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https://www.readbyqxmd.com/read/29028531/synthesis-and-biological-evaluation-of-novel-non-racemic-indole-containing-allocolchicinoids
#1
Ekaterina S Shchegravina, Alexander A Maleev, Stanislav K Ignatov, Iuliia A Gracheva, Andreas Stein, Hans-Günther Schmalz, Andrey E Gavryushin, Anastasiya A Zubareva, Elena V Svirshchevskaya, Alexey Yu Fedorov
Two novel indole-containing allocolchicinoids were prepared from naturally occurring colchicine exploiting the Curtius rearrangement and tandem Sonogashira coupling/Pd-catalyzed cyclization as the key transformations. Their cytotoxic properties, apoptosis-inducing activity, tubulin assembly inhibition and short-time cytotoxic effects were investigated. Compound 7 demonstrated the most pronounced anti-cancer activity: IC50 < 1 nM, cell cycle arrest in the G2/M phase, 25% apoptosis induction, as well as lower destructive short-time effects on HT-29 cell line in comparison with colchicine...
September 27, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29026421/comparison-of-patellar-versus-hamstring-tendon-autografts-in-arthroscopic-anterior-cruciate-ligament-reconstruction-a-6-month-follow-up-of-a-randomized-clinical-trial
#2
Alireza Sadeghpour, Adel Ebrahimpour, Bahamin Attar, Zahra Azizian
BACKGROUND: The purpose of this study was to compare the outcomes of anterior cruciate ligament (ACL) reconstruction using the patellar versus hamstring tendon (HT) autograft. MATERIALS AND METHODS: In this randomized clinical trial, fifty patients undergoing arthroscopic ACL reconstruction were randomized into two equal groups: Those treated with either autogenous patellar tendon grafts (PT group) or HT group grafts. All patients were reviewed immediately after surgery, at 6 and 12 weeks after surgery, and then at 6 months using the International Knee Documentation Committee evaluation form...
2017: Journal of Research in Medical Sciences: the Official Journal of Isfahan University of Medical Sciences
https://www.readbyqxmd.com/read/29025984/synthesis-and-biological-evaluation-of-a-novel-18-f-labeled-adnectin-as-a-pet-radioligand-for-imaging-pd-l1-expression
#3
David J Donnelly, Ralph Adam Smith, Paul Morin, Dasa Lipovsek, Jochem Gokemeijer, Daniel Cohen, Virginie Lafont, Tritin Tran, Erin Lee Cole, Martin Wright, Joonyoung Kim, Adrienne Pena, Daniel Kukral, Douglas D Dischino, Patrick Chow, Jinping Gan, Olufemi Adelakun, Xi-Tao Wang, Kai Cao, David Lueng, Samuel Bonacorsi, Wendy Hayes
The programmed death protein (PD-1) and its ligand (PD-L1) play critical roles in a checkpoint pathway cancer cells exploit to evade the immune system. A same-day PET imaging agent for measuring PD-L1 status in primary and metastatic lesions could be important for optimizing drug therapy. Herein, we have evaluated the tumor targeting of an anti-PD-L1 Adnectin after (18)F-fluorine labeling. Methods: An anti-PD-L1 Adnectin was labeled with (18)F in two steps. This synthesis featured fluorination of a novel prosthetic group, followed by a copper-free click conjugation to a modified Adnectin to generate (18)F-BMS-986192...
October 12, 2017: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/29024872/a-salicylaldiminato-pt-ii-complex-with-dimethylpropylene-linkage-synthesis-structural-characterization-and-antineoplastic-activity
#4
Mohammad Azam, Saud I Al-Resayes, Saied M Soliman, Agata Trzesowska-Kruszynska, Rafal Kruszynski, Zahid Khan
A novel (salicylaldiminato)Pt(II) complex with two different molecular structures, one solventless ((salicylaldiminato)Pt(II)) 1 and another one solvated ((salicylaldiminato)Pt(II). C2H5OH), 1·C2H5OH, has been obtained by the reaction of a salen ligand with [PtCl2(DMSO)2] in ethanol at room temperature. The asymmetric unit of solventless 1 contains 9 such complex molecules whereas 1·C2H5OH contains 2 complex molecules and one ethanol molecule. To get insights into the structure and bonding, DFT and TDFT calculation have been carried out...
October 5, 2017: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/29024676/perinatal-fluoxetine-prevents-the-effect-of-pre-gestational-maternal-stress-on-5-ht-in-the-pfc-but-maternal-stress-has-enduring-effects-on-mpfc-synaptic-structure-in-offspring
#5
Mary Gemmel, Nikolaos Kokras, Christina Dalla, Jodi L Pawluski
Maternal affective disorders are frequently treated with selective serotonin reuptake inhibitor medications (SSRIs); with up to 10% of women being prescribed these medications during pregnancy. Infant development depends on the early serotonergic environment, which is altered by perinatal SSRIs, raising concern about how these medications affect neural outcomes. While clinical and preclinical research suggests an impact of SSRIs on the developing brain, more research is needed to determine the effects on neuroplasticity, the serotonergic system, and the hypothalamic-pituitary-adrenal axis in neural regions mediating behavior...
October 9, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29024630/improved-chemoradiation-treatment-using-trifluridine-in-human-colorectal-cancer-cells-in-vitro
#6
Kazuaki Matsuoka, Takashi Kobunai, Mamoru Nukatsuka, Teiji Takechi
We aimed to assess the combined effect of trifluridine (FTD) and ionizing radiation (IR) on colorectal cancer cells in vitro. Colorectal cancer cells, HT-29, HCT-15, and HCT 116, showing low, medium, and high sensitivity to IR, respectively, were treated with the combinations of FTD and IR, and evaluated by the clonogenic survival assay. The radiation dose modification factors (DMFs) were calculated as the ratio of radiation doses producing equivalent surviving fractions following the FTD/IR treatment, or IR alone...
October 9, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29022008/inflammatory-activation-of-human-cardiac-fibroblasts-leads-to-altered-calcium-signaling-decreased-connexin-43-expression-and-increased-glutamate-secretion
#7
Eva Skiöldebrand, Annika Lundqvist, Ulrika Björklund, Mikael Sandstedt, Anders Lindahl, Elisabeth Hansson, Lillemor Mattsson Hultén
Cardiac fibroblasts, which are abundant in heart tissue, are involved not only in extracellular matrix homeostasis and repair, but also in cardiac remodeling after a myocardial infarction that, in turn, can lead to loss of cardiac function and heart failure. Ca(2+) signaling is functionally important in many cell types, but the roles of fibroblast signaling and inflammation in the pathogenesis of heart disease are unclear. Here, we tested the hypothesis that inflammatory activation affects cardiac fibroblasts, both in terms of Ca(2+) signaling and their capacity for intercellular communication through the gap junction channel protein connexin 43 (Cx43)...
October 2017: Heliyon
https://www.readbyqxmd.com/read/29020659/3d-gait-analysis-with-and-without-an-orthopedic-walking-boot
#8
H Gulgin, K Hall, A Luzadre, E Kayfish
INTRODUCTION: Orthopedic walking boots have been widely used in place of traditional fiberglass casts for a variety of orthopedic injuries and post-surgical interventions. These walking boots create a leg length discrepancy (LLD). LLD has been shown to alter the kinematics and kinetics of gait and are associated with lumbar and lower limb conditions such as: foot over pronation, low back pain, scoliosis, and osteoarthritis of the hip and knee joints. Past gait analyses research with orthopedic boots is limited to findings on the ipsilateral limb...
October 5, 2017: Gait & Posture
https://www.readbyqxmd.com/read/29020658/evaluation-of-the-performance-of-a-new-automated-hiv-combination-assay
#9
Valeria Ghisetti, Catherine Coignard, Tiziano Allice, Ly Thoai Duong
BACKGROUND: More and more countries test for HIV infection using combination assays that simultaneously detect p24 antigen and HIV antibodies. OBJECTIVE: To assess the performance of a new HIV combo assay: LIAISON(®) XL murex HIV Ab/Ag HT. STUDY DESIGN: The assays were examined with a total of 3090 samples that included 769 selected HIV antibody-negative samples, 1849 unselected HIV samples, 15 HIV-1 p24 Ag reference samples, 90 primary HIV-1 infection (PHI) samples, 167 HIV-1 antibody-positive samples (well characterized of groups M and O), 95 HIV-1 antibody-positive samples and 105 HIV-2 antibody-positive samples...
September 21, 2017: Journal of Clinical Virology: the Official Publication of the Pan American Society for Clinical Virology
https://www.readbyqxmd.com/read/29020039/er%C3%AE-36-a-variant-of-estrogen-receptor-%C3%AE-is-predominantly-localized-in-mitochondria-of-human-uterine-smooth-muscle-and-leiomyoma-cells
#10
Yitang Yan, Linda Yu, Lysandra Castro, Darlene Dixon
ERα36 is a naturally occurring, membrane-associated, isoform of estrogen receptor α. The expression of ERα36 is due to alternative splicing and different promoter usage. ERα36 is a dominant-negative effector of ERα66-mediated transactivational activities and has the potential to trigger membrane-initiated mitogenic, nongenomic, estrogen signaling; however, the subcellular localization of ERα36 remains controversial. To determine the cellular localization of ERα36 in estrogen-responsive human uterine smooth muscle (ht-UtSMC) and leiomyoma (fibroid; ht-UtLM) cells, we conducted systematic confocal microscopy and subcellular fractionation analysis using ERα36 antibodies...
2017: PloS One
https://www.readbyqxmd.com/read/29019881/assessment-of-left-ventricular-performance-in-heart-transplant-recipients-by-three-dimensional-speckle-tracking-imaging
#11
Dan Wang, Li Zhang, Qingyu Zeng, Mingxing Xie
To calculate left ventricular (LV) global performance values in heart transplant (HT) recipients by three-dimensional speckle tracking imaging (3D-STI) and to observe the changes in LV global performance over time after HT and investigate the correlated factors.The 30 HT patients were divided into 2 groups according to postoperative time: 1 month postoperatively (HT-1) group and 6 months postoperatively (HT-2) group. Thirty healthy subjects were enrolled as control group. 3D-STI was performed to assess LV torsion, LV systolic dyssynchrony index (SDI), and LV global strain (GS)...
October 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/29019086/family-history-influences-the-tumor-characteristics-and-prognosis-of-breast-cancers-developing-during-postmenopausal-hormone-therapy
#12
Rainer Fagerholm, Maria Faltinova, Kirsi Aaltonen, Kristiina Aittomäki, Päivi Heikkilä, Mervi Halttunen-Nieminen, Heli Nevanlinna, Carl Blomqvist
Long term use of postmenopausal hormone therapy (HT) has been reported to increase breast cancer risk. On the other hand, observational studies suggest that breast cancers diagnosed during HT may have a more favorable prognosis. While family history is a risk factor for breast cancer, and genetic factors also influence prognosis, the role of family history in combination with HT use has been little studied. We investigated the relationship between HT, family history, and prognosis in 584 (267 exposed) familial and 952 (460 exposed) non-familial breast cancer cases, using three survival end points: death from breast cancer (BCS), distant disease free survival (DDFS), and local recurrence free survival (LRFS)...
October 10, 2017: Familial Cancer
https://www.readbyqxmd.com/read/29018333/cadherin-13-deficiency-increases-dorsal-raphe-5-ht-neuron-density-and-prefrontal-cortex-innervation-in-the-mouse-brain
#13
Andrea Forero, Olga Rivero, Sina Wäldchen, Hsing-Ping Ku, Dominik P Kiser, Yvonne Gärtner, Laura S Pennington, Jonas Waider, Patricia Gaspar, Charline Jansch, Frank Edenhofer, Thérèse J Resink, Robert Blum, Markus Sauer, Klaus-Peter Lesch
Background: During early prenatal stages of brain development, serotonin (5-HT)-specific neurons migrate through somal translocation to form the raphe nuclei and subsequently begin to project to their target regions. The rostral cluster of cells, comprising the median and dorsal raphe (DR), innervates anterior regions of the brain, including the prefrontal cortex. Differential analysis of the mouse 5-HT system transcriptome identified enrichment of cell adhesion molecules in 5-HT neurons of the DR. One of these molecules, cadherin-13 (Cdh13) has been shown to play a role in cell migration, axon pathfinding, and synaptogenesis...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/28994012/comparative-in-vitro-toxicity-evaluation-of-heavy-metals-lead-cadmium-arsenic-and-methylmercury-on-ht-22-hippocampal-cell-line
#14
Venkatanaidu Karri, Vikas Kumar, David Ramos, Eliandre Oliveira, Marta Schuhmacher
Heavy metals are considered some of the most toxic environmental pollutants. Exposure to heavy metals including lead (Pb), cadmium (Cd), arsenic (As), and methyl mercury (MeHg) has long been known to cause damage to human health. Many recent studies have supported the hippocampus as the major target for these four metals for inflicting cognitive dysfunction. In the present study, we proposed hippocampal relevant in vitro toxicity of Pb, Cd, As, and MeHg in HT-22 cell line. This study reports, initially, cytotoxic effects in acute, subchronic, chronic exposures...
October 9, 2017: Biological Trace Element Research
https://www.readbyqxmd.com/read/28993881/maximal-rate-of-heart-rate-increase-correlates-with-fatigue-recovery-status-in-female-cyclists
#15
Maximillian J Nelson, Clint R Bellenger, Rebecca L Thomson, Eileen Y Robertson, Kade Davison, Daniela Schäfer Olstad, Jonathan D Buckley
PURPOSE: Being able to identify how an athlete is responding to training would be useful to optimise adaptation and performance. The maximal rate of heart rate increase (rHRI), a marker of heart rate acceleration has been shown to correlate with performance changes in response to changes in training load in male athletes; however, it has not been established if it also correlates with performance changes in female athletes. METHODS: rHRI and cycling performance were assessed in six female cyclists following 7 days of light training (LT), 14 days of heavy training (HT) and a 10 day taper period...
October 9, 2017: European Journal of Applied Physiology
https://www.readbyqxmd.com/read/28993239/regulation-of-nadph-oxidase-nox4-by-delta-iodolactone-il-%C3%AE-in-thyroid-cancer-cells
#16
Thomasz Lisa, Romina Oglio, Leonardo Salvarredi, Marina Perona, Luciano Rossich, Silvia Copelli, Mario Pisarev, Guillermo Juvenal
INTRODUCTION: Iodine is not used only by the thyroid to synthesize thyroid hormones but also directly influences a number of thyroid parameters such as thyroid proliferation and function. Several iodinated lipids, biosynthesized by the thyroid, were postulated as intermediaries in the action of iodide. Among these, iodolactone (IL-δ) and 2-iodohexadecanal (2-IHDA) have shown to inhibit several thyroid parameters. The antiproliferative effect of IL-δ is not restricted to the thyroid gland...
October 6, 2017: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/28991641/cardioprotection-of-stevioside-on-stunned-rat-hearts-a-mechano-energetical-study
#17
María I Ragone, Patricia Bonazzola, Germán A Colareda, María Lara Lazarte, Fiorella Bruno, Alicia E Consolini
BACKGROUND: The sweetener and hypoglycemic properties of stevioside (STV) are well known, as the main component of the plant Stevia rebaudiana. Given its extensive use in diabetic patients, it was of interest to evaluate its effects on the most frequent cardiovascular disease, the coronary insufficiency. PURPOSE: To study whether STV could be cardioprotective against ischemia-reperfusion (I/R) in a model of "stunning" in rat hearts. STUDY DESIGN: A preclinical study was performed in isolated hearts from rats in the following groups: non-treated rats whose hearts were perfused with STV 0...
November 15, 2017: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/28991443/renewable-alkenes-from-the-hydrothermal-treatment-of-polyhydroxyalkanoates-containing-sludge
#18
Cristian Torri, Tom Detert Oude Weme, Chiara Samorì, Alisar Kiwan, Derk W F Wim Brilman
Polyhydroxyalkanoates (PHA) are a key constituent of excess sludge produced by Aerobic Sewage Sludge Treatment plants. The accumulation of significant amount of PHA inside aerobic microbial cells occurs when a surplus of an easily degradable carbon source (e.g. volatile fatty acids, VFA) is found in combination with other nutrients limitation. Herein, hydrothermal treatment (HT) of PHA-containing sludge at 300 and 375°C was demonstrated to be effective in converting most (>70% w/w) of the bacterial PHA stored inside microbial cells into alkene/CO2 gas mixtures...
October 9, 2017: Environmental Science & Technology
https://www.readbyqxmd.com/read/28990263/early-aspirin-initiation-following-heart-transplantation-is-associated-with-reduced-risk-of-allograft-vasculopathy-during-long-term-follow-up
#19
Yael Peled, Jacob Lavee, Eugenia Raichlin, Moshe Katz, Michael Arad, Yigal Kassif, Amir Peled, Elad Asher, Dan Elian, Yedael Har-Zahav, Nir Shlomo, Dov Freimark, Ilan Goldenberg, Robert Klempfner
AIM: Cardiac allograft vasculopathy (CAV) is a major cause of morbidity and mortality after heart transplantation (HT). Enhanced platelet reactivity is a contributing factor. We aimed to investigate the association between early initiation of aspirin therapy post-HT and the 15-year risk of the development of CAV. METHODS: We studied 206 patients who underwent HT between 1991and 2016. Multivariate Cox proportional hazards regression modeling was employed to evaluate the association between early aspirin initiation and the long-term risk of CAV...
October 9, 2017: Clinical Transplantation
https://www.readbyqxmd.com/read/28990216/left-atrial-volume-changes-is-an-early-marker-of-end-organ-damage-in-essential-hypertension-a-multidisciplinary-approach-to-an-old-problem
#20
Batur Kanar, Beste Ozben, Hatice Selen Kanar, Aysu Arsan, Kursat Tigen
PURPOSE: Left atrial (LA) volume has been shown to be a predictor of adverse cardiovascular outcomes. The aim of this study was to evaluate the relation between LA phasic volumes and hypertensive end-organ damage (EOD), by using real time three-dimensional echocardiography (RT3DE) in patients with essential hypertension (HT). METHODS: The study included 95 essential hypertensive patients (60 ± 10 years, 37 males). The patients were divided into three according to the presence of EOD, namely microalbuminuria and retinal vascular changes detected by direct ophthalmoscopy...
October 9, 2017: Echocardiography
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