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https://www.readbyqxmd.com/read/28212337/synthesis-anti-breast-cancer-activity-and-molecular-docking-study-of-a-new-group-of-acetylenic-quinolinesulfonamide-derivatives
#1
Krzysztof Marciniec, Bartosz Pawełczak, Małgorzata Latocha, Leszek Skrzypek, Małgorzata Maciążek-Jurczyk, Stanisław Boryczka
In this study, a series of regioisomeric acetylenic sulfamoylquinolines are designed, synthesized, and tested in vitro for their antiproliferative activity against three human breast cacer cell lines (T47D, MCF-7, and MDA-MB-231) and a human normal fibroblast (HFF-1) by 4-[3-(4-iodophenyl)-2-(4-nitrophenyl)-2H-5-tetrazolio]-1,3-benzene disulfonate (WST-1) assay. The antiproliferative activity of the tested acetylenic quinolinesulfonamides is comparable to that of cisplatin. The bioassay results demonstrate that most of the tested compounds show potent antitumor activities, and that some compounds exhibit better effects than the positive control cisplatin against various cancer cell lines...
February 16, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28212280/biofilm-formation-and-immunomodulatory-activity-of-proteus-mirabilis-clinically-isolated-strains
#2
Alessandra Fusco, Lorena Coretti, Vittoria Savio, Elisabetta Buommino, Francesca Lembo, Giovanna Donnarumma
Urinary tract infections (UTIs) and catheter-associated UTIs (CAUTIs) are the principal hospital-acquired infections. Proteus mirabilis is characterized by several virulence factors able to promote adhesion and biofilm formation and ameliorate the colonization of urinary tract and the formation of crystalline biofilms on the abiotic surface of the urinary catheters. Since, to date, the role of P. mirabilis in the etiopathogenesis of different types of urinary tract infections is not well established, in this study we sought to characterize two different clinically isolated strains of P...
February 15, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28212032/chrodrimanins-k-n-and-related-meroterpenoids-from-the-fungus-penicillium-sp-scs-kfd09-isolated-from-a-marine-worm-sipunculus-nudus
#3
Fan-Dong Kong, Qing-Yun Ma, Sheng-Zhuo Huang, Pei Wang, Jun-Feng Wang, Li-Man Zhou, Jing-Zhe Yuan, Hao-Fu Dai, You-Xing Zhao
Six new meroterpenoids, chrodrimanins K-N (1-4), including two uncommon chlorinated ones (1 and 2), and verruculides B2 (5) and B3 (6), as well as seven known ones (7-13), were isolated from the fermentation broth of Penicillium sp. SCS-KFD09 isolated from a marine worm, Sipunculus nudus, from Haikou Bay, China. The structures including the absolute configurations of the new compounds were unambiguously elucidated by spectroscopic data, X-ray diffraction analysis, and ECD spectra analysis along with quantum ECD calculations...
February 17, 2017: Journal of Natural Products
https://www.readbyqxmd.com/read/28211697/benchmarking-density-functionals-for-chemical-bonds-of-gold
#4
Kasper Planeta Kepp
Gold plays a major role in nanochemistry, catalysis, and electrochemistry. Accordingly, hundreds of studies apply density functionals to study chemical bonding with gold, yet there is no systematic attempt to assess the accuracy of these methods applied to gold. This paper reports a benchmark against 51 experimental bond enthalpies of AuX systems and seven additional polyatomic and cationic molecules. 12 density functionals were tested, covering meta functionals, hybrids with variable HF exchange, double-hybrid, dispersion-corrected and non-hybrid GGA functionals...
February 17, 2017: Journal of Physical Chemistry. A
https://www.readbyqxmd.com/read/28211481/effects-of-strength-training-on-osteogenic-differentiation-and-bone-strength-in-aging-female-wistar-rats
#5
Monique Patricio Singulani, Camila Tami Stringhetta-Garcia, Leandro Figueiredo Santos, Samuel Rodrigues Lourenço Morais, Mário Jefferson Quirino Louzada, Sandra Helena Penha Oliveira, Antonio Hernandes Chaves Neto, Rita Cássia Menegati Dornelles
The effects of strength training (ST) on the mechanical bone strength and osteogenic differentiation of bone marrow mesenchymal stromal cells (BMSCs) from adult, aged and exercised aged rats were determined. The exercised aged animals displayed higher values of areal bone mineral density, compression test, alkaline phosphatase activity (ALP) and biological mineralization, while oil red O staining for adipocytes was lower. ST increased gene expression of runt-related transcription factor 2 (Runx2), osterix (Osx) as well as bone matrix protein expression, and reduced expression of peroxisome proliferator-activated receptor gamma (Pparγ)...
February 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28211263/increased-regurgitant-flow-causes-endocardial-cushion-defects-in-an-avian-embryonic-model-of-congenital-heart-disease
#6
Stephanie M Ford, Matthew T McPheeters, Yves T Wang, Pei Ma, Shi Gu, James Strainic, Christopher Snyder, Andrew M Rollins, Michiko Watanabe, Michael W Jenkins
BACKGROUND: The relationship between changes in endocardial cushion and resultant congenital heart diseases (CHD) has yet to be established. It has been shown that increased regurgitant flow early in embryonic heart development leads to endocardial cushion defects, but it remains unclear how abnormal endocardial cushions during the looping stages might affect the fully septated heart. The goal of this study was to reproducibly alter blood flow in vivo and then quantify the resultant effects on morphology of endocardial cushions in the looping heart and on CHDs in the septated heart...
February 17, 2017: Congenital Heart Disease
https://www.readbyqxmd.com/read/28211076/comparison-of-conditional-bias-adjusted-estimators-for-interim-analysis-in-clinical-trials-with-survival-data
#7
Masashi Shimura, Masahiko Gosho, Akihiro Hirakawa
Group sequential designs are widely used in clinical trials to determine whether a trial should be terminated early. In such trials, maximum likelihood estimates are often used to describe the difference in efficacy between the experimental and reference treatments; however, these are well known for displaying conditional and unconditional biases. Established bias-adjusted estimators include the conditional mean-adjusted estimator (CMAE), conditional median unbiased estimator, conditional uniformly minimum variance unbiased estimator (CUMVUE), and weighted estimator...
February 17, 2017: Statistics in Medicine
https://www.readbyqxmd.com/read/28210626/osteogenic-differentiation-capacity-of-in-vitro-cultured-human-skeletal-muscle-for-expedited-bone-tissue-engineering
#8
Chunlei Miao, Lulu Zhou, Lufeng Tian, Yingjie Zhang, Wei Zhang, Fanghong Yang, Tianyi Liu, Shengjian Tang, Fangjun Liu
Expedited bone tissue engineering employs the biological stimuli to harness the intrinsic regenerative potential of skeletal muscle to trigger the reparative process in situ to improve or replace biological functions. When genetically modified with adenovirus mediated BMP2 gene transfer, muscle biopsies from animals have demonstrated success in regenerating bone within rat bony defects. However, it is uncertain whether the human adult skeletal muscle displays an osteogenic potential in vitro when a suitable biological trigger is applied...
2017: BioMed Research International
https://www.readbyqxmd.com/read/28210096/interactive-data-exploration-with-smart-drill-down
#9
Manas Joglekar, Hector Garcia-Molina, Aditya Parameswaran
We present smart drill-down, an operator for interactively exploring a relational table to discover and summarize "interesting" groups of tuples. Each group of tuples is described by a rule. For instance, the rule (a, b, ⋆, 1000) tells us that there are a thousand tuples with value a in the first column and b in the second column (and any value in the third column). Smart drill-down presents an analyst with a list of rules that together describe interesting aspects of the table. The analyst can tailor the definition of interesting, and can interactively apply smart drill-down on an existing rule to explore that part of the table...
May 2016: Proceedings
https://www.readbyqxmd.com/read/28209719/adaptive-nk-cells-can-persist-in-patients-with-gata2-mutation-depleted-of-stem-and-progenitor-cells
#10
Heinrich Schlums, Moonjung Jung, Hongya Han, Jakob Theorell, Venetia Bigley, Samuel C C Chiang, David S J Allan, Jan K Davidson-Moncada, Rachel E Dickinson, Tim D Holmes, Amy P Hsu, Danielle Townsley, Thomas Winkler, Weixin Wang, Pål Aukrust, Ingvild Nordøy, Katherine R Calvo, Steve M Holland, Matthew Collin, Cynthia E Dunbar, Yenan T Bryceson
Heterozygous GATA2 mutation is associated with immunodeficiency, lymphedema, and myelodysplastic syndrome. Disease presentation is variable, often coinciding with loss of circulating dendritic cells, monocytes, B cells, and NK cells. Nonetheless, in a proportion of patients carrying GATA2 mutation, NK cells persist. We found that peripheral blood NK cells in symptomatic patients uniformly lacked expression of the transcription factor PLZF, as well as expression of intracellular signaling proteins FcϵRγ, SYK, and EAT-2 in a variegated manner...
February 16, 2017: Blood
https://www.readbyqxmd.com/read/28208772/transcriptional-and-behavioral-responses-of-zebrafish-larvae-to-microcystin-lr-exposure
#11
Eleni Tzima, Iliana Serifi, Ioanna Tsikari, Ainhoa Alzualde, Ioannis Leonardos, Thomais Papamarcaki
Microcystins are cyclic heptapeptides that constitute a diverse group of toxins produced by cyanobacteria. One of the most toxic variants of this family is microcystin-LR (MCLR) which is a potent inhibitor of protein phosphatase 2A (PP2A) and induces cytoskeleton alterations. In this study, zebrafish larvae exposed to 500 μg/L of MCLR for four days exhibited a 40% reduction of PP2A activity compared to the controls, indicating early effects of the toxin. Gene expression profiling of the MCLR-exposed larvae using microarray analysis revealed that keratin 96 (krt96) was the most downregulated gene, consistent with the well-documented effects of MCLR on cytoskeleton structure...
February 9, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28208300/near-infrared-probe-based-on-rhodamine-derivative-for-highly-sensitive-and-selective-lysosomal-ph-tracking
#12
Guangle Niu, Panpan Zhang, Weimin Liu, Mengqi Wang, Hongyan Zhang, Jiasheng Wu, Liping Zhang, Pengfei Wang
The development of near-infrared fluorescent probes with low pKa, high selectivity, high photostability, and high sensitivity for lysosomal pH detection is of great importance. In the present work, we developed a novel near-infrared lysosomal pH probe (Lyso-hNR) based on a rhodamine derivative. Lyso-hNR showed fast, highly sensitive, and highly selective fluorescence response to acidic pH caused by the H(+)-induced structure changes from the nonfluorescent spirolactam form to the highly emissive open-ring form...
February 7, 2017: Analytical Chemistry
https://www.readbyqxmd.com/read/28206964/association-of-15-hydroxyprostaglandin-dehydrogenate-and-poor-prognosis-of-obese-breast-cancer-patients
#13
Ruxing Wu, Tao Liu, Peiwen Yang, Xiyou Liu, Fei Liu, Ya Wang, Huihua Xiong, Shiying Yu, Xiaoyuan Huang, Liang Zhuang
In order to explore the new mechanism that obesity worsens the prognosis of breast cancer, we reanalyzed the data about gene expression of normal, overweight, and obese breast cancer patients to explore potential genes and validate its function by clinical and experimental data. The fold change of 15-hydroxyprostaglandin dehydrogenate (HPGD) gene which displayed declining trend with BMI increase was 0.46 in obese versus normal weight patients. HPGD protein was highest expressed in normal weight group and lowest expressed in obese group...
February 11, 2017: Oncotarget
https://www.readbyqxmd.com/read/28206698/fkbp10-deletion-in-osteoblasts-leads-to-qualitative-defects-in-bone
#14
Caressa D Lietman, Joohyun Lim, Ingo Grafe, Yuqing Chen, Hao Ding, Xiaohong Bi, Catherine G Ambrose, Nadja Fratzl-Zelman, Paul Roschger, Klaus Klaushofer, Wolfgang Wagermaier, Ingo Schmidt, Peter Fratzl, Jyoti Rai, MaryAnn Weis, David Eyre, Douglas R Keene, Deborah Krakow, Brendan H Lee
Osteogenesis Imperfecta (OI), also known as brittle bone disease, displays a spectrum of clinical severity from mild (OI type I) to severe early lethality (OI type II), with clinical features including low bone mass, fractures and deformities. Mutations in the FK506 Binding Protein 10 (FKBP10), gene encoding the 65KDa protein FKBP65, cause a recessive form of OI and Bruck syndrome, the latter being characterized by joint contractures in addition to low bone mass. We previously showed that Fkbp10 expression is limited to bone, tendon and ligaments in postnatal tissues...
February 16, 2017: Journal of Bone and Mineral Research: the Official Journal of the American Society for Bone and Mineral Research
https://www.readbyqxmd.com/read/28205614/cxcr2-deficient-mice-display-macrophage-dependent-exaggerated-acute-inflammatory-responses
#15
Douglas P Dyer, Kenneth Pallas, Laura Medina Ruiz, Fabian Schuette, Gillian J Wilson, Gerard J Graham
CXCR2 is an essential regulator of neutrophil recruitment to inflamed and damaged sites and plays prominent roles in inflammatory pathologies and cancer. It has therefore been highlighted as an important therapeutic target. However the success of the therapeutic targeting of CXCR2 is threatened by our relative lack of knowledge of its precise in vivo mode of action. Here we demonstrate that CXCR2-deficient mice display a counterintuitive transient exaggerated inflammatory response to cutaneous and peritoneal inflammatory stimuli...
February 16, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28205583/flavichalasines-a-m-cytochalasan-alkaloids-from-aspergillus-flavipes
#16
Guangzheng Wei, Dongdong Tan, Chunmei Chen, Qingyi Tong, Xiao-Nian Li, Jinfeng Huang, Junjun Liu, Yongbo Xue, Jianping Wang, Zengwei Luo, Hucheng Zhu, Yonghui Zhang
Two new tetracyclic cytochalasans, flavichalasines A and B (1 and 2), three new pentacyclic cytochalasans, flavichalasines C-E (3-5), and eight new tricyclic cytochalasans, flavichalasines F-M (6-13), together with eight known analogues (14-21), were isolated from the solid culture of Aspergillus flavipes. Structures of these new compounds were elucidated on the basis of extensive spectroscopic analyses including 1D, 2D NMR and HRESIMS data. Their absolute configurations were determined by comparison of their experimental ECD with either computed ECD or experimental ECD spectrum of known compound...
February 13, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28204819/lncrna-co-expression-network-model-for-the-prognostic-analysis-of-acute-myeloid-leukemia
#17
Jia-Qi Pan, Yan-Qing Zhang, Jing-Hua Wang, Ping Xu, Wei Wang
Acute myeloid leukemia (AML) is a highly heterogeneous hematologic malignancy with great variability of prognostic behaviors. Previous studies have reported that long non-coding RNAs (lncRNAs) play an important role in AML and may thus be used as potential prognostic biomarkers. However, thus use of lncRNAs as prognostic biomarkers in AML and their detailed mechanisms of action in this disease have not yet been well characterized. For this purpose, in the present study, the expression levels of lncRNAs and mRNAs were calculated using the RNA-seq V2 data for AML, following which a lncRNA‑lncRNA co-expression network (LLCN) was constructed...
February 13, 2017: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/28204807/phytosphingosine-1-phosphate-and-epidermal-growth-factor-synergistically-restore-extracellular-matrix-in-human-dermal-fibroblasts-in-vitro-and-in-vivo
#18
Seung Bin Kwon, Sungkwan An, Min Jung Kim, Ka Ram Kim, Young Min Choi, Kyu Joong Ahn, In-Sook An, Hwa Jun Cha
Phytosphingosine-1-phosphate (PhS1P), which is found in plants and fungi, is generated by the phosphorylation of phytosphingosine and is structurally similar to molecules that promote cellular growth and proliferation. The aim of this study was to ascertain whether PhS1P displays synergistic effects together with epidermal growth factor (EGF), which is also critical for activating proliferation, migration and survival pathways. We utilized cultured human dermal fibroblasts (HDFs) and a number of assays, including western blotting, cell migration assays, quantitative (real-time) PCR, and viability assays...
January 23, 2017: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/28203671/heat-shock-antagonizes-uva-induced-responses-in-murine-melanocytes-and-melanoma-cells-an-unexpected-interaction
#19
Leonardo Vinícius Monteiro de Assis, Maria Nathália Moraes, Ana Maria de Lauro Castrucci
The skin is under the influence of oscillatory factors such as light and temperature. This organ possesses a local system that controls several aspects in a time-dependent manner; moreover, the skin has a well-known set of opsins whose function is still unknown. We demonstrate that heat shock reduces Opn2 expression in normal Melan-a melanocytes, while the opposite effect is found in malignant B16-F10 cells. In both cell lines, UVA radiation increases the expression of Opn4 and melanin content. Clock genes and Xpa, a DNA repair gene, of malignant melanocytes are more responsive to UVA radiation when compared to normal cells...
February 16, 2017: Photochemical & Photobiological Sciences
https://www.readbyqxmd.com/read/28203419/diagnosis-of-mitral-valve-cleft-using-real-time-3-dimensional-echocardiography
#20
Xinchun Yuan, Aiyun Zhou, Li Chen, Cheng Zhang, Yan Zhang, Pan Xu
BACKGROUND: Mitral valve cleft (MVC) is the most common cause of congenital mitral insufficiency, and MVC may occur alone or in association with other congenital heart lesions. Direct suture and valvuloplasty are the major and effective treatments for mitral regurgitation (MR) caused by MVC. Therefore, it is important to determine the location and magnitude of the pathological damage due to MVC when selecting a surgical procedure for treatment. This study explored the application value of transthoracic real-time 3-dimensional (3D) echocardiography (RT-3DE) in the diagnosis of MVC...
January 2017: Journal of Thoracic Disease
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