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https://www.readbyqxmd.com/read/29161777/structure-based-design-and-evaluation-of-synthetic-porphyrin-derivatives-as-g-quadruplex-stabilizing-anticancer-agents
#1
R N Bhadane, D B Meshram, R M Gilhotra
G-quadruplex structures formed in telomeres and proto-oncogene represent a potentially useful target for anticancer drugs. Stabilization of this arrangement may inhibit the further action of different enzymes involved in cancer cell immortalization. In present work structure based drug design and synthesis was carried out on series of meso-substituted porphyrin analogues. The interaction of porphyrin derivatives with G-quadruplex DNA has been explored by virtual screening procedure. Some of the potential binding agents were then synthesized and evaluated in-vitro by MTT and PCR stop assay...
November 2017: Journal of Experimental Therapeutics & Oncology
https://www.readbyqxmd.com/read/29161765/mir-335-inhibited-cell-proliferation-of-lung-cancer-cells-by-target-tra2%C3%AE
#2
Jian Liu, Tingting Bian, Jia Feng, Li Qian, Jianguo Zhang, Daishan Jiang, Qing Zhang, Xiaoli Li, Yifei Liu, Jiahai Shi
Accumulating evidence has suggested that the dysregulation of miRNAs is an important factor in the pathogenesis of lung cancer. Here, we demonstrate that miR-335 expression is reduced in non-small cell lung cancer (NSCLC) tumors relative to non-cancerous adjacent tissues, whilst the expression of Tra2β is increased. In addition, clinical data revealed that the increased Tra2β and decreased miR-335 expression observed in NSCLC cells was associated with poor patient survival rates. In-vitro experimentation showed that the overexpression of miR-335 inhibited the growth, invasion and migration capabilities of A459 lung cancer cells, by targeting Tra2β...
November 21, 2017: Cancer Science
https://www.readbyqxmd.com/read/29161763/quantifying-the-relationship-between-inhibition-of-vegfr-2-drug-induced-blood-pressure-elevation-and-hypertension
#3
Teresa Collins, Kelly Gray, Michal Bista, Matt Skinner, Christopher Hardy, Haiyun Wang, Jerome T Mettetal, Alexander R Harmer
BACKGROUND AND PURPOSE: Several anti-angiogenic cancer drugs that inhibit VEGF receptor (VEGFR) signalling for efficacy are associated with a 15-60% incidence of hypertension. Tyrosine kinase inhibitors (TKIs) that have off-target activity at VEGFR-2 may also cause blood pressure elevation as an undesirable side effect. Therefore, the ability to translate VEGFR-2 off-target potency into blood pressure elevation would be useful in development of novel TKIs. EXPERIMENTAL APPROACH: We sought to quantify the relationship between VEGFR-2 inhibition and blood pressure elevation for a range of kinase inhibitors...
November 21, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29161755/kv-1-channel-expression-and-vasomotor-function-in-human-coronary-resistance-arteries
#4
Yoshinori Nishijima, Ankush Korishettar, Dawid S Chabowski, Sheng Cao, Xiaodong Zheng, David D Gutterman, David X Zhang
OBJECTIVES: KV channels are important regulators of vascular tone, but the identity of specific KV channels involved and their regulation in disease remain less well understood. We determined the expression of KV 1 channel subunits and their role in cAMP-mediated dilation in coronary resistance arteries from subjects with and without coronary artery disease (CAD). METHODS: Human coronary arteries and arterioles (HCA) from non-CAD and CAD patients were assessed for mRNA and protein expression of KV 1 channel subunits with molecular techniques and for vasodilator response with isolated arterial myography...
November 21, 2017: Microcirculation: the Official Journal of the Microcirculatory Society, Inc
https://www.readbyqxmd.com/read/29161753/improving-the-efficacy-of-proteasome-inhibitors-in-the-treatment-of-renal-cell-carcinoma-by-combination-with-the-hiv-protease-inhibitors-lopinavir-or-nelfinavir
#5
Dominik Abt, Andrej Besse, Lenka Sedlarikova, Marianne Kraus, Juergen Bader, Tobias Silzle, Martina Vodinska, Ondrej Slaby, Hans-Peter Schmid, Daniel Stephan Engeler, Christoph Driessen, Lenka Besse
OBJECTIVES: To assess the potential of second-generation proteasome inhibition by carfilzomib and its combination with the HIV-protease inhibitors (HIV-PIs) lopinavir and nelfinavir in vitro for improved treatment of clear cell renal cell cancer (ccRCC). MATERIALS AND METHODS: Cytotoxicity, reactive oxygen species (ROS) production and unfolded protein response (UPR) activation of proteasome inhibitors, HIV-PIs and their combination was assessed in 3 cell lines and primary cells derived from 3 ccRCC tumors by MTS assay, flow cytometry, quantitative PCR and western blot, respectively...
November 21, 2017: BJU International
https://www.readbyqxmd.com/read/29161746/exercise-performed-concomitantly-with-particulate-matter-exposure-inhibits-lung-injury
#6
Adriano Silva-Renno, Guilherme Crisitanini Baldivia, Manoel C Oliveira-Junior, Maysa Alves Rodrigues Brandao-Rangel, Elias El-Mafarjeh, Marisa Dolhnikoff, Thaís Mauad, Jôse Mára Britto, Paulo Hilário Nascimento Saldiva, Luis Vicente Franco Oliveira, Ana P Ligeiro-Oliveira, Gustavo Silveira Graudenz, Rodolfo Paula Vieira
Air pollution is a growing problem worldwide, inducing and exacerbating several diseases. Among the several components of air pollutants, particulate matter (PM), especially thick (10-2.5 µm; PM 10) and thin (≤2.5 µm; PM 2.5), are breathable particles that easily can be deposited within the lungs, resulting in pulmonary and systemic inflammation. Although physical activity is strongly recommended, its effects when practiced in polluted environments are questionable. Therefore, the present study evaluated the pulmonary and systemic response of concomitant treadmill training with PM 2...
November 21, 2017: International Journal of Sports Medicine
https://www.readbyqxmd.com/read/29161719/palmitic-acid-curcumin-ester-facilitates-protection-of-neuroblastoma-against-oligomeric-a%C3%AE-40-insult
#7
Zhangyang Qi, Meihao Wu, Yun Fu, Tengfei Huang, Tingting Wang, Yanjie Sun, Zhibo Feng, Changzheng Li
BACKGROUND/AIMS: The generation of reactive oxygen species (ROS) caused by amyloid-β (Aβ) is considered to be one of mechanisms underlying the development of Alzheimer's disease. Curcumin can attenuate Aβ-induced neurotoxicity through ROS scavenging, but the protective effect of intracellular curcumin on neurocyte membranes against extracellular Aβ may be compromised. To address this issue, we synthesized a palmitic acid curcumin ester (P-curcumin) which can be cultivated on the cell membrane and investigated the neuroprotective effect of P-curcumin and its interaction with Aβ...
November 20, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/29161701/yin-yang-1-dynamically-regulates-antiviral-innate-immune-responses-during-viral-infection
#8
Jie Zan, Hao Zhang, Ai-Ping Gu, Kai-Lun Zhong, Min-Yi Lu, Xiao-Xin Bai, Jin-Yang Zhang, Jun Cai
BACKGROUND/AIMS: Type I interferon (IFN-1) production and IFN-1 signaling play critical roles in the host antiviral innate immune responses. Although transcription factor Yin Yang 1 (YY1) has been reported to have a dual activator/repressor role during the regulation of interferon beta (IFN-β) promoter activity, the roles of YY1 in the regulation of upstream signaling pathways leading to IFN-1 induction and IFN-1 signaling during viral infection remain to be elucidated. METHODS: The roles of YY1 in IFN-1 production and IFN-1 signaling were investigated using immunoblotting, real-time PCR, small interfering RNA (siRNA)-mediated YY1 knockdown, YY1 overexpression by transient transfection, and co-immunoprecipitation, using mouse cells...
November 20, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/29161690/catechins-blunt-the-effects-of-oxldl-and-its-primary-metabolite-phosphatidylcholine-hydroperoxide-on-endothelial-dysfunction-through-inhibition-of-oxidative-stress-and-restoration-of-enos-in-rats
#9
Hao-Hsiang Chang, Chen-Yen Chien, Kuo-Hsin Chen, Shih-Chung Huang, Chiang-Ting Chien
BACKGROUND/AIMS: We explored the effects of catechins (decaffeinated green tea extracts containing (-)-epicatechin, (-)-epigallocatechin, (-)-epicatechin gallate and (-)-epigallocatechin gallate) on atherosclerosis risk factors, oxidized low-density lipoprotein (oxLDL) and its primary metabolite, phosphatidylcholine hydroperoxide (PCOOH) induced oxidative injury in cultured endothelial cell line and rats. METHODS: We used endothelial cell line and male Wistar rats to determine the effect of catechins on oxLDL or PCOOH induced oxidative injury including apoptosis, H2O2 level, vascular responses and urinary 8-isoprostane and nitrite/nitrate concentration...
November 22, 2017: Kidney & Blood Pressure Research
https://www.readbyqxmd.com/read/29161662/deiodination-of-iopamidol-by-zero-valent-iron-zvi-enhances-formation-of-iodinated-disinfection-by-products-during-chloramination
#10
Huiyu Dong, Zhimin Qiang, Junfeng Lian, Jin Li, Jianwei Yu, Jiuhui Qu
Iodinated X-ray contrast media (ICM) is considered as one of iodine sources for formation of toxic iodinated disinfection byproducts (I-DBPs) during disinfection. This study investigated transformation of a typical ICM, iopamidol (IPM) by zero valent iron (ZVI) and the effect of transformation on the formation of I-DBPs during chloramination. It was found that the presence of ZVI could deiodinate IPM into I(-) and the transformation of IPM exhibited a pseudo-first-order kinetics. Acidic circumstance, SO4(2-), Cl(-) and monochloramine could promote the transformation of IPM by ZVI, while SiO3(2-) inhibited the transformation of IPM...
November 14, 2017: Water Research
https://www.readbyqxmd.com/read/29161661/chlorogenic-acid-prevents-diabetic-nephropathy-by-inhibiting-oxidative-stress-and-inflammation-through-modulation-of-the-nrf2-ho-1-and-nf-%C3%A4-b-pathways
#11
Liping Bao, Jushuang Li, Dongqing Zha, Lian Zhang, Ping Gao, Tao Yao, Xiaoyan Wu
Oxidative and inflammatory damage have been suggested to play important roles in the pathogenesis of diabetic nephropathy (DN). Chlorogenic acid (CGA) is one of the most abundant polyphenols and has known immunoprotective, antioxidant and anti-inflammatory properties. In the present study, animal experiments were designed to examine the protective effects of CGA in DN, and cellular experiments were designed to explore the underlying mechanisms. CGA significantly attenuated diabetic renal damage based on histological pathology and molecular biological methods...
November 18, 2017: International Immunopharmacology
https://www.readbyqxmd.com/read/29161627/nanoscaled-red-blood-cells-facilitate-breast-cancer-treatment-by-combining-photothermal-photodynamic-therapy-and-chemotherapy
#12
Guoyun Wan, Bowei Chen, Ling Li, Dan Wang, Shurui Shi, Tao Zhang, Yue Wang, Lianyun Zhang, Yinsong Wang
Red blood cells (RBCs)-based vesicles have been widely used for drug delivery due to their unique advantages. Intact RBCs contain a large amount of oxyhemoglobin (oxyHb), which can assist with photodynamic therapy (PDT). Indocyanine green (ICG), a photosensitizer both for photothermal therapy (PTT) and PDT, shows potent anticancer efficacy when combined with chemotherapeutic drug doxorubicin (DOX). In this study, we prepared nanoscaled RBCs (RAs) containing oxyHb and gas-generating agent ammonium bicarbonate (ABC) for co-loading and controlled release of ICG and DOX, thus hoping to achieve synergistic effects of PTT/PDT and chemotherapy against breast cancer...
November 14, 2017: Biomaterials
https://www.readbyqxmd.com/read/29161574/fast-spectroscopic-monitoring-of-inhibitors-in-the-2g-ethanol-process
#13
Ariane S S Pinto, Marcelo P A Ribeiro, Cristiane S Farinas
One of the main challenges of second generation (2G) ethanol production is the high quantities of phenolic compounds and furan derivatives generated in the pretreatment of the lignocellulosic biomass, which inhibit the enzymatic hydrolysis and fermentation steps. Fast monitoring of these inhibitory compounds could provide better control of the pretreatment, hydrolysis, and fermentation processes by enabling the implementation of strategic process control actions. We investigated the feasibility of monitoring these inhibitory compounds by ultraviolet-visible (UV-Vis) spectroscopy associated with partial least squares (PLS) regression...
November 14, 2017: Bioresource Technology
https://www.readbyqxmd.com/read/29161568/feasibility-of-high-concentration-cellulosic-bioethanol-production-from-undetoxified-whole-monterey-pine-slurry
#14
Chengyu Dong, Ying Wang, Han Zhang, Shao-Yuan Leu
The economic feasibility of high-concentration cellulosic bioethanol production remains challenging because it requires easily available feedstock and low energy consumption process. Simultaneous saccharification and fermentation (SSF) of sulfite pretreated Momentary pine slurry at 20% (w/w) loadings increased ethanol concentration from 59.3 g/L to 68.5 g/L by washing strategy. Effects of inhibitors in pretreatment liquor were further investigated. Besides HMF, furfural and acetic acid, other inhibitors and/or their synergistic effects proved to be responsible for a lower fermentability...
November 11, 2017: Bioresource Technology
https://www.readbyqxmd.com/read/29161499/polymerization-of-well-aligned-organic-nanowires-on-a-ferromagnetic-rare-earth-surface-alloy
#15
Mikel Abadía, Maxim Ilyn, Ignacio Piquero-Zulaica, Pierluigi Gargiani, Celia Rogero, Jose Enrique Ortega, Jens Brede
The high reactivity of magnetic substrate toward molecular overlayers has so far inhibited the realization of more sophisticated on-surface reactions thereby depriving these interfaces of a significant class of chemically tailored organics such as graphene nanoribbons, oligonuclear spin-chains, and metal-organic networks. Here, we present a multi-technique characterization of the polymerization of 4,4″-dibromo-p-terphenyl precursors into ordered poly (p-phenylene) arrays on top of the bi-metallic GdAu$_2$ surface alloy...
November 21, 2017: ACS Nano
https://www.readbyqxmd.com/read/29161409/transfer-and-metabolism-of-cortisol-by-the-isolated-perfused-human-placenta
#16
Laura I Stirrat, Bram G Sengers, Jane E Norman, Natalie Z M Homer, Ruth Andrew, Rohan M Lewis, Rebecca M Reynolds
Context: Fetal overexposure to glucocorticoids in utero is associated with fetal growth restriction and is postulated to be a key mechanism linking suboptimal fetal growth with cardiovascular disease in later life. Objective: To develop a model to predict maternal-fetal glucocorticoid transfer. We hypothesised placental 11β-HSD2 would be the major rate-limiting step in maternal cortisol transfer to the fetus. Design: We used a deuterated cortisol tracer in the ex vivo placental perfusion model, in combination with computational modelling, to investigate the role of interconversion of cortisol and its inactive metabolite cortisone on transfer of cortisol from mother to fetus...
November 16, 2017: Journal of Clinical Endocrinology and Metabolism
https://www.readbyqxmd.com/read/29161390/thiopental-to-desflurane-an-anaesthetic-journey-where-are-we-going-next
#17
J R Sneyd
Development targets in anaesthetic pharmacology have evolved from minimizing harm caused by unwanted effects through an era in which rapid onset and offset of drug effect were prioritised. Today's anaesthetists have access to a library of effective drugs whose characteristics offer controllable hypnosis, analgesia and paralysis with manageable off-target effects. The availability of these agents at generic prices inhibits commercial interest and this is reflected in the limited number of current anaesthetic drug development projects...
December 1, 2017: British Journal of Anaesthesia
https://www.readbyqxmd.com/read/29161383/basal-forebrain-gating-by-somatostatin-neurons-drives-prefrontal-cortical-activity
#18
Nelson Espinosa, Alejandra Alonso, Cristian Morales, Pedro Espinosa, Andrés E Chávez, Pablo Fuentealba
The basal forebrain provides modulatory input to the cortex regulating brain states and cognitive processing. Somatostatin-expressing neurons constitute a heterogeneous GABAergic population known to functionally inhibit basal forebrain cortically projecting cells thus favoring sleep and cortical synchronization. However, it remains unclear if somatostatin cells can regulate population activity patterns in the basal forebrain and modulate cortical dynamics. Here, we demonstrate that somatostatin neurons regulate the corticopetal synaptic output of the basal forebrain impinging on cortical activity and behavior...
November 17, 2017: Cerebral Cortex
https://www.readbyqxmd.com/read/29161356/medial-orbitofrontal-cortex-mediates-effort-related-responding-in-rats
#19
Alexandra Münster, Wolfgang Hauber
The medial orbitofrontal cortex (mOFC) is known to support flexible control of goal-directed behavior. However, limited evidence suggests that the mOFC also mediates the ability of organisms to work with vigor towards a selected goal, a hypothesis that received little consideration to date. Here we show that excitotoxic mOFC lesion increased responding under a progressive ratio (PR) schedule of reinforcement, that is, the highest ratio achieved, and increased the preference for the high effort-high reward option in an effort-related decision-making task, but left intact outcome-selective Pavlovian-instrumental transfer and outcome-specific devaluation...
November 17, 2017: Cerebral Cortex
https://www.readbyqxmd.com/read/29161332/osteoglycin-inhibition-by-microrna-mir-155-impairs-myogenesis
#20
Paula Paccielli Freire, Sarah Santiloni Cury, Grasieli de Oliveira, Geysson Javier Fernandez, Leonardo Nazario Moraes, Bruno Oliveira da Silva Duran, Juarez Henrique Ferreira, César Seigi Fuziwara, Edna Teruko Kimura, Maeli Dal-Pai-Silva, Robson Francisco Carvalho
Skeletal myogenesis is a regulated process in which mononucleated cells, the myoblasts, undergo proliferation and differentiation. Upon differentiation, the cells align with each other, and subsequently fuse to form terminally differentiated multinucleated myotubes. Previous reports have identified the protein osteoglycin (Ogn) as an important component of the skeletal muscle secretome, which is expressed differentially during muscle development. However, the posttranscriptional regulation of Ogn by microRNAs during myogenesis is unknown...
2017: PloS One
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