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https://www.readbyqxmd.com/read/28719882/antileishmanial-activity-and-tubulin-polymerization-inhibition-of-podophyllotoxin-derivatives-on-leishmania-infantum
#1
José Miguel Escudero-Martínez, Yolanda Pérez-Pertejo, Rosa M Reguera, María Ángeles Castro, María Victoria Rojo, Carolina Santiago, Andrés Abad, Pablo Anselmo García, José Luis López-Pérez, Arturo San Feliciano, Rafael Balaña-Fouce
Leishmania microtubules play an important role not only in cell division, but also in keeping the shape of the parasite and motility of its free-living stages. Microtubules result from the self-assembly of alpha and beta tubulins, two phylogenetically conserved and very abundant eukaryotic proteins in kinetoplastids. The colchicine binding domain has inspired the discovery and development of several drugs currently in clinical use against parasites. However, this domain is less conserved in kinetoplastids and may be selectively targeted by new compounds...
June 28, 2017: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/28719879/four-types-of-attenuation-of-phenol-and-cresols-in-microcosms-under-simulated-marine-conditions-a-kinetic-study
#2
Yuejie Wang, Fanping Meng, Yufei Lin, Weiyan Duan, Qunqun Liu
Phenol, o-cresol, m-cresol, and p-cresol were selected to conduct microcosm experiments to examine their attenuation under simulated marine conditions, aiming at estimating natural attenuation and the contribution of oxidation, photolysis, biodegradation, and volatilisation to total attenuation of phenol and three cresols in the marine environment. The development of attenuation in microcosms showed the relevance of the pseudo-first-order kinetic for all phenols. The half-lives of phenol, o-cresol, m-cresol, and p-cresol attenuation under optimal conditions were 7...
July 11, 2017: Chemosphere
https://www.readbyqxmd.com/read/28719746/structure-activity-study-of-ghrelin-1-8-resulting-in-high-affinity-fluorine-bearing-ligands-for-the-ghrelin-receptor
#3
Carlie L Charron, Jin-Qiang Hou, Mark S McFarland, Savita Dhanvantari, Michael S Kovacs, Leonard G Luyt
The ghrelin receptor, also known as the growth hormone secretagogue receptor 1a (GHS-R1a), is a G-protein coupled receptor that is differentially expressed in healthy tissue and several cancers, including prostate, testicular, and ovarian. Selectively targeting the ghrelin receptor using fluorine-18 tagged entities would allow localization and visualization of ghrelin receptor expressing carcinomas using PET imaging. The endogenous ligand ghrelin, a 28 amino acid peptide with 3.1 nM affinity, has poor in vivo stability...
July 18, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28719603/the-%C3%A2-100-lab-a-3d-printable-open-source-platform-for-fluorescence-microscopy-optogenetics-and-accurate-temperature-control-during-behaviour-of-zebrafish-drosophila-and-caenorhabditis-elegans
#4
Andre Maia Chagas, Lucia L Prieto-Godino, Aristides B Arrenberg, Tom Baden
Small, genetically tractable species such as larval zebrafish, Drosophila, or Caenorhabditis elegans have become key model organisms in modern neuroscience. In addition to their low maintenance costs and easy sharing of strains across labs, one key appeal is the possibility to monitor single or groups of animals in a behavioural arena while controlling the activity of select neurons using optogenetic or thermogenetic tools. However, the purchase of a commercial solution for these types of experiments, including an appropriate camera system as well as a controlled behavioural arena, can be costly...
July 2017: PLoS Biology
https://www.readbyqxmd.com/read/28719335/experimental-infection-with-and-maintenance-of-cell-fusing-agent-virus-flavivirus-in-aedes-aegypti
#5
Maria Angelica Contreras-Gutierrez, Hilda Guzman, Saravanan Thangamani, Nikos Vasilakis, Robert B Tesh
During the past two decades, there has been a dramatic increase in the recognition and characterization of novel insect-specific flaviviruses (ISFVs). Some of these agents are closely related to important mosquito-borne flavivirus pathogens. Results of experimental studies suggest that mosquitoes and mosquito cell cultures infected with some ISFVs are refractory to superinfection with related flavivirus pathogens; and it has been proposed that ISFVs potentially could be used to alter the vector competence of mosquitoes and reduce transmission of specific flavivirus pathogens, such as dengue, West Nile, or Zika viruses...
July 2017: American Journal of Tropical Medicine and Hygiene
https://www.readbyqxmd.com/read/28719247/telehealth-in-schools-using-a-systematic-educational-model-based-on-fiction-screenplays-interactive-documentaries-and-three-dimensional-computer-graphics
#6
Diogo Julien Miranda, Chao Lung Wen
BACKGROUND: Preliminary studies suggest the need of a global vision in academic reform, leading to education re-invention. This would include problem-based education using transversal topics, developing of thinking skills, social interaction, and information-processing skills. We aimed to develop a new educational model in health with modular components to be broadcast and applied as a tele-education course. MATERIALS AND METHODS: We developed a systematic model based on a "Skills and Goals Matrix" to adapt scientific contents on fictional screenplays, three-dimensional (3D) computer graphics of the human body, and interactive documentaries...
July 18, 2017: Telemedicine Journal and E-health: the Official Journal of the American Telemedicine Association
https://www.readbyqxmd.com/read/28719188/phage-selection-of-cyclic-peptides-for-application-in-research-and-drug-development
#7
Kaycie Deyle, Xu-Dong Kong, Christian Heinis
Cyclic peptides can bind to protein targets with high affinities and selectivities, which makes them an attractive modality for the development of research reagents and therapeutics. Additional properties, including low inherent toxicity, efficient chemical synthesis, and facile modification with labels or immobilization reagents, increase their attractiveness. Cyclic peptide ligands against a wide range of protein targets have been isolated from natural sources such as bacteria, fungi, plants, and animals...
July 18, 2017: Accounts of Chemical Research
https://www.readbyqxmd.com/read/28718982/design-and-solution-phase-synthesis-of-membrane-targeting-lipopeptides-with-selective-antibacterial-activity
#8
Mohini Mohan Konai, Utsarga Adhikary, Jayanta Haldar
Designing selective antibacterial molecules remains an unmet goal in the field of membrane targeting agents. To this aim, herein we report the rational design and synthesis of a new class of lipopeptides which possess highly selective bacterial killing over mammalian cells. The selective interaction with bacterial over mammalian membranes was established through various spectroscopic as well as microscopic experiments including biophysical studies with the model membranes. A detailed antibacterial structure-activity relationship was delineated after preparing a series of molecules consisting of the peptide moieties with varied sequence of amino acids such as D-phenylalanine, D-leucine and D-lysine...
July 18, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28718669/fruit-peel-polyphenolic-extract-induced-apoptosis-in-human-breast-cancer-cells-is-associated-with-ros-production-and-modulation-of-p38mapk-erk1-2-and-the-akt-signaling-pathway
#9
Martin Kello, Lucia Kulikova, Janka Vaskova, Alexandra Nagyova, Jan Mojzis
Polyphenols represent a large group of natural substances with different biological properties. Currently, polyphenols are well studied due to their free radicals' scavenging and antioxidant activities. However, some studies indicate that polyphenols also exhibit pro-oxidant properties. In this study, the possible involvement of the pro-oxidant activities of fruit polyphenols was investigated in relation to apoptosis induction. To determine the type of cell death induced by fruit polyphenols (Flavine; F7), we assessed a series of assays, including measurements of caspase-7 activation, membrane mitochondrial potential changes, reactive oxygen (ROS) and nitrogen species production, lipid peroxidation, antioxidant enzymes activities, and PARP cleavage...
July 18, 2017: Nutrition and Cancer
https://www.readbyqxmd.com/read/28718636/long-chain-alkyl-esters-of-hydroxycinnamic-acids-as-promising-anticancer-agents-selective-induction-of-apoptosis-in-cancer-cells
#10
José C J M D S Menezes, Najmeh Edraki, Shrivallabh Kamat, Mahsima Khoshneviszadeh, Zahra Kayani, Hossein Hadavand Mirzaei, Ramin Miri, Nasrollah Erfani, Maryam Nejati, José A S Cavaleiro, Tiago B Silva, Luciano Saso, Fernanda M Borges, Omidreza Firuzi
Cancer is the major cause of morbidity and mortality worldwide. Hydroxycinnamic acids (HCAs) are naturally-occurring compounds and their alkyl esters may possess enhanced biological activities. We evaluated C4, C14, C16 and C18 alkyl esters of p-coumaric, ferulic, sinapic and caffeic acids (19 compounds) for their cytotoxic activity against four human cancer cells and also examined their effect on cell cycle alteration and apoptosis induction. The tetradecyl (1c) and hexadecyl (1d) esters of p-coumaric acid and tetradecyl ester of caffeic acid (4c), but not the parental HCAs, were selectively effective against MOLT-4 (human lymphoblastic leukemia) cells with IC50 values of 0...
July 18, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28718426/targeting-tgf-%C3%AE-signaling-in-cancer
#11
REVIEW
Selcuk Colak, Peter Ten Dijke
The transforming growth factor (TGF)-β signaling pathway is deregulated in many diseases, including cancer. In healthy cells and early-stage cancer cells, this pathway has tumor-suppressor functions, including cell-cycle arrest and apoptosis. However, its activation in late-stage cancer can promote tumorigenesis, including metastasis and chemoresistance. The dual function and pleiotropic nature of TGF-β signaling make it a challenging target and imply the need for careful therapeutic dosing of TGF-β drugs and patient selection...
January 2017: Trends in Cancer
https://www.readbyqxmd.com/read/28718394/multiple-possible-inaccuracies-cast-doubt-on-a-recent-report-suggesting-selective-serotonin-reuptake-inhibitors-to-be-toxic-and-ineffective
#12
Fredrik Hieronymus, Alexander Lisinski, Jakob Näslund, Elias Eriksson
According to a systematic review on the use of selective serotonin reuptake inhibitors (SSRIs) in adult depression that was recently published in BMC Psychiatry, the results of which have been widely disseminated in lay media, these drugs increase the risk for serious adverse events (SAEs) while exerting poor antidepressant efficacy. A cursory analysis, however, suggests the analysis of SAEs conducted by the authors to be marred by both methodological inaccuracies and blatant errors. After having corrected for these apparent mistakes, we conducted a sensitivity analysis in which we also accounted for a possible moderating effect of age; while this suggests SSRIs to be safe drugs in the non-elderly, they do confirm what is already known, that is, that they may enhance the risk for SAEs in the old...
July 18, 2017: Acta Neuropsychiatrica
https://www.readbyqxmd.com/read/28718051/coronary-heart-disease-preoperative-gesture-interactive-diagnostic-system-based-on-augmented-reality
#13
Yi-Bo Zou, Yi-Min Chen, Ming-Ke Gao, Quan Liu, Si-Yu Jiang, Jia-Hui Lu, Chen Huang, Ze-Yu Li, Dian-Hua Zhang
Coronary heart disease preoperative diagnosis plays an important role in the treatment of vascular interventional surgery. Actually, most doctors are used to diagnosing the position of the vascular stenosis and then empirically estimating vascular stenosis by selective coronary angiography images instead of using mouse, keyboard and computer during preoperative diagnosis. The invasive diagnostic modality is short of intuitive and natural interaction and the results are not accurate enough. Aiming at above problems, the coronary heart disease preoperative gesture interactive diagnostic system based on Augmented Reality is proposed...
August 2017: Journal of Medical Systems
https://www.readbyqxmd.com/read/28717940/alopecia-areata-a-comprehensive-review-of-pathogenesis-and-management
#14
REVIEW
Ralph M Trüeb, Maria Fernanda Reis Gavazzoni Dias
Alopecia areata is a common hair loss condition that is characterized by acute onset of non-scarring hair loss in usually sharply defined areas ranging from small patches to extensive or less frequently diffuse involvement. Depending on its acuity and extent, hair loss is an important cause of anxiety and disability. The current understanding is that the condition represents an organ-specific autoimmune disease of the hair follicle with a genetic background. Genome-wide association studies provide evidence for the involvement of both innate and acquired immunity in the pathogenesis, and mechanistic studies in mouse models of alopecia areata have specifically implicated an IFN-γ-driven immune response, including IFNγ, IFNγ-induced chemokines and cytotoxic CD8 T cells as the main drivers of disease pathogenesis...
July 17, 2017: Clinical Reviews in Allergy & Immunology
https://www.readbyqxmd.com/read/28717880/environmental-exposure-does-not-explain-putative-maladaptation-in-road-adjacent-populations
#15
Steven P Brady
While the ecological consequences of roads are well described, little is known of their role as agents of natural selection, which can shape adaptive and maladaptive responses in populations influenced by roads. This knowledge gap persists despite a growing appreciation for the influence of evolution in human-altered environments. There, insights indicate that natural selection typically results in local adaptation. Thus, populations influenced by road-induced selection should evolve fitness advantages in their local environment...
July 17, 2017: Oecologia
https://www.readbyqxmd.com/read/28717842/selective-matrix-metalloproteinase-inhibition-increases-breaking-strength-and-reduces-anastomotic-leakage-in-experimentally-obstructed-colon
#16
Peter-Martin Krarup, Mikkel Eld, Lars Nannestad Jorgensen, Mark Berner Hansen, Magnus S Ågren
PURPOSE: Colonic obstruction causes loss of collagen and impairment of anastomotic integrity by matrix metalloproteinases (MMPs). Unexpectedly, pharmacological MMP inhibition increased anastomotic leakage (AL) in obstructed colon possibly due to the non-selective nature of these compounds and the experimental model applied. We therefore studied the effects of selective MMP inhibition on the healing of anastomoses in colon obstructed by a novel laparoscopic technique. METHODS: Left colon was obstructed in 38 male Sprague-Dawley rats (226-284 g)...
July 17, 2017: International Journal of Colorectal Disease
https://www.readbyqxmd.com/read/28717803/hot-off-the-press
#17
Robert A Hill, Andrew Sutherland
A personal selection of 32 recent papers is presented covering various aspects of current developments in bioorganic chemistry and novel natural products such as svetamycin B from a Streptomyces species.
July 18, 2017: Natural Product Reports
https://www.readbyqxmd.com/read/28717592/epas1-variants-in-high-altitude-tibetan-wolves-were-selectively-introgressed-into-highland-dogs
#18
Bridgett vonHoldt, Zhenxin Fan, Diego Ortega-Del Vecchyo, Robert K Wayne
BACKGROUND: Admixture can facilitate adaptation. For example, black wolves have obtained the variant causing black coat color through past hybridization with domestic dogs and have higher fitness than gray colored wolves. Another recent example of the transfer of adaptive variation between the two species has been suggested by the similarity between high altitude Tibetan mastiffs and wolves at the EPAS1 gene, a transcription factor induced in low oxygen environments. METHODS: Here, we investigate the directionality of admixture in EPAS1 between 28 reference highland gray wolves, 15 reference domestic dogs, and 21 putatively admixed highland wolves...
2017: PeerJ
https://www.readbyqxmd.com/read/28717387/human-mediated-evolution-in-a-threatened-species-juvenile-life-history-changes-in-snake-river-salmon
#19
Robin S Waples, Anna Elz, Billy D Arnsberg, James R Faulkner, Jeffrey J Hard, Emma Timmins-Schiffman, Linda K Park
Evaluations of human impacts on Earth's ecosystems often ignore evolutionary changes in response to altered selective regimes. Freshwater habitats for Snake River fall Chinook salmon (SRFCS), a threatened species in the US, have been dramatically changed by hydropower development and other watershed modifications. Associated biological changes include a shift in juvenile life history: Historically essentially 100% of juveniles migrated to sea as subyearlings, but a substantial fraction have migrated as yearlings in recent years...
August 2017: Evolutionary Applications
https://www.readbyqxmd.com/read/28717385/changes-in-diet-associated-with-cancer-an-evolutionary-perspective
#20
Frédéric Thomas, Sophie Rome, Frédéric Mery, Erika Dawson, Jacques Montagne, Peter A Biro, Christa Beckmann, François Renaud, Robert Poulin, Michel Raymond, Beata Ujvari
Changes in diet are frequently correlated with the occurrence and progression of malignant tumors (i.e., cancer) in both humans and other animals, but an integrated conceptual framework to interpret these changes still needs to be developed. Our aim is to provide a new perspective on dietary changes in tumor-bearing individuals by adapting concepts from parasitology. Dietary changes may occur alongside tumor progression for several reasons: (i) as a pathological side effect with no adaptive value, (ii) as the result of self-medication by the host to eradicate the tumor and/or to slow down its progression, (iii) as a result of host manipulation by the tumor that benefits its progression, and finally (iv) as a host tolerance strategy, to alleviate and repair damages caused by tumor progression...
August 2017: Evolutionary Applications
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