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https://www.readbyqxmd.com/read/27914363/new-insights-into-the-sar-and-drug-combination-synergy-of-2-quinolin-4-yloxy-acetamides-against-mycobacterium-tuberculosis
#1
Bruno Couto Giacobbo, Kenia Pissinate, Valnês Rodrigues-Junior, Anne Drumond Villela, Estêvão Silveira Grams, Bruno Lopes Abbadi, Fernanda Teixeira Subtil, Nathalia Sperotto, Rogério Valim Trindade, Davi Fernando Back, Maria Martha Campos, Luiz Augusto Basso, Pablo Machado, Diógenes Santiago Santos
2-(Quinolin-4-yloxy)acetamides have been described as potent and selective in vitro inhibitors of Mycobacterium tuberculosis (Mtb) growth. Herein, a new series of optimized compounds were found to demonstrate highly potent antitubercular activity, with minimum inhibitory concentration (MIC) values against drug-susceptible and drug-resistant Mycobacterium tuberculosis strains in the submicromolar range. Furthermore, the most active compounds had no apparent toxicity to mammalian cells, and they showed intracellular activities similar to those of isoniazid and rifampin in a macrophage model of Mtb infection...
November 23, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27914362/an-overview-of-the-binding-models-of-fgfr-tyrosine-kinases-in-complex-with-small-molecule-inhibitors
#2
REVIEW
Weiyan Cheng, Mixiang Wang, Xin Tian, Xiaojian Zhang
The fibroblast growth factor receptor (FGFR) family receptor tyrosine kinase (RTK) includes four structurally related members, termed as FGFR1, FGFR2, FGFR3, and FGFR4. Given its intimate role in the progression of several solid tumors, excessive FGFR signaling provides an opportunity for anticancer therapy. Along with extensive pharmacological studies validating the therapeutic potential of targeting the FGFRs for cancer treatment, co-crystal structures of FGFRs/inhibitors are continuously coming up to study the mechanism of actions and explore new inhibitors...
November 25, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27914320/biochemical-precursor-effects-on-the-fatty-acid-production-in-cell-suspension-cultures-of-theobroma-cacao-l
#3
O Parra, A M Gallego, A Urrea, L F Rojas, C Correa, L Atehortúa
Cocoa butter (CB) is composed of 96% palmitic, stearic, oleic, linoleic and linolenic fatty acids that are responsible for the hardness, texture and fusion properties of chocolate. Through in vitro plant cell culture it is possible to modify CB lipid profiles and to study the fatty acid biosynthesis pathway on a subcellular level, evaluating fundamental aspects to enhance in vitro fatty acid production in a specific and controlled way. In this research, culture media was supplemented with acetate, biotin, pyruvate, bicarbonate and glycerol at three different concentrations and the effects on the biomass production (g/L), cell viability, and fatty acids profile and production was evaluated in in vitro cell suspensions culture...
November 25, 2016: Plant Physiology and Biochemistry: PPB
https://www.readbyqxmd.com/read/27914270/surface-mediated-transfection-of-a-pdna-vector-encoding-short-hairpin-rna-to-downregulate-tgf-%C3%AE-1-expression-for-the-prevention-of-in-stent-restenosis
#4
He Zhang, Ke-Feng Ren, Hao Chang, Jin-Lei Wang, Jian Ji
In-stent restenosis is one of the most serious modes of failure of cardiovascular stent implant. Although drug-eluting stents have been proven to reduce in-stent restenosis, the nonspecific inhibitory effects of anti-proliferative drugs, such as rapamycin, result in delayed re-endothelialization and fatal late stent thrombosis. Although many studies have focused on promoting rapid re-endothelialization, a feasible method of reducing excessive extracellular matrix (ECM) production and cell proliferation might provide a promising way to efficiently inhibit the restenosis in vivo...
November 24, 2016: Biomaterials
https://www.readbyqxmd.com/read/27914269/targeted-hydroxyethyl-starch-prodrug-for-inhibiting-the-growth-and-metastasis-of-prostate-cancer
#5
Kaidong Zhao, Di Li, Weiguo Xu, Jianxun Ding, Weiqian Jiang, Mingqiang Li, Chunxi Wang, Xuesi Chen
Prostate cancer is one of the most prevalent malignancies among men. Although chemotherapy has been an effective therapeutic approach for treating metastatic prostate cancer, serious undesired side effects have hampered its wide application clinically. In this work, a pH-responsive LHRH-conjugated hydroxyethyl starch-doxorubicin (HES-DOX/LHRH) prodrug was facilely synthesized by conjugating oxidized HES (HES-CHO) with DOX and LHRH through an acid-sensitive Schiff base bond. The resulting prodrug spontaneously self-assembled into nanoscopic micelle with a radius of about 55 nm in an aqueous environment...
November 23, 2016: Biomaterials
https://www.readbyqxmd.com/read/27914268/anti-adhesive-antimicrobial-peptide-coating-prevents-catheter-associated-infection-in-a-mouse-urinary-infection-model
#6
Kai Yu, Joey C Y Lo, Mei Yan, Xiaoqiang Yang, Donald E Brooks, Robert E W Hancock, Dirk Lange, Jayachandran N Kizhakkedathu
Catheter-associated urinary tract infections (CAUTIs) represent one of the most common hospital acquired infections with significant economic consequences and increased patient morbidity. CAUTIs often start with pathogen adhesion and colonization on the catheter surface followed by biofilm formation. Current strategies to prevent CAUTIs are insufficiently effective and antimicrobial coatings based on antimicrobial peptides (AMPs) hold promise in curbing CAUTIs. Here we report an effective surface tethering strategy to prepare AMP coatings on polyurethane (PU), a common biomedical plastic used for catheter manufacture, by using an anti-adhesive hydrophilic polymer coating...
November 24, 2016: Biomaterials
https://www.readbyqxmd.com/read/27914264/pattern-based-sensing-of-triple-negative-breast-cancer-cells-with-dual-ligand-cofunctionalized-gold-nanoclusters
#7
Yu Tao, Mingqiang Li, Debra T Auguste
Early detection of breast cancer is a critical component in patient prognosis and establishing effective therapy regimens. Here, we developed an easily accessible yet potentially powerful sensor to detect cancer cell targets by utilizing seven dual-ligand cofunctionalized gold nanoclusters (AuNCs) as both effective cell recognition elements and signal transducers. On the basis of this AuNC multichannel sensor, we have successfully distinguished healthy, cancerous and metastatic human breast cells with excellent reproducibility and high sensitivity...
November 25, 2016: Biomaterials
https://www.readbyqxmd.com/read/27914258/centralised-decentralised-or-hybrid-sanitation-systems-economic-evaluation-under-urban-development-uncertainty-and-phased-expansion
#8
Ivar Roefs, Brendo Meulman, Jan H G Vreeburg, Marc Spiller
Sanitation systems are built to be robust, that is, they are dimensioned to cope with population growth and other variability that occurs throughout their lifetime. It was recently shown that building sanitation systems in phases is more cost effective than one robust design. This phasing can take place by building small autonomous decentralised units that operate closer to the actual demand. Research has shown that variability and uncertainty in urban development does affect the cost effectiveness of this approach...
November 23, 2016: Water Research
https://www.readbyqxmd.com/read/27914250/chitosan-nanoparticles-as-carrier-systems-for-the-plant-growth-hormone-gibberellic-acid
#9
Anderson Espirito Santo Pereira, Paula Mayara Silva, Jhones Luis Oliveira, Halley Caixeta Oliveira, Leonardo Fernandes Fraceto
This work concerns the development of nanocarriers composed of alginate/chitosan (ALG/CS) and chitosan/tripolyphosphate (CS/TPP) for the plant growth regulator gibberellic acid (GA3). ALG/CS nanoparticles with and without GA3 presented mean size of 450±10nm, polydispersity index (PDI) of 0.3, zeta potential of -29±0.5mV, concentrations of 1.52×10(11) and 1.92×10(11) nanoparticles mL(-1), respectively, and 100% encapsulation efficiency. CS/TPP nanoparticles with and without GA3 presented mean size of 195±1nm, PDI of 0...
November 23, 2016: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/27914228/osteoblastic-extraosseous-osteosarcoma-of-the-neck
#10
Andro Košec, Majda Vučić, Vladimir Bedeković, Mirko Ivkić
Extraosseous osteosarcoma as a primary tumor of the neck is exceedingly rare, with only a few cases reported to date. The most appropriate therapy is still under investigation. We report a case of an aggressive, right-sided, advanced-stage extraosseous osteosarcoma in a female patient. A 48-year-old woman presented with a right-sided infra-parotid mass encompassing neck regions II and III, measuring over 6 cm in craniocaudal diameter. She was initially treated by wide surgical resection. The definitive histopathologic diagnosis was osteoblastic extraosseous osteosarcoma...
November 16, 2016: Journal of Oral and Maxillofacial Surgery
https://www.readbyqxmd.com/read/27914214/antithrombin-improves-the-maternal-and-neonatal-outcomes-but-not-the-angiogenic-factors-in-extremely-growth-restricted-fetuses-at-28-weeks-of-gestation
#11
Midori Fujisaki, Ken Furuta, Masanao Ohhashi, Seishi Furukawa, Yuki Kodama, Yasuyuki Kawagoe, Hiroshi Sameshima, Tsuyomu Ikenoue
AIMS: Severe preterm fetal growth restriction (FGR) remote from term is problematic. We aimed to investigate the effect of maternally-administered antithrombin on maternal and neonatal outcomes. A prospective, one-arm, pilot study was performed in 14 women with severe FGR (≤5th centile) at <28 weeks of gestation, without hypertensive disorders. Maternal plasma concentrations of soluble Feline McDonough Sarcoma (FMS)-like trypsin kinase-1 (sFlt-1) and placental growth factor (PlGF) were measured and categorized into three groups: group 1; low sFlt-1 and high PlGF, group 2; moderate sFlt-1 and low PlGF, and group 3; high sFlt-1 and low PlGF...
December 3, 2016: Journal of Perinatal Medicine
https://www.readbyqxmd.com/read/27914208/effect-of-rhizobacterial-consortia-from-undisturbed-arid-and-agro-ecosystems-on-wheat-growth-under-differing-conditions
#12
N G Inostroza, P J Barra, L Y Wick, M L Mora, M A Jorquera
Plant-growth promoting rhizobacteria (PGPR) are studied as complements/alternatives to chemical fertilization in agriculture. Poor information however, exists on the potential of PGPR from undisturbed ecosystems. Here, we evaluated the plant growth-promoting (PGP) effect of rhizobacterial consortia from undisturbed Chilean arid-ecosystems (Consortium C1) and agro-ecosystems (Consortium C2) on plant biomass production. The PGP effects of C1 and C2 were assayed in wheat seedlings (Triticum aestivum L.) grown in pots under growth chamber conditions and in pots placed in an open greenhouse under natural conditions, using two different Chilean Andisols (Piedras Negras and Freire series) kept either at 30% or 60% of their maximum water holding capacity (MWHC)...
December 3, 2016: Letters in Applied Microbiology
https://www.readbyqxmd.com/read/27914202/probiotic-roles-of-lactobacillus-spp-in-swine-insights-from-gut-microbiota
#13
REVIEW
Valerie Diane V Valeriano, Marilen P Balolong, Dae-Kyung Kang
The use of lactobacilli as probiotics in swine has been gaining attention due to their ability to improve growth performance and carcass quality, prevent gastrointestinal infection, and most importantly, their 'generally recognised as safe' status. Previous studies support the potential of lactobacilli to regulate host immune systems, enhance gut metabolic capacities, and maintain balance in the gut microbiota. Research on swine gut microbiota has revealed complex gut microbial community structure and showed the importance of Lactobacillus to the host's health...
December 3, 2016: Journal of Applied Microbiology
https://www.readbyqxmd.com/read/27914199/filamin-a-synaptic-organizer-in-drosophila-determines-glutamate-receptor-composition-and-membrane-growth
#14
GaYoung Lee, Thomas L Schwarz
Filamin is a scaffolding protein that functions in many cells as an actin-crosslinker. FLN90, an isoform of the Drosophila ortholog Filamin/cheerio that lacks the actin-binding domain, is here shown to govern the growth of postsynaptic membrane folds and the composition of glutamate receptor clusters at the larval neuromuscular junction. Genetic and biochemical analyses revealed that FLN90 is present surrounding synaptic boutons. FLN90 is required in the muscle for localization of the kinase dPak and, downstream of dPak, for localization of the GTPase Ral and the exocyst complex to this region...
December 3, 2016: ELife
https://www.readbyqxmd.com/read/27914187/enhanced-nutrition-improves-growth-and-increases-blood-adiponectin-concentrations-in-very-low-birth-weight-infants
#15
Elin W Blakstad, Sissel J Moltu, Britt Nakstad, Marit B Veierød, Kenneth Strømmen, Pétur B Júlíusson, Astrid N Almaas, Arild E Rønnestad, Kristin Brække, Christian A Drevon, Per O Iversen
BACKGROUND: Adequate nutrient supply is essential for optimal postnatal growth in very low birth weight (VLBW, birth weight<1,500 g) infants. Early growth may influence the risk of metabolic syndrome later in life. OBJECTIVE: To evaluate growth and blood metabolic markers (adiponectin, leptin, and insulin-like growth factor-1 (IGF-1)) in VLBW infants participating in a randomized nutritional intervention study. DESIGN: Fifty VLBW infants were randomized to an enhanced nutrient supply or a standard nutrient supply...
2016: Food & Nutrition Research
https://www.readbyqxmd.com/read/27914126/effects-of-platelet-rich-plasma-on-kidney-regeneration-in-gentamicin-induced-nephrotoxicity
#16
Abbas Moghadam, Tahereh Talaei Khozani, Afsaneh Mafi, Mohammad Reza Namavar, Farzaneh Dehghani
Platelet-rich plasma (PRP) as a source of growth factors may induce tissue repairing and improve fibrosis. This study aimed to assess the effects of PRP on kidney regeneration and fibrosis in gentamicin (GM)-induced nephrotoxicity rat model by stereological study. Thirty-two male rats were selected. Nephrotoxicity was induced in animals by administration of GM (80 mg/kg/daily, intraperitoneally [IP], 8 day) and animals were treated by PRP (100 μL, intra-cortical injection using surgical microscopy, single dose)...
January 2017: Journal of Korean Medical Science
https://www.readbyqxmd.com/read/27914124/atypical-neonatal-marfan-syndrome-with-p-glu1073lys-mutation-of-fbn1-the-first-case-in-korea
#17
Ju Sun Heo, Joo Young Song, Eun Young Choi, Eun Hee Kim, Ji Hee Kim, So Eun Park, Ji Hyun Jeon
Neonatal Marfan syndrome (nMFS) is considered to be on the most severe end of the spectrum of type I fibrillinopathies. The common features of nMFS include ascending aortic dilatation, severe mitral and/or tricuspid valve insufficiency, ectopia lentis, arachnodactyly, joint contractures, crumpled ear, loose skin, and pulmonary emphysema.We describe a newborn male diagnosed with nMFS. He presented several atypical features, such as diaphragmatic eventration, severe hydronephrosis with hydroureter, and dilated cisterna magna...
January 2017: Journal of Korean Medical Science
https://www.readbyqxmd.com/read/27914087/in-vitro-and-in-vivo-biofilm-formation-by-pathogenic-streptococci
#18
Yashuan Chao, Caroline Bergenfelz, Anders P Håkansson
This manuscript presents novel approaches to grow and evaluate Streptococcal biofilm formation using the human respiratory pathogen Streptococcus pneumoniae (the pneumococcus) as the main model organism on biological surfaces in vitro and in vivo. Most biofilm models are based on growth on abiotic surfaces, which is relevant for many pathogens whose growth on surfaces or medical devices is a major cause of disease transmission and infections, especially in hospital environments. However, most infections with commensal organisms require biofilm formation on biological surfaces in the host at the site of colonization or infection...
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/27914027/the-role-of-guided-growth-as-it-relates-to-limb-lengthening
#19
REVIEW
Peter M Stevens
For decades, the classic indication for limb lengthening has been reserved for anisomelia that was expected to reach or exceed 5 cm at maturity. Epiphysiodesis was reserved for discrepancies in the 2-5 cm range. With the increasing sophistication of fixators, including rail, hexapod, and hybrid, complex deformities may be corrected simultaneously while moderate to extreme lengthening is achieved. More recently, iterations of telescoping intramedullary rods have further strengthened our armamentarium. Meanwhile, permanent epiphysiodesis techniques, both open and percutaneous, have yielded to more versatile and reversible tethering of one (angle) or both (length) sides of a physis...
December 2, 2016: Journal of Children's Orthopaedics
https://www.readbyqxmd.com/read/27914018/encapsulation-of-%C3%AE-sitosterol-in-polyurethane-by-sol-gel-electrospinning
#20
Musarat Amina, Touseef Amna, Nawal Al-Musayeib, Sami A Zabin, M Shamshi Hassan, Myung-Seob Khil
Pristine β-sitosterol or in combination with other phytosterols is utilized in an array of enriched commercial foods. Considering the presence of β-sitosterol in different functional foods and its potential role in prevention and cure of neurodegenerative diseases, the aims of our investigation were to encapsulate β-sitosterol in nanofibers and to estimate influence of β-sitosterol on proliferation of fibroblasts. Electrospun nanofibers have widely been used as scaffolds to mimic natural extracellular matrix...
December 2, 2016: Applied Biochemistry and Biotechnology
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