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https://www.readbyqxmd.com/read/29158524/mechanisms-underlying-the-antiproliferative-effects-of-a-series-of-quinoxaline-derived-chalcones
#1
Tânia R Mielcke, Thaís C Muradás, Eduardo C Filippi-Chiela, Maria Eduarda A Amaral, Luiza W Kist, Maurício R Bogo, Alessandra Mascarello, Patrícia D Neuenfeldt, Ricardo J Nunes, Maria M Campos
The present study aimed to characterize the effects of quinoxaline-derived chalcones, designed on the basis of the selective PI3Kγ inhibitor AS605240, in oral cancer cells. Three lead compounds, namely N9, N17 and N23, were selected from a series of 20 quinoxaline-derived chalcones, based on an initial screening using human and rat squamous cell carcinoma lineages, representing compounds with at least one methoxy radical at the A-ring. The selected chalcones, mainly N9 and N17, displayed marked antiproliferative effects, via apoptosis and autophagy induction, with an increase of sub-G1 population and Akt inhibition...
November 20, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29157002/effects-of-circadian-clock-protein-per1b-on-zebrafish-visual-functions
#2
Ke Nie, Kun Wang, Deng-Feng Huang, Yu-Bin Huang, Wu Yin, Da-Long Ren, Han Wang, Bing Hu
The circadian clock is an endogenous and entrainable time-keeping mechanism with a period of approximately 24 h, operated by transcription/translation feedback loops composed of circadian clock genes and their proteins. The visual system displays robust circadian changes. Relatively little, however, is known about the mechanisms underlying visual circadian rhythmicity. Zebrafish period1b (per1b), as a canonical circadian clock gene, is involved in circadian regulation. Here, we observed that zebrafish per1b mutants exhibit visual defects including reduced behavioral contrast sensitivity and significant retinal dopaminergic deficiency...
November 20, 2017: Chronobiology International
https://www.readbyqxmd.com/read/29155009/thresholds-for-sine-wave-corrugations-defined-by-binocular-disparity-in-random-dot-stereograms-factor-analysis-of-individual-differences-revealstwo-stereoscopic-mechanisms-tuned-for-spatial-frequency
#3
David H Peterzell, Ignacio Serrano-Pedraza, Michael Widdall, Jenny C A Read
Threshold functions for sinusoidal depth corrugations typically reach their minimum (highest sensitivity) at spatial frequencies of 0.2-0.4 cycles/degree (cpd), with lower thresholds for horizontal than vertical corrugations at low spatial frequencies. To elucidate spatial frequency and orientation tuning of stereoscopic mechanisms, we measured the disparity sensitivity functions, and used factor analytic techniques to estimate the existence of independent underlying stereo channels. The data set (N=30 individuals) was for horizontal and vertical corrugations of spatial frequencies ranging from 0...
November 15, 2017: Vision Research
https://www.readbyqxmd.com/read/29150587/a-passion-for-cats-and-people
#4
(no author information available yet)
Sheila Wills has worked extensively but not exclusively with cats. More recently she was appointed director of an organisation that accredits veterinary CPD and awards veterinary qualifications worldwide.
November 18, 2017: Veterinary Record
https://www.readbyqxmd.com/read/29140819/positive-and-negative-impacts-of-a-continuing-professional-development-intervention-on-pharmacist-practice-a-balanced-measure-evaluation
#5
Sukhjinder Sidhu, Sean K Gorman, Richard S Slavik, Tasha Ramsey, Nicole Bruchet, Sarah Murray
INTRODUCTION: Evaluations of behavior change interventions aimed at improving professional practice are increasingly focused on impacts at the practice and patient outcome levels. Many of these evaluations assume that if the intended changes occur, the result represents an improvement. However, given the systemic nature of clinical practice, a change in one area can produce changes in other areas as well, some of which may adversely affect the patient. Balancing measures are used to determine whether unintended consequences of an intervention have been introduced into other areas of the system...
November 14, 2017: Journal of Continuing Education in the Health Professions
https://www.readbyqxmd.com/read/29131831/substrate-specificity-of-human-metallocarboxypeptidase-d-comparison-of-the-two-active-carboxypeptidase-domains
#6
Javier Garcia-Pardo, Sebastian Tanco, Lucía Díaz, Sayani Dasgupta, Juan Fernandez-Recio, Julia Lorenzo, Francesc X Aviles, Lloyd D Fricker
Metallocarboxypeptidase D (CPD) is a membrane-bound component of the trans-Golgi network that cycles to the cell surface through exocytic and endocytic pathways. Unlike other members of the metallocarboxypeptidase family, CPD is a multicatalytic enzyme with three carboxypeptidase-like domains, although only the first two domains are predicted to be enzymatically active. To investigate the enzymatic properties of each domain in human CPD, a critical active site Glu in domain I and/or II was mutated to Gln and the protein expressed, purified, and assayed with a wide variety of peptide substrates...
2017: PloS One
https://www.readbyqxmd.com/read/29123298/hands-on-experience-cpd-and-clinically-proven-solutions
#7
(no author information available yet)
No abstract text is available yet for this article.
November 10, 2017: British Dental Journal
https://www.readbyqxmd.com/read/29119190/reactivity-and-regioselectivity-in-diels-alder-reactions-of-anion-encapsulated-fullerenes
#8
Cheng-Xing Cui, Zhao-Pei Zhang, Lei Zhu, Ling-Bo Qu, Yu-Ping Zhang, Yu Lan
Encapsulation and surface chemical modification are methodologies to enhance the properties of fullerenes for various applications. Herein, density functional theory calculations are performed to study the Diels-Alder (DA) reactivity of anion encapsulated C60, including [X@C60](-) (X = F, Cl, Br, or I), [S@C60](2-), and [N@C60](3-). Computational results reveal that encapsulated Cl(-), Br(-), I(-), or S(2-) anions are located close to the center of the C60 molecule; however, encapsulated F(-) is displaced from the center...
November 22, 2017: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/29114355/molecular-cytogenetic-characterization-and-comparison-of-the-two-cultivated-canavalia-species-fabaceae
#9
Chao-Wen She, Lin Wei, Xiang-Hui Jiang
The two cultivated Canavalia (Adanson, 1763) species, Canavalia gladiata (N. J. von Jacquin, 1788) A. P. de Candolle, 1825 and Canavalia ensiformis (Linnaeus, 1753) A. P. de Candolle, 1825 are closely related based on morphological and molecular phylogenetic data. However, the similarities and differences in genome organization between them have not been evaluated at molecular cytogenetic level. Here, detailed karyotypes of both species were constructed using combined PI and DAPI (CPD) staining, rDNA-FISH and self-genomic in situ hybridization (sGISH)...
2017: Comparative Cytogenetics
https://www.readbyqxmd.com/read/29112988/relationship-between-spending-on-electronic-cigarettes-30-day-use-and-disease-symptoms-among-current-adult-cigarette-smokers-in-the-u-s
#10
Tingting Yao, Wendy Max, Hai-Yen Sung, Stanton A Glantz, Rachel L Goldberg, Julie B Wang, Yingning Wang, James Lightwood, Janine Cataldo
OBJECTIVE: To examine the relationship between spending on electronic cigarettes (e-cigarettes) and disease symptoms compared with the relationship between 30-day e-cigarette use and disease symptoms among adult cigarette smokers in the U.S. METHODS: We analyzed data from the Tobacco and Attitudes Beliefs Survey which included 533 respondents aged 24+ who were current cigarette smokers and e-cigarette ever users. Fifteen self-reported disease symptoms were included as outcome variables...
2017: PloS One
https://www.readbyqxmd.com/read/29110298/long-term-genoprotection-effect-of-sechium-edule-fruit-extract-against-uva-irradiation-in-keratinocytes
#11
Elodie Metral, Walid Rachidi, Odile Damour, Frédéric Demarne, Nicolas Bechetoille
Photoprotection is essential to prevent the long-term deleterious effects of ultraviolet (UV), including skin cancer and photoaging. So far, there has been an increase in the use of natural bioactive phytochemicals for the development of more effective skin photoprotective agents. However, the molecular mechanisms underlying the photochemoprotection activity of such compounds remain largely unknown. The objective of this study was to investigate the effects of a Sechium edule fruit extract (SEE) in terms of photoprotection against UVA in primary human keratinocytes...
November 7, 2017: Photochemistry and Photobiology
https://www.readbyqxmd.com/read/29109511/ash1l-histone-methyltransferase-regulates-the-handoff-between-damage-recognition-factors-in-global-genome-nucleotide-excision-repair
#12
Chiara Balbo Pogliano, Marco Gatti, Peter Rüthemann, Zuzana Garajovà, Lorenza Penengo, Hanspeter Naegeli
Global-genome nucleotide excision repair (GG-NER) prevents ultraviolet (UV) light-induced skin cancer by removing mutagenic cyclobutane pyrimidine dimers (CPDs). These lesions are formed abundantly on DNA wrapped around histone octamers in nucleosomes, but a specialized damage sensor known as DDB2 ensures that they are accessed by the XPC initiator of GG-NER activity. We report that DDB2 promotes CPD excision by recruiting the histone methyltransferase ASH1L, which methylates lysine 4 of histone H3. In turn, methylated H3 facilitates the docking of the XPC complex to nucleosomal histone octamers...
November 6, 2017: Nature Communications
https://www.readbyqxmd.com/read/29101868/disinfection-and-healing-effects-of-222-nm-uvc-light-on-methicillin-resistant-staphylococcus-aureus-infection-in-mouse-wounds
#13
Kouji Narita, Krisana Asano, Yukihiro Morimoto, Tatsushi Igarashi, Michael R Hamblin, Tianhong Dai, Akio Nakane
UVC radiation is known to be highly germicidal. However, exposure to 254-nm-UVC light causes DNA lesions such as cyclobutane pyrimidine dimers (CPD) in human cells, and can induce skin cancer after long-term repeated exposures. It has been reported that short wavelength UVC is absorbed by proteins in the membrane and cytosol, and fails to reach the nucleus of human cells. Hence, irradiation with 222-nm UVC might be an optimum combination of effective disinfection and biological safety to human cells. In this study, the biological effectiveness of 222-nm UVC was investigated using a mouse model of a skin wound infected with methicillin-resistant Staphylococcus aureus (MRSA)...
October 27, 2017: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/29101813/cytotoxic-and-cytostatic-effects-of-digitoxigenin-monodigitoxoside-dgx-in-human-lung-cancer-cells-and-its-link-to-na-k-atpase
#14
Naira Fernanda Zanchett Schneider, Lara Persich, Sayonarah C Rocha, Ana Carolina Pacheco Ramos, Vanessa Faria Cortes, Izabella Thaís Silva, Jennifer Munkert, Rodrigo M Pádua, Wolfgang Kreis, Alex G Taranto, Leandro A Barbosa, Fernão C Braga, Cláudia M O Simões
Cardiac glycosides (CGs) are natural compounds widely used to treat several cardiac conditions and more recently have been recognized as potential antitumor agents. They are known as Na,K-ATPases ligands, which is a promising drug target in cancer. In this study, the short and long-lasting cytotoxic effects of the natural cardenolide digitoxigenin monodigitoxoside (DGX) were evaluated against two non-small cell lung cancer lines (A549 and H460 cells). It was found that DGX induced cytotoxic effects in both cells and the apoptotic effects were more pronounced on H460 cells...
November 1, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29098941/efflux-transporter-breast-cancer-resistance-protein-dominantly-expresses-on-the-membrane-of-red-blood-cells-hinders-partitioning-of-its-substrates-into-the-cells-and-alters-drug-drug-interaction-profiles
#15
Pu Shi, Mingxiang Liao, Bei-Ching Chuang, Robert Griffin, Judy Shi, Marc Hyer, John K Fallon, Philip C Smith, Chao Li, Cindy Q Xia
1. Red blood cell (RBC) partitioning is important in determining pharmacokinetic and pharmacodynamic properties of a compound; however, active transport across RBC membranes is not well understood, particularly without transporter-related cell membrane proteomics data. 2. In this study, we quantified breast cancer resistance protein (BCRP/Bcrp) and MDR1/P-glycoprotein (P-gp) protein expression in RBCs from humans, monkeys, dogs, rats, and mice using nanoLC/MS/MS, and evaluated their effect on RBC partitioning and plasma exposure of their substrates...
November 3, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/29098885/formulation-strategy-towards-minimizing-viscosity-mediated-negative-food-effect-on-disintegration-and-dissolution-of-immediate-release-tablets
#16
Kamran Zaheer, Peter Langguth
Food induced viscosity can delay disintegration and subsequent release of API from solid dosage form which may lead to severe reduction in the bioavailability of BCS type III compounds. Formulations of such tablets need to be optimized in view of this postprandial viscosity factor. In this study, three super disintegrants, croscarmellose sodium (CCS), cross-linked polyvinylpolypyrrolidone (CPD) and sodium starch glycolate (SSG) were assessed for their efficiency under simulated fed state. Tablets containing these disintegrants were compressed at 10 KN and 30 KN, while taking lactose as a soluble filler...
November 3, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/29089850/characterization-of-enterococcal-community-isolated-%C3%A2-from-an-artisan-istrian-raw-milk-cheese-biotechnological-and-safety-aspects
#17
Mirna Mrkonjic Fuka, Ana Zgomba Maksimovic, Irina Tanuwidjaja, Natasa Hulak, Michael Schloter
In this study, prevalence, biotechnological and safety profiles of 588 Enterococcus isolates isolated from raw milk and Istrian cheese during different stages of ripening were analyzed. Despite the low and variable presence of enterococci in milk ((3.65±2.93) log CFU/mL), highly comparable enterococcal populations were established after 30 days of cheese ripening ((7.96±0.80) log CFU/g), confirming Enterococcus spp. as a major part of the core microbiota of Istrian cheese. The dominant species were E. faecium (53...
September 2017: Food Technology and Biotechnology
https://www.readbyqxmd.com/read/29083287/the-impact-of-e-cigarettes-on-smoking-and-related-outcomes-in-veteran-smokers-with-psychiatric-comorbidity
#18
Gerald W Valentine, Kathryn Hefner, Peter I Jatlow, Robert A Rosenheck, Ralitza Gueorguieva, Mehmet Sofuoglu
OBJECTIVE: Compared to the general U.S. population, smokers with comorbid psychiatric and/or substance use disorders (SUD) have lower quit rates after evidence-based treatments, and disproportionately high smoking-related deaths. Improved modalities for reducing tobacco-related harm in this subpopulation are needed. Because electronic cigarettes (e-cigarettes) can now deliver physiologically relevant levels of nicotine to consumers, they represent an additional nicotine delivery system that could be used in cessation interventions...
October 30, 2017: Journal of Dual Diagnosis
https://www.readbyqxmd.com/read/29056674/the-awareness-of-the-international-veterinary-profession-of-evidence-based-veterinary-medicine-and-preferred-methods-of-training
#19
Selene J Huntley, Rachel S Dean, Marnie L Brennan
Evidence-based veterinary medicine (EVM) is an evolving discipline in veterinary medicine so it is important to periodically "benchmark" opinion about EVM across the profession. An international survey to assess veterinarians' awareness of EVM was conducted. Veterinarians were surveyed via an online questionnaire (all countries) or a postal questionnaire (UK only). Participants were asked whether they had heard of EVM, where they had first heard the term, and their preferences of method for receiving continuing professional development (CPD)...
March 8, 2017: Veterinary Sciences
https://www.readbyqxmd.com/read/29054834/evaluation-of-web-based-continuing-professional-development-courses-aggregate-mixed-methods-model
#20
Arezoo Ebn Ahmady, Megan Barker, Myra Fahim, Rosa Dragonetti, Peter Selby
BACKGROUND: Many continuing professional development (CPD) Web-based programs are not explicit about underlying theory and fail to demonstrate impact. OBJECTIVE: The aim of this study was to develop and apply an aggregate mixed-methods evaluation model to describe the paradigm, theoretical framework, and methodological approaches used to evaluate a CPD course in tobacco dependence treatment, the Training Enhancement in Applied Cessation Counseling and Health (TEACH) project...
October 20, 2017: JMIR Medical Education
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