needed. One possible strategy to achieve this lies in combining antimalarial quinolones with the pharmacological effects of transition metals. We investigated the antimalarial activity of four platinum(ii) complexes composed of chloroquine and phosphine ligands, denoted as WV-90, WV-92, WV-93 and WV-94...
September 29, 2017: Metallomics: Integrated Biometal Science
https://www.readbyqxmd.com/read/28953997/antimycobacterial-and-antimalarial-activities-of-endophytic-fungi-associated-with-the-ancient-and-narrowly-endemic-neotropical-plant-vellozia-gigantea-from-brazil
#12
Mariana C Ferreira, Charles L Cantrell, David E Wedge, Vívian N Gonçalves, Melissa R Jacob, Shabana Khan, Carlos A Rosa, Luiz H Rosa
BACKGROUND: Endophytic fungi, present mainly in the Ascomycota and Basidiomycota phyla, are associated with different plants and represent important producers of bioactive natural products. Brazil has a rich biodiversity of plant species, including those reported as being endemic. Among the endemic Brazilian plant species, Vellozia gigantea (Velloziaceae) is threatened by extinction and is a promising target to recover endophytic fungi. OBJECTIVE: The present study focused on bioprospecting of bioactive compounds of the endophytic fungi associated with V...
October 2017: Memórias do Instituto Oswaldo Cruz
https://www.readbyqxmd.com/read/28948379/systemic-lupus-erythematosus-patients-with-high-disease-activity-are-associated-with-accelerated-incidence-of-osteonecrosis-a-systematic-review-and-meta-analysis
#13
Kui Zhang, Yan Zheng, Junfeng Jia, Jin Ding, Zhenbiao Wu
Osteonecrosis (ON) is one of the serious complications for systemic lupus erythematosus (SLE); we aimed to study the risk relationship between disease activity and incidence of ON in SLE patients. The PubMed, Embase, and Cochrane library databases were searched for papers published up to May 2016 with English-language restriction; studies that compared disease activity between SLE patients with and without ON would be included, and eight studies involving a total of 1119 SLE patients were included. The incidence of ON in SLE was significantly associated with high patient's disease activity, including the degree (pool odds ratio 2...
September 25, 2017: Clinical Rheumatology
https://www.readbyqxmd.com/read/28939626/remission-and-low-disease-activity-status-ldas-protect-lupus-patients-from-damage-occurrence-data-from-a-multiethnic-multinational-latin-american-lupus-cohort-gladel
#14
Manuel Francisco Ugarte-Gil, Daniel Wojdyla, Guillermo J Pons-Estel, Luis J Catoggio, Cristina Drenkard, Judith Sarano, Guillermo A Berbotto, Eduardo F Borba, Emilia Inoue Sato, João C Tavares Brenol, Oscar Uribe, Luis A Ramirez Gómez, Marlene Guibert-Toledano, Loreto Massardo, Mario H Cardiel, Luis H Silveira, Rosa Chacón-Diaz, Graciela S Alarcón, Bernardo A Pons-Estel
OBJECTIVE: To evaluate disease activity statuses' (DAS') impact on systemic lupus erythematosus (SLE) outcomes. MATERIALS AND METHODS: Four DAS were defined: remission off-therapy: SLE Disease Activity Index (SLEDAI)=0, no prednisone or immunosuppressive drugs (IS); remission on-therapy: SLEDAI=0, prednisone ≤5 mg/day and/or IS (maintenance); low (L) DAS: SLEDAI ≤4, prednisone ≤7.5 mg/day and/or IS (maintenance); non-optimally controlled: SLEDAI >4 and/or prednisone >7...
September 22, 2017: Annals of the Rheumatic Diseases
https://www.readbyqxmd.com/read/28936796/biosurfactants-produced-by-bacillus-subtilis-a1-and-pseudomonas-stutzeri-na3-reduce-longevity-and-fecundity-of-anopheles-stephensi-and-show-high-toxicity-against-young-instars
#15
Punniyakotti Parthipan, Raja Kumaresan Sarankumar, Anitha Jaganathan, Pandian Amuthavalli, Ranganathan Babujanarthanam, Pattanathu K S M Rahman, Kadarkarai Murugan, Akon Higuchi, Giovanni Benelli, Aruliah Rajasekar
Anopheles stephensi acts as vector of Plasmodium parasites, which are responsible for malaria in tropical and subtropical areas worldwide. Currently, malaria management is a big challenge due to the presence of insecticide-resistant strains as well as to the development of Plasmodium species highly resistant to major antimalarial drugs. Therefore, the present study focused on biosurfactant produced by two bacteria Bacillus subtilis A1 and Pseudomonas stutzeri NA3, evaluating them for insecticidal applications against malaria mosquitoes...
September 21, 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/28934264/profiling-molecular-factors-associated-with-pyknosis-and-developmental-arrest-induced-by-an-opioid-receptor-antagonist-and-dihydroartemisinin-in-plasmodium-falciparum
#16
Hiroko Asahi, Shin-Ichi Inoue, Mamoru Niikura, Keisuke Kunigo, Yutaka Suzuki, Fumie Kobayashi, Fujiro Sendo
Malaria continues to be a devastating disease, largely caused by Plasmodium falciparum infection. We investigated the effects of opioid and cannabinoid receptor antagonists on the growth of intraerythrocytic P. falciparum. The delta opioid receptor antagonist 7-benzylidenenaltrexone (BNTX) and the cannabinoid receptor antagonists rimonaband and SR144528 caused growth arrest of the parasite. Notably BNTX and the established antimalarial drug dihydroartemisinin induced prominent pyknosis in parasite cells after a short period of incubation...
2017: PloS One
https://www.readbyqxmd.com/read/28932197/antiplasmodial-activity-and-toxicological-assessment-of-curcumin-plga-encapsulated-nanoparticles
#17
Zulaikha A Busari, Kabiru A Dauda, Olajumoke A Morenikeji, Funmilayo Afolayan, Oyetunde T Oyeyemi, Jairam Meena, Debasis Sahu, Amulya K Panda
Curcumin is a polyphenolic pigment isolated from the rhizomes of Curcuma longa (turmeric), a medicinal plant widely used in the ancient Indian and Chinese medicine. The antiplasmodial activity of curcumin is often hampered by its fast metabolism and poor water solubility, thus its incorporation into a delivery system could circumvent this problem. This study aimed to evaluate the in vivo antiplasmodial activity and the toxicity assessment of curcumin incorporated into poly (lactic-co-glycolic) acid (PLGA) nanoparticles...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28927276/alkoxycarbonate-ester-prodrugs-of-preclinical-drug-candidate-elq-300-for-prophylaxis-and-treatment-of-malaria
#18
Lisa Frueh, Yuexin Li, Michael W Mather, Qigui Li, Sovitj Pou, Aaron Nilsen, Rolf W Winter, Isaac P Forquer, April M Pershing, Lisa H Xie, Martin J Smilkstein, Diana Caridha, Dennis R Koop, Robert F Campbell, Richard J Sciotti, Mara Kreishman-Deitrick, Jane X Kelly, Brian Vesely, Akhil B Vaidya, Michael K Riscoe
ELQ-300 is a preclinical antimalarial drug candidate that is active against liver, blood, and transmission stages of Plasmodium falciparum. While ELQ-300 is highly effective when administered in a low multidose regimen, poor aqueous solubility and high crystallinity have hindered its clinical development. To overcome its challenging physiochemical properties, a number of bioreversible alkoxycarbonate ester prodrugs of ELQ-300 were synthesized. These bioreversible prodrugs are converted to ELQ-300 by host and parasite esterase action in the liver and bloodstream of the host...
October 13, 2017: ACS Infectious Diseases
https://www.readbyqxmd.com/read/28917450/a-novel-class-of-plasmodial-clpp-protease-inhibitors-as-potential-antimalarial-agents
#19
Sourabh Mundra, Vandana Thakur, Angelica M Bello, Sumit Rathore, Mohd Asad, Lianhu Wei, Jane Yang, Sai Kumar Chakka, Radhakrishnan Mahesh, Pawan Malhotra, Asif Mohmmed, Lakshmi P Kotra
The prokaryotic ATP-dependent ClpP protease, localized in the relict plastid of malaria parasite, represents a potential drug target. In the present study, we utilized in silico structure-based screening and medicinal chemistry approaches to identify a novel pyrimidine series of compounds inhibiting P. falciparum ClpP protease activity and evaluated their antiparasitic activities. Structure-activity relationship indicated that morpholine moiety at C2, an aromatic substitution at N3 and a 4-oxo moiety on the pyrimidine are important for potent inhibition of ClpP enzyme along with antiparasiticidal activity...
September 5, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28917086/kostchyienones-a-and-b-new-antiplasmodial-and-cytotoxicity-of-limonoids-from-the-roots-of-pseudocedrela-kotschyi-schweinf-harms
#20
Lazare S Sidjui, Yves O D Nganso, Rufin M K Toghueo, Brussine N K Wakeu, Joel T Dameue, Pierre Mkounga, Achyut Adhikari, Mehreen Lateef, Gabriel N Folefoc, Muhammad S Ali
Two new limonoids, kostchyienones A (1) and B (2), along with 12 known compounds 3-14 were isolated from the roots of Pseudocedrela kostchyi. Compound (7) was isolated for the first time from a natural source. Their structures were elucidated on the basis of spectroscopic evidence. Compounds 1-6 and 13-14 gave IC50 values ranging from 0.75 to 5.62 μg/mL for antiplasmodial activity against chloroquine-sensitive (Pf3D7) and chloroquine-resistant (PfINDO) strains of Plasmodium falciparum. Compound 5 showed moderate potential cytotoxicity against the HEK239T cell line with an IC50 value of 22...
September 16, 2017: Zeitschrift Für Naturforschung. C, A Journal of Biosciences
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