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https://www.readbyqxmd.com/read/29456818/synthesis-and-antiplasmodial-activity-of-novel-phenanthroline-derivatives-an-in-vivo-study
#1
Azar Tahghighi, Safoura Karimi, Arezoo Rafie Parhizgar, Sedigheh Zakeri
Objectives: Due to the rapid increased drug resistance to Plasmodium parasites, an urgent need to achieve new antiplasmodial drugs is felt. Therefore, in this study, the new synthetic phenanthroline derivatives were synthesized with antiplasmodial activity. Materials and Methods: A series of 1,10-phenanthroline derivatives containing amino-alcohol and amino-ether substituents were synthesized via facile procedures, starting with 5,6-epoxy-1,10-phenanthroline. Their antiplasmodial activity was then evaluated using Peter's 4-day suppressive test against Plasmodium berghei-infected mice (ANKA strain)...
February 2018: Iranian Journal of Basic Medical Sciences
https://www.readbyqxmd.com/read/29453896/the-anti-malarial-mefloquine-inhibits-nf-%C3%AE%C2%BAb-signaling-and-induces-apoptosis-in-colorectal-cancer-cells
#2
Xin Xu, Jun Wang, Kunkun Han, Shaoyan Li, Feng Xu, Yili Yang
The NF-κB signaling pathway is activated in many colorectal cancer (CRC) cells and in the tumor microenvironment, which plays a critical role in cancer initiation, development, and response to therapies. We found in the present study that the widely used antimalarial drug mefloquine was a NF-κB inhibitor that blocked the activation of IκBα kinase, leading to the reduction of IκBα degradation, decrease of p65 phosphorylation, and suppressed expression of NF-κB target genes in colorectal cancer cells. We also found that mefloquine induced growth arrest and apoptosis of colorectal cancer cells harboring phosphorylated p65 in culture and mice...
February 17, 2018: Cancer Science
https://www.readbyqxmd.com/read/29451780/using-i-in-vitro-i-evolution-and-whole-genome-analysis-iviewga-to-discover-next-generation-targets-for-antimalarial-drug-discovery
#3
Madeline R Luth, Purva Gupta, Sabine Ottilie, Elizabeth A Winzeler
Although many new anti-infectives have been discovered and developed solely using phenotypic cellular screening and assay optimization, most researchers recognize that structure-guided drug design is more practical and less costly. In addition, a greater chemical space can be interrogated with structure-guided drug design. The practicality of structure-guided drug design has launched a search for the targets of compounds discovered in phenotypic screens. One method that has been used extensively in malaria parasites for target discovery and chemical validation is in vitro evolution and whole genome analysis (IVIEWGA)...
February 16, 2018: ACS Infectious Diseases
https://www.readbyqxmd.com/read/29451019/antimicrobial-substances-from-the-rare-actinomycete-nonomuraea-rhodomycinica-nr4-asc07-t
#4
Khomsan Supong, Paranee Sripreechasak, Wongsakorn Phongsopitanun, Somboon Tanasupawat, Kannawat Danwisetkanjana, Nantiya Bunbamrung, Pattama Pittayakhajonwut
Nonomuraea rhodomycinica NR4-ASC07 T is a rare actinomycete isolated from soil in Sirindhorn peat swamp forest. The crude extract of its culture broth exhibited antimicrobial and anticancer against diverse human pathogens and cancer cells. The chemical investigation of the crude extract led to the isolation of two new metabolites named nonomuric acid (1) and 3-hydroxy deoxydaunorubicinol aglycone (2), along with two known bioactive compounds [ε-rhodomycinone (3) and 7-deoxy-13-dihydrocarminomycinone (4)]. Compounds 1 and 3 showed antimalarial activity with the half maximal inhibitory concentration (IC 50 ) of 8...
February 16, 2018: Natural Product Research
https://www.readbyqxmd.com/read/29449583/mesoporous-silica-nanocarriers-encapsulated-antimalarials-with-high-therapeutic-performance
#5
Saliu Alao Amolegbe, Yui Hirano, Joseph Oluwatope Adebayo, Olusegun George Ademowo, Elizabeth Abidemi Balogun, Joshua Ayoola Obaleye, Antoniana Ursine Krettli, Chengzhong Yu, Shinya Hayami
The use of nanocarriers in drug delivery is a breakeven research and has received a clarion call in biomedicine globally. Herein, two newly nano-biomaterials: MCM-41 encapsulated quinine (MCM-41 ⊃ QN) (1) and 3-phenylpropyl silane functionalized MCM-41 loaded QN (pMCM-41 ⊃ QN) (2) were synthesized and well characterized. 1 and 2 along with our two already reported nano-antimalarial drugs (MCM-41 ⊃ ATS) (3) and 3-aminopropyl silane functionalized MCM-41 contained ATS (aMCM-41 ⊃ ATS) (4) were screened in vitro for their activity against P...
February 15, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29445390/approaches-and-recent-developments-for-the-commercial-production-of-semi-synthetic-artemisinin
#6
REVIEW
Stephanie H Kung, Sean Lund, Abhishek Murarka, Derek McPhee, Chris J Paddon
The antimalarial drug artemisinin is a natural product produced by the plant Artemisia annua . Extracts of A. annua have been used in Chinese herbal medicine for over two millennia. Following the re-discovery of A. annua extract as an effective antimalarial, and the isolation and structural elucidation of artemisinin as the active agent, it was recommended as the first-line treatment for uncomplicated malaria in combination with another effective antimalarial drug (Artemisinin Combination Therapy) by the World Health Organization (WHO) in 2002...
2018: Frontiers in Plant Science
https://www.readbyqxmd.com/read/29436997/pyrazole-schiff-base-hybrid-as-an-anti-malarial-agent-synthesis-in-vitro-screening-and-molecular-docking-study
#7
Shilpy Aggarwal, Deepika Paliwal, Dhirender Kaushik, Girish Kumar Gupta, Ajay Kumar
BACKGROUND: Malaria, one of the most vital infectious diseases caused by protozoan parasites of the Plasmodium genus. As P. falciparum, the cause of most of the severe cases of malaria, is increasingly resistant to available drugs such as amodioquine, chloroquine, artemisinin, and antifolates, there is an urgent need of identify new targets for chemotherapy Objective: This study screened novel pyrazole derivatives carrying iminium & benzothiazole group for antimalarial potential against P...
February 12, 2018: Combinatorial Chemistry & High Throughput Screening
https://www.readbyqxmd.com/read/29434987/acridone-suppresses-the-proliferation-of-human-breast-cancer-cells-in-vitro-via-atp-binding-cassette-subfamily-g-member-2
#8
Licheng Xu, Shuyan Li, Zhi Liang, Haixia Lin, Rongzhan Fu
In the past decades, the tricyclic acridone ring system has become a focus of major research by medicinal chemists due to the biological significance of this moiety in drug design and discovery. Acridone has substantial bio-potential since it performs crucial functions, including antibacterial, antimalarial, antiviral and anti-neoplastic activities. However, the anticancer effect and the underlying mechanisms of acridone on breast cancer cells remains unclear. In the present study, the anti-tumor function and the underlying mechanisms of acridone were evaluated in vitro...
February 2018: Oncology Letters
https://www.readbyqxmd.com/read/29422048/tools-for-surveillance-of-anti-malarial-drug-resistance-an-assessment-of-the-current-landscape
#9
REVIEW
Christian Nsanzabana, Djibrine Djalle, Philippe J Guérin, Didier Ménard, Iveth J González
To limit the spread and impact of anti-malarial drug resistance and react accordingly, surveillance systems able to detect and track in real-time its emergence and spread need to be strengthened or in some places established. Currently, surveillance of anti-malarial drug resistance is done by any of three approaches: (1) in vivo studies to assess the efficacy of drugs in patients; (2) in vitro/ex vivo studies to evaluate parasite susceptibility to the drugs; and/or (3) molecular assays to detect validated gene mutations and/or gene copy number changes that are associated with drug resistance...
February 8, 2018: Malaria Journal
https://www.readbyqxmd.com/read/29420756/potent-plasmodium-falciparum-gametocytocidal-compounds-identified-by-exploring-the-kinase-inhibitor-chemical-space-for-dual-active-antimalarials
#10
Mariëtte E van der Watt, Janette Reader, Alisje Churchyard, Sindisiwe H Nondaba, Sonja B Lauterbach, Jandeli Niemand, Sijuade Abayomi, Riëtte A van Biljon, Jessica I Connacher, Roelof D J van Wyk, Claire Le Manach, Tanya Paquet, Diego González Cabrera, Christel Brunschwig, Anjo Theron, Sonia Lozano-Arias, Janneth F I Rodrigues, Esperanza Herreros, Didier Leroy, James Duffy, Leslie J Street, Kelly Chibale, Dalu Mancama, Theresa L Coetzer, Lyn-Marie Birkholtz
Objectives: Novel chemical tools to eliminate malaria should ideally target both the asexual parasites and transmissible gametocytes. Several imidazopyridazines (IMPs) and 2-aminopyridines (2-APs) have been described as potent antimalarial candidates targeting lipid kinases. However, these have not been extensively explored for stage-specific inhibition of gametocytes in Plasmodium falciparum parasites. Here we provide an in-depth evaluation of the gametocytocidal activity of compounds from these chemotypes and identify novel starting points for dual-acting antimalarials...
February 6, 2018: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/29411150/correction-to-design-synthesis-conformational-and-molecular-docking-study-of-some-novel-acyl-hydrazone-based-molecular-hybrids-as-antimalarial-and-antimicrobial-agents
#11
Parvin Kumar, Kulbir Kadyan, Meenakshi Duhan, Jayant Sindhu, Vineeta Singh, Baljeet Singh Saharan
After publication of the original article [1], the following error was reported in the Results section of the Abstract: "antifungal activity against one yeast i.e. Aspergillus niger" should read: "antifungal activity against one fungus i.e. Aspergillus niger". The authors would like to confirm all antifungal activity has been screened against fungi not yeast.
February 6, 2018: Chemistry Central Journal
https://www.readbyqxmd.com/read/29407988/machine-learning-prioritizes-synthesis-of-primaquine-ureidoamides-with-high-antimalarial-activity-and-attenuated-cytotoxicity
#12
Jurica Levatić, Kristina Pavić, Ivana Perković, Lidija Uzelac, Katja Ester, Marijeta Kralj, Marcel Kaiser, Matthias Rottmann, Fran Supek, Branka Zorc
Primaquine (PQ) is a commonly used drug that can prevent the transmission of Plasmodium falciparum malaria, however toxicity limits its use. We prepared five groups of PQ derivatives: amides 1a-k, ureas 2a-k, semicarbazides 3a,b, acylsemicarbazides 4a-k and bis-ureas 5a-v, and evaluated them for antimalarial activity in vitro against the erythrocytic stage of P. falciparum NF54. Particular substituents, such as trityl (in 2j and 5r) and methoxybenzhydryl (in 3b and 5v) were associated with a favorable cytotoxicity-to-activity ratio...
January 31, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29407943/first-homology-model-of-plasmodium-falciparum-glucose-6-phosphate-dehydrogenase-discovery-of-selective-substrate-analog-based-inhibitors-as-novel-antimalarial-agents
#13
Nelson Alencar, Irene Sola, María Linares, Jordi Juárez-Jiménez, Caterina Pont, Antonio Viayna, David Vílchez, Cristina Sampedro, Paloma Abad, Susana Pérez-Benavente, Jerónimo Lameira, José M Bautista, Diego Muñoz-Torrero, F Javier Luque
In Plasmodium falciparum the bifunctional enzyme glucose-6-phosphate dehydrogenase‒6-phosphogluconolactonase (PfG6PD‒6PGL) is involved in the catalysis of the first reaction of the pentose phosphate pathway. Since this enzyme has a key role in parasite development, its unique structure represents a potential target for the discovery of antimalarial drugs. Here we describe the first 3D structural model of the G6PD domain of PfG6PD‒6PGL. Compared to the human enzyme (hG6PD), the 3D model has enabled the identification of a key difference in the substrate-binding site, which involves the replacement of Arg365 in hG6PD by Asp750 in PfG6PD...
February 1, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29406996/the-role-of-antimalarial-quality-in-the-emergence-and-transmission-of-resistance
#14
Aleisha R Brock, Joshua V Ross, Sunil Parikh, Adrian Esterman
The emergence and transmission of antimalarial resistance is hampering malaria eradication efforts and is shortening the useful therapeutic life of currently available antimalarials. Drug selection pressure has been identified as a contributing factor to the emergence and transmission of resistance, especially population treatment coverage and sub-therapeutic concentrations of active pharmaceutical ingredient (API) in the bloodstream. Medicine quality can be defined as good quality or poor quality. Poor quality antimalarials can be falsified, substandard or degraded and are estimated to make up between 10 and 50% of the antimalarial market in developing countries, and can be a source of sub-therapeutic doses of antimalarial API(s)...
February 2018: Medical Hypotheses
https://www.readbyqxmd.com/read/29398445/optimization-of-antimalarial-and-anticancer-activities-of-e-methyl-2-7-chloroquinolin-4-ylthio-3-4-hydroxyphenyl-acrylate
#15
Jesús A Romero, María E Acosta, Neira D Gamboa, Michael R Mijares, Juan B De Sanctis, Jaime E Charris
Chemically modified versions of bioactive substances, are particularly useful in overcoming barriers associated with drug formulation, drug delivery and poor pharmacokinetic properties. In this study, a series of fourteen (E)-methyl 2-(7-chloroquinolin-4-ylthio)-3-(4-hydroxyphenyl) acrylate (2-15) were prepared by using a one step synthesis from 1 previously described by us as potential antimalarial and antitumor agent. Molecules were evaluated as inhibitors of β-hematin formation, where most of them showed a significant inhibition value (% > 70)...
February 2, 2018: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29398201/antimalarial-polyoxygenated-cyclohexene-derivatives-from-the-roots-of-uvaria-cherrevensis
#16
Ratsami Lekphrom, Kwanjai Kanokmedhakul, Florian Schevenels, Somdej Kanokmedhakul
Three new polyoxygenated cyclohexene derivatives named cherrevenisyls A and B (1 and 2), and ellipeiopsol E (3), along with fifteen known compounds, were isolated from the roots of Uvaria cherrevensis. Their structures were determined by spectroscopic methods including 2D NMR techniques and mass spectrometry. The absolute configurations of 1 and 2 were assigned. Compounds 1, 2 and 5 showed antimalarial activity against Plasmodium falciparum with IC50 ranging from 3.34-7.34μg/mL. Compounds 5-18 exhibited cytotoxicity against three cancer cell lines (KB, MCF-7 and NCI-H187) with IC50 values in ranging from 1...
February 1, 2018: Fitoterapia
https://www.readbyqxmd.com/read/29391779/biological-activity-quantitative-structure-activity-relationship-analysis-and-molecular-docking-of-xanthone-derivatives-as-anticancer-drugs
#17
Isnatin Miladiyah, Jumina Jumina, Sofia Mubarika Haryana, Mustofa Mustofa
Background: Xanthone derivatives have a wide range of pharmacological activities, such as those involving antibacterial, antiviral, antimalarial, anthelmintic, anti-inflammatory, antiprotozoal, and anticancer properties. Among these, we investigated the anticancer properties of xanthone. This research aimed to analyze the biological activity of ten novel xanthone derivatives, to investigate the most contributing-descriptors for their cytotoxic activities, and to examine the possible mechanism of actions of xanthone compound through molecular docking...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29389671/a-controlled-human-malaria-infection-model-enabling-evaluation-of-transmission-blocking-interventions
#18
Katharine A Collins, Claire Yt Wang, Matthew Adams, Hayley Mitchell, Melanie Rampton, Suzanne Elliott, Isaie J Reuling, Teun Bousema, Robert Sauerwein, Stephan Chalon, Jörg J Möhrle, James S McCarthy
BACKGROUND: Drugs and vaccines that can interrupt the transmission of Plasmodium falciparum will be important for malaria control and elimination. However, models for early clinical evaluation of candidate transmission-blocking interventions are currently unavailable. Here we describe a new model for evaluating malaria transmission from humans to Anopheles mosquitoes using controlled human malaria infection (CHMI). METHODS: Seventeen healthy malaria-naïve volunteers underwent CHMI by intravenous inoculation of P...
February 1, 2018: Journal of Clinical Investigation
https://www.readbyqxmd.com/read/29386159/bioanalytical-method-development-and-validation-for-quantification-of-morachalcone-a-in-rabbit-plasma-using-high-performance-liquid-chromatography
#19
Michael Raharja Gani, - Isnaeni, Amirudin Prawita, Achmad Fuad Hafid, Aty Widyawaruyanti
Artocarpus champeden (A. champeden) ethanol extract has been reported as antimalarial activity and prospective to be developed as phytomedicine products. The active marker compound was identical with known prenylated chalcone compound, Morachalcone A. To further develop phytomedicine products from A. champeden especially in aspects of bioavailability and pharmacokinetic, a valid, selective and sensitive analytical method becomes important to determine morachalcone A in plasma. The aim of study was to develop and validate selectivity and sensitivity of High Performance Liquid Chromatography (HPLC) method to determine morachalcone A in rabbit plasma...
January 2018: Pakistan Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29383139/dihydroartemisinin-attenuates-autoimmune-thyroiditis-by-inhibiting-the-cxcr3-pi3k-akt-nf-%C3%AE%C2%BAb-signaling-pathway
#20
Huijuan Liu, Qin Tian, Xiaoyu Ai, Yuan Qin, Zhanhong Cui, Meng Li, Jiahuan Yang, Denghui Zhai, Yanrong Liu, Shuang Chen, Jing Meng, Tao Sun, Honggang Zhou, Cheng Yang
Dihydroartemisinin (DHA) is the first generation of naturally occurring artemisinin derivatives with antimalarial activity. Recent research showed that this drug also features immunosuppressive and anti-inflammatory properties. Autoimmune thyroiditis (AIT) is a common organ-specific autoimmune disease with no available effective drug treatment. In this study, we investigated effects of DHA on AIT in vitro and in vivo. Results showed that DHA can visibly reduce antithyroglobulin antibody and thyroid peroxidase antibody levels and regulate T helper cells (Th) 1/Th2 imbalance of experimental AIT mice...
December 29, 2017: Oncotarget
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