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Inhibitory control

Mostafa M Ghorab, Mansour S Alsaid, Ghada H Al-Ansary, Ghada A Abdel-Latif, Dalal A Abou El Ella
Twenty novel chromene derivatives carrying different sulfonamide moieties (3-22) were designed and synthesized. All the newly prepared compounds were evaluated for their in vitro anticancer activity against breast cancer cell line (T47D). Most of the synthesized compounds showed good to moderate activity (IC50 = 8.8-108.9 μM), where compound 16 (IC50 = 8.8 μM) exhibited higher activity compared to doxorubicin (IC50 = 9.8 μM). In order to determine the mechanism of the anticancer activity in T47D cells, the effect of the most potent compounds (5-8, 11-14, and 16-18) on the aromatase activity was tested...
October 13, 2016: European Journal of Medicinal Chemistry
Xuehua Piao, Soh Yamazaki, Sachiko Komazawa-Sakon, Sanae Miyake, Osamu Nakabayashi, Takeyuki Kurosawa, Tetsuo Mikami, Minoru Tanaka, Nico Van Rooijen, Masaki Ohmuraya, Akira Oikawa, Yuko Kojima, Soichiro Kakuta, Yasuo Uchiyama, Masato Tanaka, Hiroyasu Nakano
: Tissue-resident macrophages and bone marrow (BM)-derived monocytes play a crucial role in the maintenance of tissue homeostasis; however, their contribution to recovery from acute tissue injury is not fully understood. To address this issue, we generated an acute murine liver injury model using hepatocyte-specific Cflar-deficient (Cflar(Hep-low) ) mice. Cellular FLICE-inhibitory protein (cFLIP) expression was downregulated in Cflar-deficient hepatocytes, which thereby increased susceptibility of hepatocytes to death receptor-induced apoptosis...
October 22, 2016: Hepatology: Official Journal of the American Association for the Study of Liver Diseases
Leili Beytollahi, Maryam Pourhajibagher, Nasim Chiniforush, Roghayeh Ghorbanzadeh, Reza Raoofian, Babak Pourakbari, Bahador Abbas
BACKGROUND: The alternative antibacterial treatments of photodynamic therapy (PDT) and photothermal therapy (PTT) significantly affect microbiota inactivation. The aim of the present research was the assessment of the antimicrobial and anti-biofilm effects of PDT with toluidine blue O (TBO) and PTT with indocyanine green (ICG) on Streptococcus mutans as a cariogenic bacterium. MATERIALS AND METHODS: The S. mutans ATCC 35668 strain was treated with final concentrations of 0...
October 18, 2016: Photodiagnosis and Photodynamic Therapy
A Aguirre-Quiñonero, L Martínez-Martínez
Infections caused by carbapenemase-producing bacteria are becoming a major clinical and public health concern. Detection of carbapenemase producing strains is often challenging, since susceptibility to carbapenems may vary significantly among carbapenemase producers. Some carbapenemases have shown to exhibit weak activity against carbapenems leading to minimum inhibitory concentrations of carbapenems below the breakpoint for defining clinical resistance and even below the proposed screening breakpoint. Thus, reliable and rapid detection of carbapenemase-activity is needed for an appropriate patient management and a rapid implementation of infection prevention and control measures...
October 18, 2016: Journal of Infection and Chemotherapy: Official Journal of the Japan Society of Chemotherapy
Wei Fan, Yanyun Li, Qing Sun, Tengjiao Ma, Bing Fan
BACKGROUND: In infected periapical tissues, Enterococcus faecalis is one of the most common dominant bacteria. Chlorhexidine has been proved to show strong antibacterial ability against E. faecalis but is ineffective in promoting mineralization for tissues around root apex. Mesoporous calcium-silicate nanoparticles are newly synthesized biomaterials with excellent ability to promote mineralization and carry-release bioactive molecules in a controlled manner. In this study, mesoporous calcium-silicate nanoparticles were functionalized with chlorhexidine and their releasing profile, antibacterial ability, effect on cell proliferation and in vitro mineralization property were evaluated...
October 21, 2016: Journal of Nanobiotechnology
William M Jackson, Nicholas Davis, Stephen A Sands, Robert A Whittington, Lena S Sun
RESEARCH QUESTION: Is there an association between regular exercise, defined as a structured program of increased physical activity at least 1 month in duration, and improvements in measures of executive functions compared with children who engage in their normal daily activities? CONTEXT: The association between increased physical activity and changes in performance on tasks of executive functions have not been well elucidated in children. Executive functioning is important to intellectual development and academic success in children, and inexpensive, nonpharmacological methods for the treatment of executive dysfunction represent an attractive interventional target...
October 2016: Journal of Neurosurgical Anesthesiology
Patrícia Napoleão, Teresa Freitas, Carlota Saldanha
AIMS: Oxidized low density lipoprotein (ox-LDL) has been reported as an inhibitor of nitric oxide (NO)-mediated dilatation in microcirculation. Oxidized LDL effect on NO metabolism of erythrocytes is not known. Therefore, this study aims to evaluate the effect of ox-LDL on erythrocytes NO metabolism. METHODS: The effect of different concentrations of human purified ox-LDL (25, 50 and 100 μg/mL) on NO metabolism was evaluated on blood of healthy subjects. RESULTS: An inhibitory effect of higher concentrations of ox-LDL on erythrocyte NO efflux levels was verified...
October 20, 2016: Clinical Hemorheology and Microcirculation
Christian Kärgel, Claudia Massau, Simone Weiß, Martin Walter, Viola Borchardt, Tillmann H C Krueger, Gilian Tenbergen, Jonas Kneer, Matthias Wittfoth, Alexander Pohl, Hannah Gerwinn, Jorge Ponseti, Till Amelung, Klaus M Beier, Sebastian Mohnke, Henrik Walter, Boris Schiffer
Neurobehavioral models of pedophilia and child sexual offending suggest a pattern of temporal and in particular prefrontal disturbances leading to inappropriate behavioral control and subsequently an increased propensity to sexually offend against children. However, clear empirical evidence for such mechanisms is still missing. Using a go/nogo paradigm in combination with functional magnetic resonance imaging (fMRI) we compared behavioral performance and neural response patterns among three groups of men matched for age and IQ: pedophiles with (N = 40) and without (N = 37) a history of hands-on sexual offences against children as well as healthy non-offending controls (N = 40)...
October 21, 2016: Human Brain Mapping
Shiyun Tang, Jianlian Shi, Chunbo Liu, Rui Jiang, Wei Zhao, Xin Liu, Nengjun Xiang, Yongkuan Chen, Qinpeng Shen, Mingming Miao, Zhihua Liu, Guangyu Yang
Three new phenylpropanoids, 3-(3,4-dimethoxy-5-methylphenyl)-3-oxopropyl acetate (1), 3-hydroxy-1-(3,4-dimethoxy-5-methylphenyl)propan-1-one (2), and 3-hydroxy-1-(4-methylbenzo[d][1,3]dioxol-6-yl) propan-1-one (3), together with three known phenylpropanoids (4-6) were isolated from the whole plant of Lavandula angustifolia. Their structures were determined by means of HRESIMS and extensive 1D and 2D NMR spectroscopic studies. Compounds 1-6 were tested for their anti-tobacoo mosaic virus (TMV) activities and cytotoxicity activities...
October 21, 2016: Natural Product Research
W Xia, C D Mørch, D Matre, O K Andersen
BACKGROUND: This study aimed to explore conditioned pain modulation (CPM) effect on long-term potentiation (LTP)-like pain amplification induced by cutaneous 10-Hz conditioning electrical stimulation (CES). METHODS: Conditioned pain modulation was induced by cold pressor conditioning stimulus (CPCS) (4 °C) which was applied immediately before CES in the active session. In the control session, water with a temperature of 32 °C was used. Twenty subjects participated in two sessions in a randomized crossover design with at least 1-week interval...
October 20, 2016: European Journal of Pain: EJP
Clare F Heisey, J Derek Kingsley
Static stretching was once recognized as a method of preparation for physical activity that would inhibit performance and increase risk of injury. However, a growing body of research suggests that static stretching may not have an inhibitory effect. Regardless, the data have not examined gender differences or the fatigue index (FI) and flexibility effects of static stretching on the back squat over multiple sets. Therefore, the purpose of this study was to examine the relationship between a static-stretch condition (SC) and control condition (CC) on flexibility and the FI of Division I female athletes during 4 sets of the back squat...
2016: International Journal of Exercise Science
Karolina Niska, Narcyz Knap, Anna Kędzia, Maciej Jaskiewicz, Wojciech Kamysz, Iwona Inkielewicz-Stepniak
Objectives: In dentistry, silver nanoparticles (AgNPs) have drawn particular attention because of their wide antimicrobial activity spectrum. However, controversial information on AgNPs toxicity limited their use in oral infections. Therefore, the aim of the present study was to evaluate the antibacterial activities against a panel of oral pathogenic bacteria and bacterial biofilms together with potential cytotoxic effects on human gingival fibroblasts of 10 nm AgNPs: non-functionalized - uncapped (AgNPs-UC) as well as surface-functionalized with capping agent: lipoic acid (AgNPs-LA), polyethylene glycol (AgNPs-PEG) or tannic acid (AgNPs-TA) using silver nitrate (AgNO3) as control...
2016: International Journal of Medical Sciences
Sha-Sha Huang, Qiu-Bing Zhang, Qing-Yan Yuan, Si-Li He, Yuan-Ming Zhang
INTRODUCTION: Activation of T lymphocytes, for which potassium channels are essential, is involved in the development of hypertension. In this study, we explored the inhibitory effects of telmisartan on the culture and proliferation of and Kv1.3 potassium channel expression in peripheral blood CD4(+) T lymphocytes derived from Xinjiang Kazakh patients with hypertension. METHODS: CD4(+) T-cell samples from hypertensive Kazakh patients and healthy Kazakh people were divided into healthy control, case control, telmisartan, and 4-aminopytidine groups...
October 2016: Journal of the Renin-angiotensin-aldosterone System: JRAAS
Zhao-Hui Wang, Xia-Qing Guo, Qi-Shun Zhang, Jian-Lei Zhang, Yan-Li Duan, Guo-Fei Li, Dong-Lin Zheng
BACKGROUND AND AIM: Long non-coding RNAs have been confirmed to play a critical role in various cancers. In the present study, the effect of long non-coding RNA (lncRNA) CCAT1 on glioma cell proliferation and its potential mechanism were investigated. METHODS AND RESULTS: Real-time PCR results showed that lncRNA-CCAT1 expression was significantly upregulated in glioma cancer tissues and cell lines compared with controls. After inhibiting CCAT1 expression in glioma cell line U251 with siRNA-CCAT1 (si-CCAT1), the cell viability and cell colony formation were decreased, the cell cycle was arrested in G1 phase, and the cell apoptosis was increased...
October 17, 2016: Biochemical and Biophysical Research Communications
Jiankang Zhang, Lixin Gao, Jianjun Xi, Li Sheng, Yanmei Zhao, Lei Xu, Yidan Shao, Shourong Liu, Rangxiao Zhuang, Yubo Zhou, Jia Li
A series of novel non-covalent piperidine-containing dipeptidyl derivatives were designed, synthesized and evaluated as proteasome inhibitors. All target compounds were tested for their proteasome chymotrypsin-like inhibitory activities, and selected derivatives were evaluated for the anti-proliferation activities against two multiple myeloma (MM) cell lines RPMI 8226 and MM-1S. Among all of these compounds, eight exhibited significant proteasome inhibitory activities with IC50 less than 20nM, and four are more potent than the positive control Carfilzomib...
October 6, 2016: Bioorganic & Medicinal Chemistry
Liang Chen, Cornelis Johannes Kleverlaan, Kunneng Liang, Deqin Yang
STATEMENT OF PROBLEM: Polyvinyl siloxane impression material has been widely used as a lingual matrix for rebuilding missing tooth structure with composite resin. The composite resin is light polymerized in contact with the polyvinyl siloxane impression material. However, polyvinyl siloxane impression material has been shown to interact with other dental materials. PURPOSE: The purpose of this study was to assess the effect of polyvinyl siloxane impression materials on the polymerization of composite resins by assessing the Vickers microhardness and degree of conversion of polyvinyl siloxane...
October 17, 2016: Journal of Prosthetic Dentistry
Nicolás M Vázquez, Graciela Fiorilli, Paulo A Cáceres Guido, Silvia Moreno
BACKGROUND: Methicillin-resistant Staphylococcus aureus (MRSA) is resistant to different commonly used antibiotics, stressing the need for further strategies to treat this human pathogen with worldwide prevalence. The use of phytochemicals within the current pharmacology is a promising approach to enhance the antimicrobial activity of common antibiotics in the battle against these bacteria. PURPOSE: The purpose of this study was to determine the antimicrobial effectiveness of carnosic acid, the major constituent of Rosmarinus officinalis L...
November 15, 2016: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
Thomas J Younts, Hannah R Monday, Barna Dudok, Matthew E Klein, Bryen A Jordan, István Katona, Pablo E Castillo
Long-term changes of neurotransmitter release are critical for proper brain function. However, the molecular mechanisms underlying these changes are poorly understood. While protein synthesis is crucial for the consolidation of postsynaptic plasticity, whether and how protein synthesis regulates presynaptic plasticity in the mature mammalian brain remain unclear. Here, using paired whole-cell recordings in rodent hippocampal slices, we report that presynaptic protein synthesis is required for long-term, but not short-term, plasticity of GABA release from type 1 cannabinoid receptor (CB1)-expressing axons...
October 19, 2016: Neuron
Fumika Mi-Ichi, Hiroki Yoshida, Shinjiro Hamano
Amebiasis is caused by Entamoeba histolytica infection and can produce a broad range of clinical signs, from asymptomatic cases to patients with obvious symptoms. The current epidemiological and clinical statuses of amebiasis make it a serious public health problem worldwide. The Entamoeba life cycle consists of the trophozoite, the causative agent for amebiasis, and the cyst, the form responsible for transmission. These two stages are connected by "encystation" and "excystation." Hence, developing novel strategies to control encystation and excystation will potentially lead to new measures to block the transmission of amebiasis by interrupting the life cycle of the causative agent...
October 2016: PLoS Pathogens
Suman Kumar Nandy, Alpana Seal
Cystatin superfamily is a large group of evolutionarily related proteins involved in numerous physiological activities through their inhibitory activity towards cysteine proteases. Despite sharing the same cystatin fold, and inhibiting cysteine proteases through the same tripartite edge involving highly conserved N-terminal region, L1 and L2 loop; cystatins differ widely in their inhibitory affinity towards C1 family of cysteine proteases and molecular details of these interactions are still elusive. In this study, inhibitory interactions of human family 1 & 2 cystatins with cathepsin L1 are predicted and their stability and viability are verified through protein docking & comparative molecular dynamics...
2016: PloS One
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